Bryan l. Roth

Q: What Schools Are Affiliated With Bryan l. Roth

Bryan l. Roth is affiliated with the following schools: University of Illinois Chicago, Brown University, University of Melbourne, Virginia Commonwealth University, Georgetown University, Case Western Reserve University, University of North Carolina at Chapel Hill

Bryan l. Roth's AcademicInfluence.com Rankings

Bryan l. Roth

Medical

#837

World Rank

#1095

Historical Rank

Pharmacology

#53

World Rank

#72

Historical Rank

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Medical

Bryan l. Roth's Degrees

PhD Pharmacology University of North Carolina at Chapel Hill
Bachelors Chemistry University of North Carolina at Chapel Hill

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Bryan l. Roth's Published Works

Number of citations in a given year to any of this author's works

Total number of citations to an author for the works they published in a given year. This highlights publication of the most important work(s) by the author

Published Works

A SARS-CoV-2 Protein Interaction Map Reveals Targets for Drug-Repurposing (2020) (3012)
Evolving the lock to fit the key to create a family of G protein-coupled receptors potently activated by an inert ligand (2007) (1580)
Relating protein pharmacology by ligand chemistry (2007) (1502)
Morphometric evidence for neuronal and glial prefrontal cell pathology in major depression∗ ∗ See accompanying Editorial, in this issue. (1999) (1433)
The expanded biology of serotonin. (2009) (1431)
Predicting new molecular targets for known drugs (2009) (1424)
Rapid, reversible activation of AgRP neurons drives feeding behavior in mice. (2011) (1089)
Functional Selectivity and Classical Concepts of Quantitative Pharmacology (2007) (1078)
Magic shotguns versus magic bullets: selectively non-selective drugs for mood disorders and schizophrenia (2004) (1044)
DREADDs for Neuroscientists (2016) (1029)
Aripiprazole, A Novel Atypical Antipsychotic Drug with a Unique and Robust Pharmacology (2003) (867)
Parkin-deficient Mice Exhibit Nigrostriatal Deficits but Not Loss of Dopaminergic Neurons* (2003) (843)
Remote Control of Neuronal Activity in Transgenic Mice Expressing Evolved G Protein-Coupled Receptors (2009) (795)
Structure of the human kappa opioid receptor in complex with JDTic (2012) (684)
Structure-based discovery of opioid analgesics with reduced side effects (2016) (671)
Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors. (1994) (669)
Salvinorin A: A potent naturally occurring nonnitrogenous κ opioid selective agonist (2002) (654)
Automated design of ligands to polypharmacological profiles (2012) (651)
Evidence for Possible Involvement of 5-HT2B Receptors in the Cardiac Valvulopathy Associated With Fenfluramine and Other Serotonergic Medications (2000) (643)
H1-Histamine Receptor Affinity Predicts Short-Term Weight Gain for Typical and Atypical Antipsychotic Drugs (2003) (633)
The promise and peril of chemical probes. (2015) (623)
Structural Features for Functional Selectivity at Serotonin Receptors (2013) (604)
Endocrine Regulation of Male Fertility by the Skeleton (2011) (542)
Nigrostriatal Dopaminergic Deficits and Hypokinesia Caused by Inactivation of the Familial Parkinsonism-Linked Gene DJ-1 (2005) (517)
DREADDs (designer receptors exclusively activated by designer drugs): chemogenetic tools with therapeutic utility. (2015) (496)
Coupling of Inositol Phospholipid Metabolism with Excitatory Amino Acid Recognition Sites in Rat Hippocampus (1986) (470)
Structure of the Nociceptin/Orphanin FQ Receptor in Complex with a Peptide Mimetic (2012) (466)
Structure of the human smoothened receptor bound to an antitumour agent (2013) (462)
Structural Basis for Molecular Recognition at Serotonin Receptors (2013) (460)
A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells. (2011) (459)
The Human Polyomavirus, JCV, Uses Serotonin Receptors to Infect Cells (2004) (448)
Ultra-large library docking for discovering new chemotypes (2019) (441)
Drugs and valvular heart disease. (2007) (439)
PRESTO-TANGO: an open-source resource for interrogation of the druggable human GPCR-ome (2015) (406)
Molecular control of δ-opioid receptor signalling (2014) (403)
An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1. (2013) (401)
Chemogenetic tools to interrogate brain functions. (2014) (378)
Allosteric sodium in class A GPCR signaling. (2014) (373)
Cloning, Characterization, and Chromosomal Localization of a Human 5‐HT6 Serotonin Receptor (1996) (366)
G-protein-coupled receptors at a glance (2003) (361)
Discovery of a novel member of the histamine receptor family. (2001) (356)
How Ligands Illuminate GPCR Molecular Pharmacology (2017) (354)
Topoisomerase inhibitors unsilence the dormant allele of Ube3a in neurons (2011) (326)
Serotonin 5‐HT2A receptors are expressed on pyramidal cells and interneurons in the rat cortex (1997) (318)
Discovery of β-Arrestin–Biased Dopamine D2 Ligands for Probing Signal Transduction Pathways Essential for Antipsychotic Efficacy (2011) (316)
Remote Control of Neuronal Signaling (2011) (315)
Inhibition of Mediodorsal Thalamus Disrupts Thalamofrontal Connectivity and Cognition (2013) (313)
The Multiplicity of Serotonin Receptors: Uselessly Diverse Molecules or an Embarrassment of Riches? (2000) (305)
Structure of the human k-opioid receptor in complex with JDTic (2012) (305)
Control of Serotonergic Function in Medial Prefrontal Cortex by Serotonin-2A Receptors through a Glutamate-Dependent Mechanism (2001) (305)
Salvinorin A: a potent naturally occurring nonnitrogenous kappa opioid selective agonist. (2002) (298)
STRUCTURE OF THE D2 DOPAMINE RECEPTOR BOUND TO THE ATYPICAL ANTIPSYCHOTIC DRUG RISPERIDONE (2018) (296)
N-Desalkylquetiapine, a Potent Norepinephrine Reuptake Inhibitor and Partial 5-HT1A Agonist, as a Putative Mediator of Quetiapine's Antidepressant Activity (2008) (289)
3,4-methylenedioxymethamphetamine (MDMA, "Ecstasy") induces fenfluramine-like proliferative actions on human cardiac valvular interstitial cells in vitro. (2003) (286)
Ligand Discovery from a Dopamine D3 Receptor Homology Model and Crystal Structure (2011) (285)
A New DREADD Facilitates the Multiplexed Chemogenetic Interrogation of Behavior (2015) (284)
A chemical-genetic approach to study G protein regulation of β cell function in vivo (2009) (283)
Paradoxical trafficking and regulation of 5-HT2A receptors by agonists and antagonists (2001) (276)
5-Hydroxytryptamine2-family receptors (5-hydroxytryptamine2A, 5-hydroxytryptamine2B, 5-hydroxytryptamine2C): where structure meets function. (1998) (274)
Crystal Structure of an LSD-Bound Human Serotonin Receptor (2017) (273)
Morphine paradoxically prolongs neuropathic pain in rats by amplifying spinal NLRP3 inflammasome activation (2016) (263)
Amisulpride is a potent 5-HT7 antagonist: relevance for antidepressant actions in vivo (2009) (259)
Molecular biology of serotonin receptors structure and function at the molecular level. (2002) (258)
Serotonin receptors represent highly favorable molecular targets for cognitive enhancement in schizophrenia and other disorders (2004) (255)
Structure of the Nanobody-Stabilized Active State of the Kappa Opioid Receptor (2018) (247)
Comprehensive characterization of the Published Kinase Inhibitor Set (2016) (246)
Structure and function of serotonin G protein-coupled receptors. (2015) (238)
Unexplored therapeutic opportunities in the human genome (2018) (238)
Pharmacogenetic Modulation of Orexin Neurons Alters Sleep/Wakefulness States in Mice (2011) (229)
Structural basis for Smoothened receptor modulation and chemoresistance to anticancer drugs (2014) (225)
Molecular targets for treating cognitive dysfunction in schizophrenia. (2007) (223)
Engineering GPCR signaling pathways with RASSLs (2008) (220)
Finding New Tricks For Old Drugs: An Efficient Route For Public-Sector Drug Discovery (2005) (215)
Salvinorin A, an Active Component of the Hallucinogenic Sage Salvia divinorum Is a Highly Efficacious κ-Opioid Receptor Agonist: Structural and Functional Considerations (2004) (205)
Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP. (2013) (197)
In silico design of novel probes for the atypical opioid receptor MRGPRX2 (2016) (191)
Multiple serotonin receptors: clinical and experimental aspects. (1994) (191)
Evidence for the Involvement of Dopamine Transporters in Behavioral Stimulant Effects of Modafinil (2009) (187)
Strategies to discover unexpected targets for drugs active at G protein-coupled receptors. (2011) (187)
Allosteric ligands for the pharmacologically dark receptors GPR68 and GPR65 (2015) (186)
Evidence for the Preferential Involvement of 5-HT2A Serotonin Receptors in Stress- and Drug-Induced Dopamine Release in the Rat Medial Prefrontal Cortex (2006) (183)
CRF RECEPTOR1 REGULATES ANXIETY BEHAVIOUR VIA SENSITIZATION OF 5-HT2 RECEPTOR SIGNALING (2010) (182)
Serotonin receptors and heart valve disease--it was meant 2B. (2011) (181)
Caveolin-1 Interacts with 5-HT2A Serotonin Receptors and Profoundly Modulates the Signaling of Selected Gαq-coupled Protein Receptors* (2004) (177)
The pipeline and future of drug development in schizophrenia (2007) (175)
Structure of a Hallucinogen-Activated Gq-Coupled 5-HT2A Serotonin Receptor (2020) (172)
In Vitro Characterization of Ephedrine-Related Stereoisomers at Biogenic Amine Transporters and the Receptorome Reveals Selective Actions as Norepinephrine Transporter Substrates (2003) (171)
Evidence for a Model of Agonist-induced Activation of 5-Hydroxytryptamine 2A Serotonin Receptors That Involves the Disruption of a Strong Ionic Interaction between Helices 3 and 6* 210 (2002) (171)
“TRUPATH, an Open-Source Biosensor Platform for Interrogating the GPCR Transducerome” (2020) (167)
Localization of 5-HT2A receptors on dopamine cells in subnuclei of the midbrain A10 cell group (2002) (162)
D4 dopamine receptor high-resolution structures enable the discovery of selective agonists (2017) (161)
5-HT2C Receptor Structures Reveal the Structural Basis of GPCR Polypharmacology (2018) (160)
A Direct Interaction of PSD-95 with 5-HT2A Serotonin Receptors Regulates Receptor Trafficking and Signal Transduction* (2003) (158)
Rapid modulation of spine morphology by the 5-HT2A serotonin receptor through kalirin-7 signaling (2009) (158)
Neurochemical profiles of some novel psychoactive substances. (2013) (156)
Structural basis for bifunctional peptide recognition at human δ-Opioid receptor (2015) (155)
The G Protein–Biased κ-Opioid Receptor Agonist RB-64 Is Analgesic with a Unique Spectrum of Activities In Vivo (2015) (155)
The Dynamin-dependent, Arrestin-independent Internalization of 5-Hydroxytryptamine 2A (5-HT2A) Serotonin Receptors Reveals Differential Sorting of Arrestins and 5-HT2A Receptors during Endocytosis* 210 (2001) (154)
Salvinorin A: the "magic mint" hallucinogen finds a molecular target in the kappa opioid receptor. (2003) (154)
Inverse agonist actions of typical and atypical antipsychotic drugs at the human 5-hydroxytryptamine(2C) receptor. (2001) (152)
Aripiprazole: a novel atypical antipsychotic drug with a uniquely robust pharmacology. (2006) (152)
Clozapine and other 5-hydroxytryptamine-2A receptor antagonists alter the subcellular distribution of 5-hydroxytryptamine-2A receptors in vitro and in vivo (1999) (146)
Identifying mechanism-of-action targets for drugs and probes (2012) (145)
5-Hydroxytryptamine2 receptors coupled to phospholipase C in rat aorta: modulation of phosphoinositide turnover by phorbol ester. (1986) (141)
WAY-100635 is a potent dopamine D4 receptor agonist (2006) (141)
Aortic recognition sites for serotonin (5HT) are coupled to phospholipase C and modulate phosphatidylinositol turnover (1984) (140)
Identification of conserved aromatic residues essential for agonist binding and second messenger production at 5-hydroxytryptamine2A receptors. (1997) (134)
Involvement of AMPA receptor phosphorylation in antidepressant actions with special reference to tianeptine (2007) (134)
Interactions of selective serotonin reuptake inhibitors with the serotonin 5-HT2C receptor (1996) (130)
The Ketamine Analogue Methoxetamine and 3- and 4-Methoxy Analogues of Phencyclidine Are High Affinity and Selective Ligands for the Glutamate NMDA Receptor (2013) (129)
2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors. (2000) (129)
Directed molecular evolution of DREADDs: a generic approach to creating next-generation RASSLs (2010) (128)
Pharmacologic manipulation of the peripheral vasculature in shock: clinical and experimental approaches. (1986) (128)
Identification of Novel Functionally Selective κ-Opioid Receptor Scaffolds (2014) (125)
Developmental regulation of 5-HT2 and 5-HT1c mRNA and receptor levels. (1991) (124)
Parallel Functional Activity Profiling Reveals Valvulopathogens Are Potent 5-Hydroxytryptamine2B Receptor Agonists: Implications for Drug Safety Assessment (2009) (123)
The highly efficacious actions of N-desmethylclozapine at muscarinic receptors are unique and not a common property of either typical or atypical antipsychotic drugs: is M1 agonism a pre-requisite for mimicking clozapine’s actions? (2005) (123)
Modulation of the autonomic nervous system and behaviour by acute glial cell Gq protein‐coupled receptor activation in vivo (2013) (123)
A cellular chemical probe targeting the chromodomains of Polycomb Repressive Complex 1 (2015) (122)
Cre‐dependent DREADD (Designer Receptors Exclusively Activated by Designer Drugs) mice (2016) (122)
Chemogenetic Inactivation of Ventral Hippocampal Glutamatergic Neurons Disrupts Consolidation of Contextual Fear Memory (2014) (121)
Virtual discovery of melatonin receptor ligands to modulate circadian rhythms (2020) (121)
Phasic and tonic components in 5-HT2 receptor-mediated rat aorta contraction: participation of Ca++ channels and phospholipase C. (1985) (120)
Multiple mechanisms of serotonergic signal transduction. (1987) (120)
Mice with altered serotonin 2C receptor RNA editing display characteristics of Prader–Willi syndrome (2010) (120)
Discovery of Human Signaling Systems: Pairing Peptides to G Protein-Coupled Receptors (2019) (119)
Structure-inspired design of β-arrestin-biased ligands for aminergic GPCRs (2017) (119)
Elucidation of The Behavioral Program and Neuronal Network Encoded by Dorsal Raphe Serotonergic Neurons (2016) (118)
Structure-functional selectivity relationship studies of β-arrestin-biased dopamine D₂ receptor agonists. (2012) (116)
The First Structure–Activity Relationship Studies for Designer Receptors Exclusively Activated by Designer Drugs (2015) (114)
Serotonin 5-HT2A receptors: molecular biology and mechanisms of regulation. (1998) (114)
Differential modes of agonist binding to 5-hydroxytryptamine(2A) serotonin receptors revealed by mutation and molecular modeling of conserved residues in transmembrane region 5. (2000) (114)
A highly conserved aspartic acid (Asp-155) anchors the terminal amine moiety of tryptamines and is involved in membrane targeting of the 5-HT(2A) serotonin receptor but does not participate in activation via a "salt-bridge disruption" mechanism. (2000) (113)
A Gαs DREADD Mouse for Selective Modulation of cAMP Production in Striatopallidal Neurons (2013) (113)
A single point mutation (Phe340-->Leu340) of a conserved phenylalanine abolishes 4-[125I]iodo-(2,5-dimethoxy)phenylisopropylamine and [3H]mesulergine but not [3H]ketanserin binding to 5-hydroxytryptamine2 receptors. (1993) (113)
Translating genome-wide association findings into new therapeutics for psychiatry (2016) (113)
PSD-95 Is Essential for Hallucinogen and Atypical Antipsychotic Drug Actions at Serotonin Receptors (2009) (112)
Studies toward the pharmacophore of salvinorin A, a potent kappa opioid receptor agonist. (2005) (111)
New Insights into the Function of M4 Muscarinic Acetylcholine Receptors Gained Using a Novel Allosteric Modulator and a DREADD (Designer Receptor Exclusively Activated by a Designer Drug) (2008) (110)
Chemical Informatics and Target Identification in a Zebrafish Phenotypic Screen (2011) (110)
Distinct cortical and striatal actions of a β-arrestin–biased dopamine D2 receptor ligand reveal unique antipsychotic-like properties (2016) (108)
Differential postnatal development of mu and delta opiate receptors. (1982) (106)
Rapid agonist-induced internalization of the 5-hydroxytryptamine2A receptor occurs via the endosome pathway in vitro. (1996) (105)
Deschloroclozapine, a potent and selective chemogenetic actuator enables rapid neuronal and behavioral modulations in mice and monkeys (2019) (105)
Elevation of arterial pressure in rats by two new vertebrate peptides FLF QPQRF-NH2 and AGE GLSSPFWSLAAPQRF-NH2 which are immunoreactive to FMRF-NH2 antiserum (1987) (105)
Pharmacosynthetics: Reimagining the pharmacogenetic approach (2013) (102)
The serotonin receptors : from molecular pharmacology to human therapeutics (2006) (102)
Antinociceptive and Hypothermic Effects of Salvinorin A Are Abolished in a Novel Strain of κ-Opioid Receptor-1 Knockout Mice (2006) (102)
DREADD Agonist 21 Is an Effective Agonist for Muscarinic-Based DREADDs in Vitro and in Vivo (2018) (102)
Imidazoline receptor antisera-selected (IRAS) cDNA: cloning and characterization. (2000) (101)
Zebrafish behavioral profiling identifies multi-target antipsychotic-like compounds (2016) (101)
Conformation Guides Molecular Efficacy in Docking Screens of Activated β-2 Adrenergic G Protein Coupled Receptor (2013) (101)
In vitro receptor screening of pure constituents of St. John's wort reveals novel interactions with a number of GPCRs (2002) (101)
l-Homocysteine Sulfinic Acid and Other Acidic Homocysteine Derivatives Are Potent and Selective Metabotropic Glutamate Receptor Agonists (2003) (100)
Structure and Function of the Third Intracellular Loop of the 5‐Hydroxytryptamine2A Receptor: The Third Intracellular Loop Is α‐Helical and Binds Purified Arrestins (1999) (97)
Salvinorin A: from natural product to human therapeutics. (2006) (96)
Novel Inhibitors of Human Histone Deacetylase (HDAC) Identified by QSAR Modeling of Known Inhibitors, Virtual Screening, and Experimental Validation (2009) (96)
Identification of the molecular mechanisms by which the diterpenoid salvinorin A binds to kappa-opioid receptors. (2005) (95)
Screening the receptorome to discover the molecular targets for plant-derived psychoactive compounds: a novel approach for CNS drug discovery. (2004) (95)
5-Hydroxytryptamine2A (5-HT2A) receptor desensitization can occur without down-regulation. (1995) (94)
Intra-islet glucagon signaling is critical for maintaining glucose homeostasis. (2019) (93)
Photochemical activation of TRPA1 channels in neurons and animals (2013) (91)
A Pharmacological Organization of G Protein-coupled Receptors (2012) (91)
A potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3). (2015) (91)
Lorcaserin and pimavanserin: emerging selectivity of serotonin receptor subtype-targeted drugs. (2013) (90)
Cell-type specific effects of endocytosis inhibitors on 5-hydroxytryptamine2A receptor desensitization and resensitization reveal an arrestin-, GRK2-, and GRK5-independent mode of regulation in human embryonic kidney 293 cells (2001) (89)
Atypical antipsychotic drug actions: unitary or multiple mechanisms for ‘atypicality’? (2003) (89)
Role of kappa-opioid receptors in the effects of salvinorin A and ketamine on attention in rats (2010) (87)
Colloidal Aggregation Causes Inhibition of G Protein-Coupled Receptors (2013) (87)
Similar ultrastructural distribution of the 5-HT2A serotonin receptor and microtubule-associated protein MAP1A in cortical dendrites of adult rat (2002) (87)
Differential ergoline and ergopeptine binding to 5-hydroxytryptamine2A receptors: ergolines require an aromatic residue at position 340 for high affinity binding. (1995) (85)
Structural insights into the human D1 and D2 dopamine receptor signaling complexes (2021) (84)
Mining the Receptorome* (2005) (83)
Development of a Rationally Designed, Low Abuse Potential, Biogenic Amine Releaser That Suppresses Cocaine Self-Administration (2005) (83)
Structural determinants of 5-HT2B receptor activation and biased agonism (2018) (83)
Caveolin-1 and Lipid Microdomains Regulate Gs Trafficking and Attenuate Gs/Adenylyl Cyclase Signaling (2009) (82)
Novel Molecular Targets of Dezocine and Their Clinical Implications (2014) (81)
XFEL structures of the human MT2 melatonin receptor reveal basis of subtype selectivity (2019) (81)
Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonists; search for cocaine medications. (2006) (80)
Evidence for distinct subcellular sites of opiate receptors. Demonstration of opiate receptors in smooth microsomal fractions isolated from rat brain. (1981) (79)
N1-(Benzenesulfonyl)tryptamines as novel 5-HT6 antagonists. (2000) (78)
Targeting the histone methyltransferase G9a activates imprinted genes and improves survival of a mouse model of Prader–Willi syndrome (2016) (78)
DREADDs: novel tools for drug discovery and development. (2014) (77)
Effect of the R(−) and S(+) isomers of MDA and MDMA on phosphotidyl inositol turnover in cultured cells expressing 5-HT2A or 5-HT2C receptors (1994) (76)
DREADD: A Chemogenetic GPCR Signaling Platform (2014) (75)
High-affinity agonist binding is not sufficient for agonist efficacy at 5-hydroxytryptamine2A receptors: evidence in favor of a modified ternary complex model. (1997) (75)
The PDZ-binding domain is essential for the dendritic targeting of 5-HT2A serotonin receptors in cortical pyramidal neurons in vitro (2003) (75)
Engineered GPCRs as tools to modulate signal transduction. (2008) (75)
Structural basis of ligand recognition at the human MT1 melatonin receptor (2019) (75)
Discovery of new GPCR ligands to illuminate new biology. (2017) (73)
Antagonist Functional Selectivity: 5-HT2A Serotonin Receptor Antagonists Differentially Regulate 5-HT2A Receptor Protein Level In Vivo (2011) (73)
International Union of Basic and Clinical Pharmacology. CX. Classification of Receptors for 5-hydroxytryptamine; Pharmacology and Function (2020) (72)
Novel Diketopiperazine Enhances Motor and Cognitive Recovery after Traumatic Brain Injury in Rats and Shows Neuroprotection In Vitro and In Vivo (2003) (72)
Direct-Pathway Striatal Neurons Regulate the Retention of Decision-Making Strategies (2013) (72)
Opportunities and Challenges of Psychiatric Drug Discovery: Roles for Scientists in Academic, Industry, and Government Settings (2008) (71)
Nanobody-enabled monitoring of kappa opioid receptor states (2020) (71)
NMR structure and dynamics of the agonist dynorphin peptide bound to the human kappa opioid receptor (2015) (70)
Structure-based design, synthesis, and biochemical and pharmacological characterization of novel salvinorin A analogues as active state probes of the kappa-opioid receptor. (2009) (70)
Agonist high and low affinity state ratios predict drug intrinsic activity and a revised Ternary complex mechanism at serotonin 5‐HT2A and 5‐HT2C receptors (2000) (69)
Chronic mianserin treatment decreases 5-HT2 receptor binding without altering 5-HT2 receptor mRNA levels. (1991) (69)
Marine algal toxin azaspiracid is an open-state blocker of hERG potassium channels. (2012) (69)
Identification of human Ether-à-go-go related gene modulators by three screening platforms in an academic drug-discovery setting. (2010) (69)
Low nNOS protein in the locus coeruleus in major depression (2004) (68)
Screening the receptorome: an efficient approach for drug discovery and target validation. (2006) (68)
Synthon-based ligand discovery in virtual libraries of over 11 billion compounds (2021) (68)
Pharmacological characterization of novel synthetic opioids (NSO) found in the recreational drug marketplace (2017) (67)
Harnessing Ion-Binding Sites for GPCR Pharmacology (2019) (66)
Structural Determinants of G-protein α Subunit Selectivity by Regulator of G-protein Signaling 2 (RGS2)* (2009) (65)
Selective κ Opioid Antagonists nor-BNI, GNTI and JDTic Have Low Affinities for Non-Opioid Receptors and Transporters (2013) (65)
Molecular Determinants for the Interaction of the Valvulopathic Anorexigen Norfenfluramine with the 5-HT2B Receptor (2005) (65)
Silencing Synapses with DREADDs (2014) (65)
The Presynaptic Component of the Serotonergic System is Required for Clozapine's Efficacy (2011) (64)
Engineered G-protein Coupled Receptors are Powerful Tools to Investigate Biological Processes and Behaviors (2009) (64)
A simple representation of three-dimensional molecular structure (2017) (63)
The interaction of a constitutively active arrestin with the arrestin-insensitive 5-HT(2A) receptor induces agonist-independent internalization. (2003) (63)
Life beyond kinases: structure-based discovery of sorafenib as nanomolar antagonist of 5-HT receptors. (2012) (63)
Design, synthesis, and validation of a β-turn mimetic library targeting protein-protein and peptide-receptor interactions. (2011) (63)
Isoquinoline Alkaloids Isolated from Corydalis yanhusuo and Their Binding Affinities at the Dopamine D1 Receptor (2008) (62)
Distribution of serotonin 5‐HT2A receptors in afferents of the rat striatum (2001) (61)
The anthelmintic praziquantel is a human serotoninergic G-protein-coupled receptor ligand (2017) (60)
Anxiolytic-like effects of 8-acetylene imidazobenzodiazepines in a rhesus monkey conflict procedure (2010) (59)
Serotonergic Antagonist Effects on Trafficking of Serotonin 5‐HT2A Receptors in Vitro and in Vivo a (1998) (59)
Activation of phosphatidylinositol turnover in rat aorta by α1-adrenergic receptor stimulation (1985) (59)
G protein-coupled receptor (GPCR) trafficking in the central nervous system: relevance for drugs of abuse. (1998) (58)
Integrated Approaches for Genome-wide Interrogation of the Druggable Non-olfactory G Protein-coupled Receptor Superfamily* (2015) (58)
Discovery of β2 Adrenergic Receptor Ligands Using Biosensor Fragment Screening of Tagged Wild-Type Receptor (2013) (58)
Securinine, a Myeloid Differentiation Agent with Therapeutic Potential for AML (2011) (58)
Salvinorin A: A novel and highly selective κ-opioid receptor agonist (2004) (58)
1-(2,5-Dimethoxy-4-(trifluoromethyl)phenyl)-2-aminopropane: a potent serotonin 5-HT2A/2C agonist. (1994) (58)
COVID-19: Famotidine, Histamine, Mast Cells, and Mechanisms (2020) (57)
Antiseizure activity of novel gamma-aminobutyric acid (A) receptor subtype-selective benzodiazepine analogues in mice and rat models. (2009) (57)
Structure, function and pharmacology of human itch GPCRs (2021) (56)
The TLQP-21 peptide activates the G-protein-coupled receptor C3aR1 via a folding-upon-binding mechanism. (2014) (56)
Donated chemical probes for open science (2018) (56)
Massively parallel screening of the receptorome. (2008) (56)
Structures of the σ2 receptor enable docking for bioactive ligand discovery (2021) (55)
Identification of receptor domains that modify ligand binding to 5-hydroxytryptamine2 and 5-hydroxytryptamine1c serotonin receptors. (1992) (55)
Fluorinated diaryl sulfides as serotonin transporter ligands: synthesis, structure-activity relationship study, and in vivo evaluation of fluorine-18-labeled compounds as PET imaging agents. (2005) (55)
SAR of psilocybin analogs: discovery of a selective 5-HT 2C agonist. (2005) (54)
New Technologies for Elucidating Opioid Receptor Function. (2016) (54)
A chemical-genetic approach for precise spatio-temporal control of cellular signaling. (2010) (53)
A structure-affinity study of the binding of 4-substituted analogues of 1-(2,5-dimethoxyphenyl)-2-aminopropane at 5-HT2 serotonin receptors. (1990) (52)
Phorbol esters inhibit alpha 1-adrenergic receptor-stimulated phosphoinositide hydrolysis and contraction in rat aorta: evidence for a link between vascular contraction and phosphoinositide turnover. (1986) (51)
Irving Page Lecture: 5-HT2A serotonin receptor biology: Interacting proteins, kinases and paradoxical regulation (2011) (51)
Structural insights into the extracellular recognition of the human serotonin 2B receptor by an antibody (2017) (50)
VEGAS as a Platform for Facile Directed Evolution in Mammalian Cells (2019) (50)
Behavioral and Physiological Effects of a Novel Kappa-Opioid Receptor-Based DREADD in Rats (2016) (49)
Identification of two serine residues essential for agonist-induced 5-HT2A receptor desensitization. (2003) (49)
Noradrenergic Synaptic Function in the Bed Nucleus of the Stria Terminalis Varies in Animal Models of Anxiety and Addiction (2013) (48)
Regulation of 5-HT2 and 5-HT1C serotonin receptor levels. Methodology and mechanisms. (1990) (48)
Serotonin-2C and -2a receptor co-expression on cells in the rat medial prefrontal cortex (2015) (48)
Insights into the regulation of 5-HT2A serotonin receptors by scaffolding proteins and kinases (2008) (48)
Binding of typical and atypical antipsychotic drugs to multiple neurotransmitter receptors. (1998) (48)
Galpha-subunits differentially alter the conformation and agonist affinity of kappa-opioid receptors. (2008) (48)
Altered hepatic vasopressin and alpha 1-adrenergic receptors after chronic endotoxin infusion. (1987) (48)
p90 ribosomal S6 kinase 2 exerts a tonic brake on G protein-coupled receptor signaling. (2006) (47)
The Neurotensin Agonist PD149163 Increases Fos Expression in the Prefrontal Cortex of the Rat (2004) (47)
Improvement of pharmacological properties of irreversible thyroid receptor coactivator binding inhibitors. (2009) (46)
SK&F 83822 distinguishes adenylyl cyclase from phospholipase C-coupled dopamine D1-like receptors: behavioural topography. (2004) (46)
Novel positive allosteric modulators of GABAA receptors: Do subtle differences in activity at α1 plus α5 versus α2 plus α3 subunits account for dissimilarities in behavioral effects in rats? (2010) (46)
Chemotype-selective Modes of Action of κ-Opioid Receptor Agonists* (2013) (45)
Rat Brain Protein Kinase C: Purification, Antibody Production, and Quantification in Discrete Regions of Hippocampus (1989) (45)
Pharmacologic analysis of non-synonymous coding h5-HT2A SNPs reveals alterations in atypical antipsychotic and agonist efficacies (2006) (45)
Selective 5-hydroxytryptamine 2C receptor agonists derived from the lead compound tranylcypromine: identification of drugs with antidepressant-like action. (2009) (45)
The activities of drug inactive ingredients on biological targets (2020) (45)
XFEL structures of the human MT2 melatonin receptor reveal the basis of subtype selectivity (2019) (44)
Discovery of G Protein-Biased D2 Dopamine Receptor Partial Agonists. (2016) (44)
Effects of a phorbol ester on rat aortic contraction and calcium influx in the presence and absence of BAY k 8644. (1987) (44)
Unexplored therapeutic opportunities in the human genome (2018) (44)
Quantitative Analysis of Focused A-To-I RNA Editing Sites by Ultra-High-Throughput Sequencing in Psychiatric Disorders (2012) (43)
N-Methylacetamide Analog of Salvinorin A: A Highly Potent and Selective κ-Opioid Receptor Agonist with Oral Efficacy (2008) (43)
A SARS-CoV-2 protein interaction map reveals targets for drug repurposing (2020) (43)
Pimavanserin tartrate: a 5-HT2A inverse agonist with potential for treating various neuropsychiatric disorders. (2008) (42)
Differential Helical Orientations among Related G Protein-coupled Receptors Provide a Novel Mechanism for Selectivity (2007) (42)
Cell-type specific effects of endocytosis inhibitors on 5-hydroxytryptamine(2A) receptor desensitization and resensitization reveal an arrestin-, GRK2-, and GRK5-independent mode of regulation in human embryonic kidney 293 cells. (2001) (41)
1,2,3,4-tetrahydrocarbazoles as 5-HT6 serotonin receptor ligands. (2004) (41)
DREADDs in Drosophila: a pharmacogenetic approach for controlling behavior, neuronal signaling, and physiology in the fly. (2013) (41)
Prostaglandins activate phosphoinositide metabolism in rat aorta. (1987) (41)
Screening the receptorome reveals molecular targets responsible for drug-induced side effects: focus on ‘fen–phen’ (2005) (40)
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one. (2008) (39)
Chemocentric informatics approach to drug discovery: identification and experimental validation of selective estrogen receptor modulators as ligands of 5-hydroxytryptamine-6 receptors and as potential cognition enhancers. (2012) (38)
Structure-Based Discovery of New Antagonist and Biased Agonist Chemotypes for the Kappa Opioid Receptor. (2017) (38)
Hepatic alpha 1-adrenergic receptor alteration in a rat model of chronic sepsis. (1986) (38)
Binding of isotryptamines and indenes at h5-HT6 serotonin receptors. (2005) (38)
The promises and perils of psychedelic pharmacology for psychiatry (2022) (38)
Pimavanserin tartrate: a 5-HT2A inverse agonist with potential for treating various neuropsychiatric disorders (2008) (37)
Insights into the structure and function of 5-HT2 familyserotonin receptors reveal novel strategies for therapeutic target development (2001) (37)
Production and characterization of a specific 5-HT2 receptor antibody (1993) (37)
Synthesis, pharmacological characterization, and structure-activity relationship studies of small molecular agonists for the orphan GPR88 receptor. (2014) (36)
5-HT2C Agonists Modulate Schizophrenia-Like Behaviors in Mice (2017) (36)
Structures of the human dopamine D3 receptor-Gi complexes. (2021) (36)
Intestinal epithelial cell-derived μ-opioid signaling protects against ischemia reperfusion injury through PI3K signaling. (2013) (35)
Development, validation, and use of quantitative structure-activity relationship models of 5-hydroxytryptamine (2B) receptor ligands to identify novel receptor binders and putative valvulopathic compounds among common drugs. (2010) (35)
Ribosomal S6 Kinase 2 Directly Phosphorylates the 5-Hydroxytryptamine 2A (5-HT2A) Serotonin Receptor, Thereby Modulating 5-HT2A Signaling* (2009) (35)
Assessing serotonin receptor mRNA editing frequency by a novel ultra high-throughput sequencing method (2010) (35)
Alterations in rat aortic alpha 1-adrenoceptors and alpha 1-adrenergic stimulated phosphoinositide hydrolysis in intraperitoneal sepsis. (1988) (35)
Molecular Determinants in the Second Intracellular Loop of the 5-Hydroxytryptamine-1A Receptor for G-Protein Coupling (2006) (35)
Discovery and Characterization of Novel GPR39 Agonists Allosterically Modulated by Zinc (2016) (35)
Synthesis and receptor assay of aromatic-ethynyl-aromatic derivatives with potent mGluR5 antagonist activity. (2005) (34)
A Miniaturized Screen of a Schistosoma mansoni Serotonergic G Protein-Coupled Receptor Identifies Novel Classes of Parasite-Selective Inhibitors (2016) (34)
Stereospecific opiate-binding sites occur in coated vesicles (1985) (33)
Salvinorin A: a novel and highly selective kappa-opioid receptor agonist. (2004) (33)
Hallucinogen actions on human brain revealed (2012) (33)
Why mice are neither miniature humans nor small rats: a cautionary tale involving 5-hydroxytryptamine-6 serotonin receptor species variants. (2003) (33)
Community guidelines for GPCR ligand bias: IUPHAR review 32 (2022) (33)
Mechanism of dopamine binding and allosteric modulation of the human D1 dopamine receptor (2021) (32)
Chemogenetics-A Transformational and Translational Platform. (2015) (32)
Binding of serotonin and N1-benzenesulfonyltryptamine-related analogs at human 5-HT6 serotonin receptors: receptor modeling studies. (2008) (32)
5-HT6 serotonin receptor binding of indolealkylamines: A preliminary structure-affinity investigation (1999) (32)
Deorphanization of Novel Peptides and Their Receptors (2010) (31)
Synthesis of a library of complex macrodiolides employing cyclodimerization of hydroxy esters. (2005) (31)
Sigma-1 receptor ligands control a switch between passive and active threat responses (2016) (31)
Schizophrenia risk gene CAV1 is both pro-psychotic and required for atypical antipsychotic drug actions in vivo (2011) (31)
An analysis of the synthetic tryptamines AMT and 5-MeO-DALT: emerging 'Novel Psychoactive Drugs'. (2013) (30)
Activation is Hallucinogenic and Antagonism is Therapeutic: Role of 5-HT2A Receptors in Atypical Antipsychotic Drug Actions (1999) (30)
Design, synthesis, and subtype selectivity of 3,6-disubstituted β-carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents for treatment of alcohol abuse. (2010) (30)
Labdane diterpenoids from Leonotis leonurus. (2013) (30)
A Last GASP for GPCRs? (2002) (30)
Arresting serotonin (2008) (30)
Genetic Deletion of p90 Ribosomal S6 Kinase 2 Alters Patterns of 5-Hydroxytryptamine2A Serotonin Receptor Functional Selectivity (2010) (30)
Functionalization at position 3 of the phenyl ring of the potent mGluR5 noncompetitive antagonists MPEP. (2005) (30)
The medicinal chemistry of 5-HT6 receptor ligands with a focus on arylsulfonyltryptamine analogs. (2010) (30)
Receptor Reserve Moderates Mesolimbic Responses to Opioids in a Humanized Mouse Model of the OPRM1 A118G Polymorphism (2015) (30)
Michael acceptor approach to the design of new salvinorin A-based high affinity ligands for the kappa-opioid receptor. (2012) (29)
Microsomal Opiate Receptors: Characterization of Smooth Microsomal and Synaptic Membrane Opiate Receptors (1984) (29)
Molecular pharmacology of metabotropic receptors targeted by neuropsychiatric drugs (2019) (29)
Binding of sulfonyl-containing arylalkylamines at human 5-HT6 serotonin receptors. (2006) (28)
Potential modes of interaction of 9-aminomethyl-9,10-dihydroanthracene (AMDA) derivatives with the 5-HT2A receptor: a ligand structure-affinity relationship, receptor mutagenesis and receptor modeling investigation. (2008) (28)
Synthesis and binding studies of 2-arylapomorphines. (2005) (28)
Tuning up the right signal: chemical and genetic approaches to study GPCR functions. (2014) (28)
Rational design, synthesis, and biological evaluation of rigid pyrrolidone analogues as potential inhibitors of prostate cancer cell growth. (2001) (28)
Three putative N‐glycosylation sites within the murine 5‐HT3A receptor sequence affect plasma membrane targeting, ligand binding, and calcium influx in heterologous mammalian cells (2004) (28)
Convenient synthesis and in vitro pharmacological activity of 2-thioanalogs of salvinorins A and B. (2007) (28)
Bespoke library docking for 5-HT2A receptor agonists with antidepressant activity (2022) (27)
Biased signaling of the proton‐sensing receptor OGR1 by benzodiazepines (2017) (27)
Biased ligands at opioid receptors: Current status and future directions (2021) (27)
The postnatal development of VIP binding sites in rat forebrain and hindbrain (1985) (27)
Conformational Ensembles in GPCR Activation (2013) (27)
Modulation of phosphatidylinositol-4,5-bisphosphate hydrolysis in rat aorta by guanine nucleotides, calcium and magnesium. (1987) (27)
Synthesis and receptor profiling of Stemona alkaloid analogues reveal a potent class of sigma ligands (2011) (27)
Kappa-opioid receptor-selective dicarboxylic ester-derived salvinorin A ligands. (2013) (27)
Where Structure Meets Function (1998) (27)
Secretin Receptors on Neuroblastoma Cell Membranes: Characterization of 125I‐Labeled Secretin Binding and Association with Adenylate Cyclase (1984) (27)
Selectivity Challenges in Docking Screens for GPCR Targets and Antitargets (2018) (27)
COVID-19: Famotidine, Histamine, Mast Cells, and Mechanisms (2021) (26)
Optimization of 2-phenylcyclopropylmethylamines as selective serotonin 2C receptor agonists and their evaluation as potential antipsychotic agents. (2015) (26)
Multi-receptor drug design: Haloperidol as a scaffold for the design and synthesis of atypical antipsychotic agents. (2012) (26)
Application of Quantitative Structure–Activity Relationship Models of 5-HT1A Receptor Binding to Virtual Screening Identifies Novel and Potent 5-HT1A Ligands (2014) (26)
Bis-spirolabdane diterpenoids from Leonotis nepetaefolia. (2012) (26)
Controlling opioid receptor functional selectivity by targeting distinct subpockets of the orthosteric site (2021) (26)
Ontogeny of serotonin and serotonin2A receptors in rat auditory cortex (2008) (25)
Benzothiazoles as probes for the 5HT1A receptor and the serotonin transporter (SERT): a search for new dual-acting agents as potential antidepressants. (2012) (25)
In Vitro and In Vivo Characterization of the Alkaloid Nuciferine (2016) (24)
Structural determinants for high 5-HT(2A) receptor affinity of spiro[9,10-dihydroanthracene]-9,3(')-pyrrolidine (SpAMDA). (2004) (24)
Design and Discovery of Functionally Selective Serotonin 2C (5-HT2C) Receptor Agonists. (2016) (24)
Identification of a new selective dopamine D4 receptor ligand. (2014) (24)
Advancing drug discovery for schizophrenia (2011) (24)
The effects of morphine on catecholamine metabolism during postnatal development (1980) (23)
Convergent synthesis of complex diketopiperazines derived from pipecolic acid scaffolds and parallel screening against GPCR targets. (2006) (23)
Structure-activity relationship studies of SYA 013, a homopiperazine analog of haloperidol. (2012) (23)
The Serotonin Receptors (2006) (23)
N-Alkyl-octahydroisoquinolin-1-one-8-carboxamides: Selective and Nonbasic κ-Opioid Receptor Ligands (2010) (23)
A novel mitragynine analog with low efficacy mu-opioid receptor agonism displays antinociception with attenuated adverse effects (2021) (23)
HTS and Rational Drug Design to Generate a Class of 5‐HT2C‐Selective Ligands for Possible Use in Schizophrenia. (2010) (23)
Identification of 6-benzylthioinosine as a myeloid leukemia differentiation-inducing compound. (2008) (22)
Generation of Designer Receptors Exclusively Activated by Designer Drugs (DREADDs) Using Directed Molecular Evolution (2010) (22)
Protamine is an antagonist of apelin receptor, and its activity is reversed by heparin (2017) (22)
Why Academic Drug Discovery Makes Sense (2006) (22)
Molecular and cellular mechanisms for the polarized sorting of serotonin receptors: relevance for genesis and treatment of psychosis. (2004) (22)
Molecular and Cellular Mechanisms of Septic Shock (1988) (21)
Synthesis, structure-affinity relationships, and modeling of AMDA analogs at 5-HT2A and H1 receptors: structural factors contributing to selectivity. (2009) (21)
1-(1-Naphthyl)piperazine as a novel template for 5-HT6 serotonin receptor ligands. (2005) (21)
Structure-based discovery of potent and selective melatonin receptor agonists (2020) (21)
Screening the receptorome for plant-based psychoactive compounds. (2005) (21)
Discrepancies in Kappa Opioid Agonist Binding Revealed through PET Imaging. (2018) (21)
LSD-stimulated behaviors in mice require β-arrestin 2 but not β-arrestin 1 (2021) (21)
Structural Insights Accelerate the Discovery of Opioid Alternatives. (2021) (21)
p90 Ribosomal S6 kinase 2, a novel GPCR kinase, is required for growth factor-mediated attenuation of GPCR signaling. (2010) (20)
Further Advances in Optimizing (2-Phenylcyclopropyl)methylamines as Novel Serotonin 2C Agonists: Effects on Hyperlocomotion, Prepulse Inhibition, and Cognition Models. (2016) (20)
An African-specific haplotype in MRGPRX4 is associated with menthol cigarette smoking (2019) (20)
Binding of amine-substituted N1-benzenesulfonylindoles at human 5-HT6 serotonin receptors. (2005) (20)
Haloperidol: towards further understanding of the structural contributions of its pharmacophoric elements at D2-like receptors. (2004) (19)
Molecular Biology and Genomic Organization of G Protein-Coupled Serotonin Receptors (2006) (19)
Opportunities and Challenges of Psychiatric Drug Discovery: Roles for Scientists in Academic, Industry, and Government Settings (2008) (18)
Perturbation of transmembrane signaling mechanisms in acute and chronic endotoxemia. (1987) (18)
High-throughput identification of G protein-coupled receptor modulators through affinity mass spectrometry screening† †Electronic supplementary information (ESI) available. See DOI: 10.1039/c7sc04698g (2018) (18)
Allosteric Antipsychotics: M4 Muscarinic Potentiators as Novel Treatments for Schizophrenia (2010) (17)
The neural basis of psychedelic action (2022) (17)
Engineering a region of bulk tolerance in the 5-HT2A receptor (1999) (17)
Interaction of chiral MS-245 analogs at h5-HT6 receptors. (2005) (17)
NOBEL 2012 Chemistry: Studies of a ubiquitous receptor family (2012) (17)
In Silico Molecular Comparisons of C. elegans and Mammalian Pharmacology Identify Distinct Targets That Regulate Feeding (2013) (16)
Geometry-affinity relationships of the selective serotonin receptor ligand 9-(aminomethyl)-9,10-dihydroanthracene. (2002) (16)
RNA interference screen for RGS protein specificity at muscarinic and protease-activated receptors reveals bidirectional modulation of signaling. (2010) (16)
2‐Substituted Tryptamines: Agents with Selectivity for 5‐HT6 Serotonin Receptors. (2000) (16)
HTS navigator: freely accessible cheminformatics software for analyzing high-throughput screening data (2014) (16)
Autoxidation of salvinorin A under basic conditions. (2005) (16)
Psilocybin for depression and anxiety associated with life-threatening illnesses (2016) (16)
Kinetic evidence for differential agonist and antagonist binding to bovine hippocampal synaptic membrane opioid receptors. (1984) (16)
Receptor screening technologies in the evaluation of Amazonian ethnomedicines with potential applications to cognitive deficits. (2011) (16)
CoMFA analyses of C-2 position salvinorin A analogs at the kappa-opioid receptor provides insights into epimer selectivity. (2010) (16)
Synthesis and Evaluation of 18F-FE-PEO in Rodents: An 18F-Labeled Full Agonist for Opioid Receptor Imaging (2013) (16)
Influence of chain length and N-alkylation on the selective serotonin receptor ligand 9-(aminomethyl)-9,10-dihydroanthracene. (2001) (16)
Ontogeny of benzomorphan-selective (κ) sites: A computerized analysis (1983) (15)
Effects of norlaudanosolinecarboxylic acids on enzymes of catecholamine metabolism. (1980) (15)
Discovery of N-Substituted (2-Phenylcyclopropyl)methylamines as Functionally Selective Serotonin 2C Receptor Agonists for Potential Use as Antipsychotic Medications. (2017) (15)
N1‐(Benzenesulfonyl)tryptamines as Novel 5‐HT6 Antagonists. (2001) (14)
Functional SNPs in Genes Encoding the 5-HT2A Receptor Modify the Affinity and Potency of Several Atypical Antipsychotic Drugs (2011) (14)
Screening the receptorome yields validated molecular targets for drug discovery. (2006) (14)
Rational Drug Design Leading to the Identification of a Potent 5-HT(2C) Agonist Lacking 5-HT(2B) Activity. (2011) (14)
Design and synthesis of dual 5-HT1A and 5-HT7 receptor ligands. (2016) (14)
How structure informs and transforms chemogenetics. (2019) (14)
A Structural Understanding of Class B GPCR Selectivity and Activation Revealed. (2020) (14)
What's All the RAVE about Receptor Internalization? (1999) (14)
9-(Aminomethyl)-9,10-dihydroanthracene is a novel and unlikely 5-HT2A receptor antagonist. (1999) (13)
Molecular insights into psychedelic drug action (2021) (13)
Bioisosteric Modification of Salvinorin A, a Potent and Selective Kappa-Opioid Receptor Agonist (2006) (13)
Exploring the relationship between binding modes of 9-(aminomethyl)-9,10-dihydroanthracene and cyproheptadine analogues at the 5-HT2A serotonin receptor. (2001) (13)
D2 Dopamine Receptor G Protein-Biased Partial Agonists Based on Cariprazine. (2019) (13)
Psychotomimetic Effects of Kappa Opioid Receptor Agonists (2012) (13)
Search for α3β₂/₃γ2 subtype selective ligands that are stable on human liver microsomes. (2013) (13)
Synthesis of potent and selective serotonin 5-HT1B receptor ligands. (2005) (13)
Contributions of molecular biology to antipsychotic drug discovery: promises fulfilled or unfulfilled? (2006) (13)
Structural insights into distinct signaling profiles of the μOR activated by diverse agonists (2021) (13)
Structure-based Design, Synthesis, Biochemical and Pharmacological Characterization of Novel Salvinorin A Analogues as Active State Probes of the κ -Opioid Receptor (2009) (13)
β-Fluorofentanyls Are pH-Sensitive Mu Opioid Receptor Agonists. (2019) (13)
The in vitro pharmacology of the β-adrenergic receptor pet ligand (s)-fluorocarazolol reveals high affinity for cloned β-adrenergic receptors and moderate affinity for the human 5-HT1A receptor (2001) (13)
Sh-I-048A, an in vitro non-selective super-agonist at the benzodiazepine site of GABAA receptors: The approximated activation of receptor subtypes may explain behavioral effects (2014) (13)
Discovery of aryl-biphenyl-2-ylmethylpiperazines as novel scaffolds for 5-HT(7) ligands and role of the aromatic substituents in binding to the target receptor. (2013) (12)
Defining Structure-Functional Selectivity Relationships (SFSR) for a Class of Non-Catechol Dopamine D1 Receptor Agonists. (2019) (12)
Fentanyl-related designer drugs W-18 and W-15 lack appreciable opioid activity in vitro and in vivo. (2017) (12)
Design and Synthesis of (2-(5-Chloro-2,2-dimethyl-2,3-dihydrobenzofuran-7-yl)cyclopropyl)methanamine as a Selective Serotonin 2C Agonist. (2015) (12)
N-methylacetamide analogue of salvinorin A: a highly potent and selective kappa opioid receptor agonist with oral efficacy (2007) (12)
Further studies on the binding of N1-substituted tryptamines at h5-HT6 receptors. (2007) (12)
Short synthesis of a novel class of salvinorin A analogs with hemiacetalic structure. (2008) (12)
Erratum: A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells (Nature Chemical Biology (2011) 7 (401-404)) (2011) (12)
trans-2-(2,5-Dimethoxy-4-iodophenyl)cyclopropylamine and trans-2-(2,5-dimethoxy-4-bromophenyl)cyclopropylamine as potent agonists for the 5-HT2 receptor family (2012) (12)
Synthesis and biological evaluation of new salvinorin A analogues incorporating natural amino acids. (2011) (12)
Demonstration of a slowly dissociating form of bovine hippocampal synaptic membrane opiate receptors. (1982) (12)
BAY k 8644, a calcium channel agonist, reverses hypotension in endotoxin-shocked rats. (1986) (11)
Single Amino Acid Variation Underlies Species-Specific Sensitivity to Amphibian Skin-Derived Opioid-like Peptides. (2015) (11)
Interaction of N1-unsubstituted and N1-benzenesulfonyltryptamines at h5-HT6 receptors. (2006) (11)
Atypical Antipsychotic Drugs: Clinical and Preclinical Studies (1996) (11)
Microsomal opiate receptors differ from synaptic membrane receptors in proteolytic sensitivity (1982) (11)
Molecular interactions between general anesthetics and the 5HT2B receptor (2015) (11)
Alterations in bidirectional transmembrane calcium flux occur without changes in protein kinase C levels in rat aorta during sepsis. (1988) (11)
Synthesis and evaluation of ligands for D2-like receptors: the role of common pharmacophoric groups. (2009) (11)
Far away from the lamppost (2018) (10)
Further evaluation of the tropane analogs of haloperidol. (2014) (10)
Receptor systems: will mining the receptorome yield novel targets for pharmacotherapy? (2005) (10)
Cell biology. A last GASP for GPCRs? (2002) (10)
Signaling snapshots of a serotonin receptor activated by the prototypical psychedelic LSD (2022) (10)
The effects of tetrahydroisoquinolinecarboxylic acids in tyrosine 3-monooxygenase. (1981) (9)
Polypharmacological Drugs: "Magic Shotguns" for Psychiatric Diseases (2012) (9)
Chemical Modifications on 4-Arylpiperazine-Ethyl Carboxamide Derivatives Differentially Modulate Affinity for 5-HT1A, D4.2, and α2A Receptors: Synthesis and In Vitro Radioligand Binding Studies (2010) (9)
4-Aminoethylpiperazinyl aryl ketones with 5-HT₁A/5-HT₇ selectivity. (2012) (9)
Cross-linking of [125I]-endorphin to -opioid receptors during development (1989) (9)
Aryl Biphenyl‐3‐ylmethylpiperazines as 5‐HT7 Receptor Antagonists (2013) (9)
Structure and Function Reveal Insights in the Pharmacology of 5-HT Receptor Subtypes (2006) (9)
High-dose olanzapine for treatment-resistant schizophrenia. (2008) (8)
Erratum: Evidence for a model of agonist-induced activation of 5-hydroxytryptamine 2A serotonin receptors that involves the disruption of a strong ionic interaction between helices 3 and 6 (Journal of Biological Chemistry (2002) 277 (11441-11449)) (2002) (8)
Pharmacology of 5-HT2 Receptors (2000) (8)
Immunohistochemical distribution of β-protein kinase C in rat hippocampus determined with an antibody against a synthetic peptide sequence (1989) (8)
Developing selectively nonselective drugs for treating CNS disorders (2006) (8)
Alterations in hepatic and aortic phospholipase-C coupled receptors and signal transduction in rat intraperitoneal sepsis. (1989) (8)
A promising chemical series of positive allosteric modulators of the μ-opioid receptor that enhance the antinociceptive efficacy of opioids but not their adverse effects (2021) (8)
A study of the structure-activity relationship of GABA(A)-benzodiazepine receptor bivalent ligands by conformational analysis with low temperature NMR and X-ray analysis. (2008) (8)
Novel oxotremorine-related heterocyclic derivatives: Synthesis and in vitro pharmacology at the muscarinic receptor subtypes. (2007) (7)
5-ZATRYPTAMINE ANALOGS AS h5-HT6 SEROTONIN RECEPTOR LIGANDS (2004) (7)
High-throughput identification of G protein-coupled receptor modulators through affinity mass spectrometry screening (2018) (7)
Receptorome screening for CNS drug discovery. (2005) (7)
Synthesis and in vitro pharmacology of novel heterocyclic muscarinic ligands. (2003) (7)
Neuronal Signal Transduction Pathways: Wasteland or the Promised Land? (2000) (7)
Molecular basis for selective activation of DREADD-based chemogenetics (2022) (7)
Differential roles of extracellular Histidine residues of GPR68 for proton-sensing and allosteric modulation by divalent metal ions. (2020) (7)
Synthesis and in vitro binding studies of substituted piperidine naphthamides. Part I: Influence of the substitution on the basic nitrogen and the position of the amide on the affinity for D2L, D4.2, and 5-HT2A receptors. (2007) (7)
Synthesis of potent and selective dopamine D(4) antagonists as candidate radioligands. (2001) (7)
Methoxy-substituted 9-aminomethyl-9,10-dihydroanthracene (AMDA) derivatives exhibit differential binding affinities at the 5-HT(2A) receptor. (2008) (7)
Binding of methoxy-substituted N1-benzenesulfonylindole analogs at human 5-HT6 serotonin receptors. (2006) (7)
Re-exploring the N-phenylpicolinamide derivatives to develop mGlu4 ligands with improved affinity and in vitro microsomal stability. (2015) (6)
The promise and peril of chemical probes (vol 11, pg 536, 2015) (2015) (6)
Synthesis and in vitro binding studies of substituted piperidine naphthamides. Part II: Influence of the substitution on the benzyl moiety on the affinity for D2L, D4.2, and 5-HT2A receptors. (2007) (6)
N-tetrahydrothiochromenoisoxazole-1-carboxamides as selective antagonists of cloned human 5-HT2B. (2010) (6)
Receptor changes in endotoxemia. (1989) (6)
A BIOCHEMICAL MECHANISM FOR VASODILATION IN SEPTIC SHOCK (1987) (6)
9-Aminomethyl-9,10-dihydroanthracene (AMDA) analogs as structural probes for steric tolerance in 5-HT2A and H1 receptor binding sites. (2010) (6)
5-Hydroxytryptamine receptors (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database (2019) (6)
Subversion of Serotonin Receptor Signaling in Osteoblasts by Kynurenine Drives Acute Myeloid Leukemia (2022) (6)
Evaluation of the eutomer of 4-{3-(4-chlorophenyl)-3-hydroxypyrrolidin-1-yl}-1-(4-fluorophenyl)butan-1-one, {(+)-SYA 09}, a pyrrolidine analog of haloperidol. (2006) (6)
N-Alkyl-octahydroisoquinolin-1-one-8-carboxamides: a Novel Class of Selective, Nonbasic, Nitrogen-Containing κ-Opioid Receptor Ligands. (2010) (6)
Structure-Based Design of a Chemical Probe Set for the 5-HT5A Serotonin Receptor. (2022) (6)
Spiro[9,10-dihydroanthracene]-9,3'-pyrrolidine-a structurally unique tetracyclic 5-HT2A receptor antagonist. (2003) (6)
The Dynamin-dependent, Arrestin-independent Internalization of 5-Hydroxytryptamine 2A (5-HT 2A ) Serotonin Receptors Reveals Differential Sorting of Arrestins and 5-HT 2A Receptors (2001) (5)
Correction: The Ketamine Analogue Methoxetamine and 3- and 4-Methoxy Analogues of Phencyclidine Are High Affinity and Selective Ligands for the Glutamate NMDA Receptor (2018) (5)
Activation of phosphatidylinositol turnover in rat aorta by alpha 1-adrenergic receptor stimulation. (1985) (5)
Screening the receptorome (2006) (5)
Crystal structures of the σ2 receptor template large-library docking for selective chemotypes active in vivo (2021) (5)
Impossible or merely difficult? Two grand challenges from a biologist's perspective. (2013) (5)
Corrigendum: The promise and peril of chemical probes. (2015) (5)
4β-Methyl-5-(3-hydroxyphenyl)morphan opioid agonist and partial agonist derived from a 4β-methyl-5-(3-hydroxyphenyl)morphan pure antagonist. (2013) (5)
VEGAS as a Platform for Facile Directed Evolution in Mammalian Cells (2019) (5)
Molecular insights into the regulation of constitutive activity by RNA editing of 5HT2C serotonin receptors (2022) (5)
Inactive and active state structures template selective tools for the human 5-HT5A receptor (2022) (5)
Polymorphic and Posttranscriptional Modifications of 5-HT Receptor Structure (2006) (5)
Structure-based design of a chemical probe set for the 5-HT5A serotonin receptor (2021) (4)
Modification of protein kinase C (PKC) activity and diacylglycerol (DAG) accumulation in hepatocytes in continuous endotoxemia. (1989) (4)
5-HT2A SNPs Alter the Pharmacological Signaling of Potentially Therapeutic Psychedelics. (2022) (4)
Norepinephrine-induced phosphorylation of a 25 kd phosphoprotein in rat aorta is altered in intraperitoneal sepsis. (1989) (4)
Erratum: The promise and peril of chemical probes (Nature Chemical Biology (2015) 11 (536-541)) (2015) (4)
Ligand recognition and allosteric modulation of the human MRGPRX1 receptor (2022) (4)
Engineering GPCR signaling pathways with (2008) (3)
Structure and Function of the Third Intracellular Loop of the 5-Hydroxytryptamine 2A Receptor: The Third Intracellular Loop Is a -Helical and Binds Puriﬁed Arrestins (1999) (3)
SAR of Psilocybin Analogues: Discovery of a Selective 5-HT2C Agonist. (2006) (3)
Selective manipulation of spinal microglia by chemogenetics: Implications for allodynia and inflammatory signaling (2015) (3)
Agonist and antagonist TRUPATH assays for G protein-coupled receptors (2022) (3)
LSD’s effects are differentially modulated in arrestin knockout mice (2021) (3)
Structure-based design of bitopic ligands for the µ-opioid receptor (2022) (3)
Title Structure and Function of the Third Intracellular Loop of the 5-Hydroxytryptamine 2 A Receptor : The Third Intracellular Loop Is α-Helical and Binds Purified (1999) (3)
An alerting structure: human orexin receptor 1 (2016) (3)
Characterization of 5-HT2 receptors linked to phospholipase C in rat aorta (1985) (3)
The Emergence of Serotonin 5‐HT2B Receptors as DRUG Antitargets (2008) (3)
Pharmacology of W-18 and W-15 (2016) (2)
Activation mechanisms for a universal signalling protein (2018) (2)
Developmental and Synaptic Regulation of 5-HT2 and 5-HT1c Serotonin Receptors (1991) (2)
Convenient Synthesis and in vitro Pharmacological Activity of 2-Thioanalogues of Salvinorins A and B. (2007) (2)
Ring substituted analogues of 5-aminomethyl-10,11-dihydro-dibenzo[a,d]cycloheptene (AMDH): potential modes of binding to the 5-HT(2A) receptor. (2003) (2)
INSIGHTS INTO THE REGULATION OF 5-HT 2A RECEPTORS BY SCAFFOLDING PROTEINS AND KINASES (2009) (2)
SnapShot: Psychedelics and serotonin receptor signaling (2023) (2)
Development of CNS multi-receptor ligands: Modification of known D2 pharmacophores. (2016) (2)
Evidence for an endacoid for the 5HT2 recognition site. (1985) (2)
Moderate chemical modifications of WAY-100635 improve the selectivity for 5-HT1A versus D4 receptors. (2012) (2)
Phosphoproteomics Illuminates Opioid Actions. (2018) (2)
Bioisosteric Modification of Salvinorin A, a Potent and Selective ϰ‐Opioid Receptor Agonist. (2006) (2)
Structure-based discovery of conformationally selective inhibitors of the serotonin transporter (2022) (2)
Structures of the entire human opioid receptor family (2023) (2)
The Emergence of 5-HT2B Receptors as Targets to Avoid in Designing and Refining Pharmaceuticals (2006) (2)
Protein engineering: electrifying cell receptors. (2008) (2)
Conference Report: Psychiatric Genomics Consortium Meeting: Pathways to Drugs, London, March 2017 (2018) (2)
Structural Determinants for High 5‐HT2A Receptor Affinity of Spiro[9,10‐dihydroanthracene]‐9,3′‐pyrrolidine (SpAMDA). (2004) (2)
Addendum: A cellular chemical probe targeting the chromodomains of Polycomb repressive complex 1 (2019) (2)
Design of fluorinated cyclopropane derivatives of 2-phenylcyclopropylmethylamine leading to identification of a selective serotonin 2C (5-HT2C) receptor agonist without 5-HT2B agonism. (2019) (2)
Structural basis of ligand recognition at the human MT1 melatonin receptor (2019) (2)
Sa1939 Intestinal Epithelial Cell (IEC)-Derived Mu-Opioid Signaling is Protective Against Ischemia Reperfusion (I/R) Induced Injury (2012) (2)
Progress towards better understanding and treatment of major psychiatric illnesses. (2005) (1)
Highly conserved aromatic residues are essential for agonist efficacy at 5-HTM receptors (1996) (1)
Publisher Correction: Structural basis of ligand recognition at the human MT1 melatonin receptor (2019) (1)
Psychedelic compounds directly excite 5-HT2A Layer 5 Pyramidal Neurons in the Prefrontal Cortex through a 5-HT2A Gq -mediated activation mechanism (2022) (1)
(250) Selective manipulation of spinal microglia by chemogenetics: implications for allodynia and inflammatory signaling (2015) (1)
Faculty Opinions recommendation of Manifold roles of β-arrestins in GPCR signaling elucidated with siRNA and CRISPR/Cas9. (2019) (1)
Historical Overview of the Concept of Functional Selectivity (2009) (1)
Structure of the human smoothened receptor in complex with ANTA XV (2014) (1)
Structure, function and pharmacology of human itch GPCRs (2021) (1)
Faculty Opinions recommendation of Bias factor and therapeutic window correlate to predict safer opioid analgesics. (2017) (1)
G-Protein Peptidomimetics Stabilize GPCR Active State Conformations. (2021) (1)
Ontogeny of benzomorphan-selective (kappa) sites: a computerized analysis. (1983) (1)
Cross-linking of [125I]beta-endorphin to mu-opioid receptors during development. (1989) (1)
Crystal structure of the LSD-bound 5-HT2B receptor (2017) (1)
Faculty Opinions recommendation of Acoustically targeted chemogenetics for the non-invasive control of neural circuits. (2018) (1)
19. Clozapine alters the subcellular distribution of 5-HT2A receptors (1998) (1)
The cranial windows of perception (2021) (1)
Simultaneous, Massively Parallel and Genome-Wide Interrogation of GPCR b-arrestin-ergic Signaling: Implications for GPCR Drug Discovery and Catecholamine Biology (2013) (1)
Crystal Structure of a nanobody-stabilized active state of the kappa-opioid receptor (2018) (1)
Faculty Opinions recommendation of Niacin lipid efficacy is independent of both the niacin receptor GPR109A and free fatty acid suppression. (2012) (1)
Rapid agonist-induced internalization of 5-ht2a receptors revealed by confocal laser microscopy (1996) (1)
Faculty Opinions recommendation of Targeted Elimination of G Proteins and Arrestins Defines Their Specific Contributions to Both Intensity and Duration of G Protein-coupled Receptor Signaling. (2016) (1)
Synthesis of Potent and Selective Dopamine D4 Antagonists as Candidate Radioligands. (2001) (1)
P272 PWZ-029, AN INVERSE AGONIST SELECTIVE FOR a5 SUBUNIT-CONTAINING GABAA RECEPTORS, ENHANCES PERFORMANCE ON AN EXECUTIVE FUNCTION TASK IN MONKEYS (2009) (1)
Faculty Opinions recommendation of Multiplexed analysis of the secretin-like GPCR-RAMP interactome. (2019) (1)
A Chemogenetic Platform for Spatio-temporal Control of β-arrestin Translocation and Signaling at G protein-Coupled Receptors (2018) (1)
110. Agonist-induced internalization of the 5HT2A receptor in vitro (1996) (1)
Role of Phosphoinositide Hydrolysis and Protein Kinase C Activation in 5HT 2 Receptor Function in Smooth Muscle (1990) (1)
Faculty Opinions recommendation of Genetic identification of C fibres that detect massage-like stroking of hairy skin in vivo. (2013) (1)
Psychedelics as Transformative Therapeutics. (2023) (1)
Structure of the N/OFQ Opioid Receptor in Complex with a Peptide Mimetic (2012) (1)
Design of first in class bitopic ligands targeting the sodium binding pocket in opioid receptors (2020) (1)
Functional Evolution of Opioid Family G Protein-Coupled Receptors (2014) (1)
BIOLOGIC MECHANISMS OF PSYCHOSIS AND ANTIPSYCHOTIC DRUG ACTIONS: FROM DOPAMINE EXCESS TO DOPAMINE STABILIZATION * (2003) (1)
Developmental regulation of 5-HT2 and 5-HT1c receptor gene expression in rat brain. (1993) (1)
Neurotensin receptor allosterism revealed in complex with a biased allosteric modulator (2022) (1)
Structural determinants of 5-HT2B receptor activation and biased agonism (2018) (1)
A Targetable Bone Marrow-Niche Axis for the Treatment of Acute Myeloid Leukemia (2021) (1)
Structural Determinants of Activation and Biased Agonism at the 5-HT2B Receptor (2018) (0)
G Protein: Methods and Protocols: Role of G Proteins in Psychiatric and Neurological Disorders. Ram K. Mishra , Glen B. Baker , Alan A. Boulton (1999) (0)
5HT and 5HT2 recognition sites are present in the 5HT receptor complex of NCB-20 cell line (1984) (0)
Nanobody-enabled monitoring of kappa opioid receptor states (2020) (0)
1.8 A Structure of the human delta opioid 7TM receptor (PSI Community Target) (2013) (0)
Psychedelics: preclinical insights provide directions for future research. (2023) (0)
Structure of the human smoothened 7TM receptor in complex with an antitumor agent (2013) (0)
Chimeric Receptor Proteins as Tools for Medicinal Chemists (1993) (0)
t identi fi cation of G protein-coupled receptor modulators through a ffi nity mass spectrometry screening † (2018) (0)
Crystal structure of the chimeric protein of 5-HT2B-BRIL in complex with ergotamine (2013) (0)
Faculty Opinions recommendation of Synthesis and pharmacological evaluation of noncatechol G protein biased and unbiased dopamine D1 receptor agonists. (2019) (0)
Structural insights from G-protein-coupled receptor complexes enable the rational engineering of improved light-activated designer receptors. (2022) (0)
XFEL crystal structure of human melatonin receptor MT1 in complex with ramelteon (2019) (0)
Author response: Donated chemical probes for open science (2018) (0)
Decision letter: ß-arrestin 2 germline knockout does not attenuate opioid respiratory depression (2020) (0)
Vision and olfaction say UNC-le to G proteins (2011) (0)
A self-activating orphan receptor (2020) (0)
XFEL crystal structure of human melatonin receptor MT2 in complex with ramelteon (2019) (0)
Virtual discovery of melatonin receptor ligands to modulate circadian rhythms (2020) (0)
Alterations in rat aortic alpha 1-adrenoceptors and alpha 1-Adrenergic stimulated phosphoinositide hydrolysis in intraperitoneal sep . 5 is CrcilKfl ! (0)
TRUPATH: An Open-Source Biosensor Platform for Interrogating the GPCR Transducerome. (2022) (0)
COVID-19: Famotidine, Histamine, Mast Cells, and Mechanisms (2020) (0)
Signaling snapshots of 5-HT 2B serotonin receptor activated by the prototypical psychedelic LSD (2022) (0)
List of Tables vi List of Figures viii List of Abbreviations ix (2008) (0)
Remote Control of Cellular Signaling Using DREADD Technology (2013) (0)
Faculty Opinions recommendation of ApoE-directed therapeutics rapidly clear β-amyloid and reverse deficits in AD mouse models. (2012) (0)
G‐protein alpha subunits differentially alter the conformation of kappa opioid receptor (2007) (0)
CryoEM structure of Gi-coupled MRGPRX2 with small molecule agonist (R)-Zinc-3573 (2021) (0)
Structural insights into the human niacin receptor HCA2-Gi signalling complex (2023) (0)
Opioid Receptor Agonists κ Chemotype-selective Modes of Action of Signal Transduction : (2013) (0)
Faculty Opinions recommendation of Mitochondrial ClpP-Mediated Proteolysis Induces Selective Cancer Cell Lethality. (2019) (0)
Faculty Opinions recommendation of Structures of the Rhodopsin-Transducin Complex: Insights into G-Protein Activation. (2019) (0)
Faculty Opinions recommendation of SEP-363856, a Novel Psychotropic Agent with a Unique, Non-D2 Receptor Mechanism of Action. (2019) (0)
Faculty Opinions recommendation of Evidence against dopamine D1/D2 receptor heteromers. (2015) (0)
Allosteric modulator LY3154207 binding to SKF-81297-bound dopamine receptor 1 in complex with miniGs protein (2021) (0)
Faculty Opinions recommendation of A transient placental source of serotonin for the fetal forebrain. (2011) (0)
Molecular and cellular mechanisms of septic shock : proceedings of a conference held in Bethesda, Maryland, February 29-March 1, 1988 (1989) (0)
Search for alpha 3 beta 2/3 gamma 2 subtype selective ligands that are stable on human liver microsomes (2012) (0)
Cryo-EM structure of SKF-81297-bound dopamine receptor 1 in complex with Gs protein (2021) (0)
Cryo-EM structure of apomorphine-bound dopamine receptor 1 in complex with Gs protein (2021) (0)
Cell-type selective deletion of RSK2 reveals insights into altered signaling in Coffin-Lowry Syndrome (2017) (0)
1-( 2 , 5-Dimethoxy-4-( trifluoromethy 1 ) phenyl )-2-aminopropane : A Potent Serotonin ~-H T ~ A / ~ c Agonist (2001) (0)
Human Protein Arginine Methyltransferase 3 in complex with 1-isoquinolin-6-yl-3-[2-oxo-2-(pyrrolidin-1-yl)ethyl]urea (2015) (0)
Faculty Opinions recommendation of A Gq-Ca2+ axis controls circuit-level encoding of circadian time in the suprachiasmatic nucleus. (2013) (0)
Next-Generation GPCR Therapeutics (2017) (0)
Further Advances in Optimizing (2-Phenylcyclopropyl)methylamines as Novel Serotonin 2C Agonists: Effects in Open Field, Prepulse Inhibition, and Cognition Models (2021) (0)
Reversal of endotoxic shock with the calcium channel agonist BAY k 8644 (1986) (0)
Crystal structure of HTR2A with inverse agonist (2020) (0)
NOREPINEPHRINE INCREASES PRODUCTION OF A NUCLEAR MESSAGE IN VASCULAR TISSUE (1988) (0)
Crystal structure of the chimeric protein of 5-HT1B-BRIL in complex with dihydroergotamine (PSI Community Target) (2013) (0)
Crystal structure of 5-HT2C in complex with ritanserin (2018) (0)
Illuminating the druggable GPCR-ome (2018) (0)
Activation mechanisms for a universal signalling protein (2018) (0)
Faculty Opinions recommendation of Platelet-derived serotonin links vascular disease and tissue fibrosis. (2011) (0)
TransductionGPCRs as Tools to Modulate Signal (2016) (0)
THE HIDDEN PHARMACOLOGY OF THE HUMAN GPCR-OME (2014) (0)
Glossary Agranulocytosis : an acute condition involving a severe and potentially fatal reduction in white blood cells (2007) (0)
5-Hydroxytryptamine receptor 6 (2006) (0)
(trifluoromethy1)phenyl) -2-aminopropane: A Potent Serotonin ~-HT~A/~c Agonist (1994) (0)
The anthelmintic praziquantel is a human serotoninergic G-protein-coupled receptor ligand (2017) (0)
D2 Functionally Selective Ligands: Novel Therapeutics? (2013) (0)
Synchrotron structure of the human delta opioid receptor in complex with a bifunctional peptide (PSI community target) (2015) (0)
Fast dissociation rates predict neither efficacy nor lack of side-effects (2004) (0)
CryoEM structure of Gi-coupled MRGPRX2 with peptide agonist Cortistatin-14 (2021) (0)
CryoEM structure of Gq-coupled MRGPRX4 with small molecule agonist MS47134 (2021) (0)
131. Clozapine-induced internalization of the 5-HT2A receptor in vitro (1998) (0)
G protein coupled receptors as targets for transformative neuropsychiatric therapeutics. (2023) (0)
Mining the Receptorome* □ S (2005) (0)
Alterations in splenic and hepatic protein kinase C in sepsis and chronic endotoxemia. (1989) (0)
An automated proximity proteomics pipeline for subcellular proteome and protein interaction mapping (2023) (0)
independent Internalization of 5-Hydroxytryptamine 2 A ( 5-HT 2 A ) Serotonin Receptors Reveals Differential Sorting of Arrestins and 5-HT 2 A Receptors during Endocytosis Permalink (2001) (0)
A self-activating orphan receptor (2020) (0)
Catalytic site mutations confer multiple states of G protein activation (2023) (0)
De Novo Design of κ-Opioid Receptor Antagonists Using a Generative Deep Learning Framework (2023) (0)
Cryo-EM structure of SKF-83959-bound dopamine receptor 1 in complex with Gs protein (2021) (0)
A Slowly Dissociating form of Bovine Hippocampal Synaptic Membrane Opiate Receptors (1984) (0)
Cellular mechanisms of salvinorin A action in vivo (2012) (0)
Faculty Opinions recommendation of Rabies screen reveals GPe control of cocaine-triggered plasticity. (2017) (0)
Faculty Opinions recommendation of SRT1720, SRT2183, SRT1460, and resveratrol are not direct activators of SIRT1. (2010) (0)
Faculty Opinions recommendation of Spatial encoding of cyclic AMP signaling specificity by GPCR endocytosis. (2014) (0)
N -Methylacetamide Analog of Salvinorin A: A Highly Potent and Selective (cid:1) -Opioid Receptor Agonist with Oral Efficacy □ S (2007) (0)
Convenient synthesis and in vitro pharmacological activity of 2-thioanalogs of salvinorin A and B (2007) (0)
Structural basis of G protein couple receptor polypharmacology (2018) (0)
Prevalent mouse phenotypes in the unexplored druggable genome (2021) (0)
Docking a bespoke ultra-large tetrahydropyridine library identifies 5-HT2A receptor agonists conferring new biology (2022) (0)
Structure of the human D4 Dopamine receptor in complex with Nemonapride (2017) (0)
Crystal structure of 5-HT2C in complex with ergotamine (2018) (0)
Structure of the human smoothened receptor 7TM bound to an antitumor agent (2013) (0)
Novel Mechanisms of Drug Treatment in Psychiatry (2008) (0)
On a bovine brain peptide functioning as a putative ligand for 5HT2 recognition sites (1984) (0)
Author response: Controlling opioid receptor functional selectivity by targeting distinct subpockets of the orthosteric site (2020) (0)
Genetic deletion of β-arrestin 2 modulates LSD-stimulated behaviors in mice (2021) (0)
Faculty Opinions recommendation of Cancer and the dopamine D2 receptor: a pharmacological perspective. (2019) (0)
Faculty Opinions recommendation of Multidimensional Tracking of GPCR Signaling via Peroxidase-Catalyzed Proximity Labeling. (2017) (0)
Faculty Opinions recommendation of Activation of the GLP-1 receptor by a non-peptidic agonist. (2020) (0)
Structure of the sodium-bound human D4 Dopamine receptor in complex with Nemonapride (2017) (0)
Faculty Opinions recommendation of Transmembrane receptor DCC associates with protein synthesis machinery and regulates translation. (2010) (0)
Mining the receptorome: an efficient approach for target discovery and validation (2009) (0)
Deschloroclozapine, a potent and selective chemogenetic actuator enables rapid neuronal and behavioral modulations in mice and monkeys (2020) (0)
Cryo-EM structure of Bromocriptine-bound dopamine receptor 2 in complex with Gi protein (2021) (0)
Pharmacologic analysis of non-synonymous coding 5-HT2A SNPs reveals alterations psychedelic drug potencies and efficacies (2021) (0)
GASTROINTESTINAL , HEPATOBILIARY , AND PANCREATIC PATHOLOGY Intestinal Epithelial Cell e Derived m-Opioid Signaling Protects against Ischemia Reperfusion Injury through PI 3 K Signaling (2013) (0)
Neuropharmacological Profiles of Antipsychotic Drugs (2010) (0)
Faculty Opinions recommendation of R-spondins function as ligands of the orphan receptors LGR4 and LGR5 to regulate Wnt/beta-catenin signaling. (2011) (0)
Synthon-based ligand discovery in virtual libraries of over 11 billion compounds (2021) (0)
Translating Genomewide Association Findings into New Therapeutics for Psychiatry 1 (2016) (0)
5-HT Receptor-Associated Proteins (FRAPs) (2006) (0)
Faculty Opinions recommendation of Quantifying secondary transport at single-molecule resolution. (2019) (0)
XFEL structure of the human delta opioid receptor in complex with a bifunctional peptide (2015) (0)
The Design And Use of Covalently Bound Agonists To Probe Kappa‐Opioid Receptors (2008) (0)
5HT/sub 2/ receptors coupled to phospholipase C in rat aorta are modulated by phorbol esters (1986) (0)
REGULATION OF NOREPINEPHRINE-MEDIATED VASCULAR CONTRACTILITY (1985) (0)
Synthesis and in vitro characterization of new salvinorin a analogs incorporating natural amino acids (2011) (0)
Restoration of orexin signaling in the dorsal raphe and locus coeruleus differntially ameliorate symptoms of narcoleptic mice (2013) (0)
Reply: H1-histamine Receptor Affinity Predicts Short-term Weight Gain for Typical and Atypical Antipsychotic Drugs (2003) (0)
How high resolution x-ray crystal structures of D2-like dopamine receptors can guide the development of novel subtype-selective drugs (2018) (0)
N1-Benzenesulfonylgramine (I) and N1-Benzenesulfonylskatole (II): Novel 5-HT6 Receptor Ligand Templates. (2004) (0)
Structural Genomics of the Human Dopamine Receptor System (2022) (0)
Faculty Opinions recommendation of Biased M1-muscarinic-receptor-mutant mice inform the design of next-generation drugs. (2020) (0)
Clozapine, risperidone and spiperone prefer distinct domains of the 5-HT2 serotonin receptor for high affinity binding (1993) (0)
Faculty Opinions recommendation of Phosphoproteomic characterization of the signaling network resulting from activation of chemokine receptor CCR2. (2020) (0)
Erratum: Synthesis and receptor profiling of Stemona alkaloid analogues reveal a potent class of sigma ligands (Proceedings of the National Academy of Sciences of the United States of America (2011) 108, 17, (6727-6732) DOI: 10.1073/pnas.1016558108) (2012) (0)
5-Hydroxytryptamine receptor 2A (2006) (0)
A molecular understanding of drug actions at G protein coupled receptors (2018) (0)
5-Hydroxytryptamine receptor 1B (2010) (0)
Ultra-large library docking for discovering new chemotypes (2019) (0)
Solution NMR structure of Dynorphin 1-13 bound to Kappa Opioid Receptor (2015) (0)
Author response: Structure-based discovery of potent and selective melatonin receptor agonists (2020) (0)
Introduction to the Biochemistry of Pain Special Issue. (2021) (0)
LQ12, A Novel PKC Activator, Enhances sAPP Secretion in PC-12 Cells (1999) (0)
431. Clozapine-induced internalization of the 5-HT2A receptor in vitro (1998) (0)
236 Regulation of the internalization of the 5HT2A receptor in vitro (1997) (0)
Dopamine Receptor D3R-Gi-PD128907 complex (2021) (0)
An autoradiographic study of mianserin-induced down regulation of serotonin (5HT2 and 5HT1C) receptors (1989) (0)
Structural insights into angiotensin receptor signaling modulation by balanced and biased agonists. (2023) (0)
Erratum: Control of serotonergic function in medial prefrontal cortex by serotonin-2A receptors through a glutamate-dependent mechanism (The Journal of Neuroscience (2001) (9856-9866)) (2002) (0)
In vivo Efficacy of Novel Type Preferring MT1 Melatonin Receptor Inverse Agonists in C3H/HeN Mouse Models of Chronobiological Behavior (2020) (0)
Identification of high affinity δ opiate receptors in bovine hippocampus synaptic plasma membranes (1982) (0)
Publisher Correction: Structural basis of ligand recognition at the human MT1 melatonin receptor (2019) (0)
A Randomized, Double-Blind Comparison of Clozapine and High-Dose Olanzapine in Treatment-Resistant Patients With Schizophrenia. Commentary (2008) (0)
Crystal structure of HTR2A with hallucinogenic agonist (2020) (0)

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