Philip S. Portoghese

Philip S. Portoghese's AcademicInfluence.com Rankings

Chemistry

#777

World Rank

#1294

Historical Rank

#334

USA Rank

Organic Chemistry

#281

World Rank

#344

Historical Rank

#75

USA Rank

chemistry Degrees

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Chemistry

Philip S. Portoghese's Degrees

PhD Medicinal Chemistry University of California, San Francisco
Bachelors Chemistry University of California, Berkeley

Why Is Philip S. Portoghese Influential?

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According to Wikipedia, Philip Salvatore Portoghese is an American medicinal chemist who has made notable contributions to the design and synthesis of ligands targeting opioid receptors. He is a Distinguished Professor of Medicinal Chemistry at the University of Minnesota, Twin Cities. He also served as the Editor-in-chief of the Journal of Medicinal Chemistry from 1972 to 2012, when the job was taken on by his departmental colleague, Gunda I. Georg, who shares the Editor-in-chief position with Shaomeng Wang at the University of Michigan.

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Philip S. Portoghese's Published Works

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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

International Union of Pharmacology. XII. Classification of opioid receptors. (1996) (711)
Naltrindole, a highly selective and potent non-peptide δ opioid receptor antagonist (1988) (515)
Binaltorphimine and nor-binaltorphimine, potent and selective kappa-opioid receptor antagonists. (1987) (497)
Antidepressant-Like Effects of κ-Opioid Receptor Antagonists in the Forced Swim Test in Rats (2003) (435)
Nor-binaltorphimine, a highly selective kappa-opioid antagonist in analgesic and receptor binding assays. (1988) (410)
Selective blockage of delta opioid receptors prevents the development of morphine tolerance and dependence in mice. (1991) (405)
A heterodimer-selective agonist shows in vivo relevance of G protein-coupled receptor dimers. (2005) (355)
Differential antagonism of delta opioid agonists by naltrindole and its benzofuran analog (NTB) in mice: evidence for delta opioid receptor subtypes. (1991) (345)
Pharmacological characterization in vivo of the novel opiate, beta-funaltrexamine. (1982) (294)
Application of the message-address concept in the design of highly potent and selective non-peptide delta opioid receptor antagonists. (1988) (291)
Differential antagonism of opioid delta antinociception by [D-Ala2,Leu5,Cys6]enkephalin and naltrindole 5'-isothiocyanate: evidence for delta receptor subtypes. (1991) (278)
A novel opioid receptor site directed alkylating agent with irreversible narcotic antagonistic and reversible agonistic activities. (1980) (274)
Opioid-induced tolerance and dependence in mice is modulated by the distance between pharmacophores in a bivalent ligand series. (2005) (274)
Antidepressant-like effects of kappa-opioid receptor antagonists in the forced swim test in rats. (2003) (261)
Effects of κ-opioid receptor ligands on intracranial self-stimulation in rats (2004) (254)
Morphine promotes the growth of HIV-1 in human peripheral blood mononuclear cell cocultures. (1990) (254)
Design of peptidomimetic delta opioid receptor antagonists using the message-address concept. (1990) (233)
The irreversible narcotic antagonistic and reversible agonistic properties of the fumaramate methyl ester derivative of naltrexone. (1981) (220)
Safety assessment of allylalkoxybenzene derivatives used as flavouring substances - methyl eugenol and estragole. (2002) (211)
Bivalent ligands and the message-address concept in the design of selective opioid receptor antagonists. (1989) (197)
A new concept on the mode of interaction of narcotic analgesics with receptors. (1965) (191)
Kappa receptor regulation of dopamine release from striatum and cortex of rats and guinea pigs. (1988) (178)
Effects of kappa-opioid receptor ligands on intracranial self-stimulation in rats. (2004) (164)
Opioid receptor-mediated inhibition of dopamine and acetylcholine release from slices of rat nucleus accumbens, olfactory tubercle and frontal cortex. (1990) (159)
The FEMA GRAS assessment of benzyl derivatives used as flavor ingredients. (2002) (159)
A highly selective δ1-opioid receptor antagonist : 7-benzylidenenaltrexone (1992) (158)
From models to molecules: opioid receptor dimers, bivalent ligands, and selective opioid receptor probes. (2001) (155)
GRAS flavoring substances 25 (2001) (145)
Effects of kappa opioids on cocaine self-administration by rhesus monkeys. (1997) (145)
Naltrindole, a highly selective and potent non-peptide delta opioid receptor antagonist. (1988) (144)
A single residue, aspartic acid 95, in the delta opioid receptor specifies selective high affinity agonist binding. (1993) (139)
A procedure for the safety evaluation of natural flavor complexes used as ingredients in food: essential oils. (2005) (133)
Spinal opioid delta antinociception in the mouse: mediation by a 5'-NTII-sensitive delta receptor subtype. (1992) (128)
Effect of antagonists selective for mu, delta and kappa opioid receptors on the reinforcing effects of heroin in rats. (1993) (127)
Selective naltrexone-derived opioid receptor antagonists. (1992) (125)
Binaltorphimine-related bivalent ligands and their kappa opioid receptor antagonist selectivity. (1988) (124)
A Bivalent Ligand (KDN-21) Reveals Spinal δ and κ Opioid Receptors Are Organized as Heterodimers That Give Rise to δ1 and κ2 Phenotypes. Selective Targeting of δ−κ Heterodimers (2004) (122)
Effect of Mu Opioid Receptor Blockade on Alcohol Intake in Rats Bred for High Alcohol Drinking (1998) (119)
The delta2-opioid receptor antagonist naltriben selectively attenuates alcohol intake in rats bred for alcohol preference (1995) (118)
Pharmacological profiles of β-funaltrexamine (β-FNA) and β-chlornaltrexamine (β-CNA) on the mouse vas deferens preparation (1982) (117)
Modulation of mu-mediated antinociception in the mouse involves opioid delta-2 receptors. (1992) (117)
Morphine amplifies HIV-1 expression in chronically infected promonocytes cocultured with human brain cells (1994) (114)
Narcotic antagonistic potency of bivalent ligands which contain beta-naltrexamine. Evidence for bridging between proximal recognition sites. (1982) (107)
A bivalent ligand (KDAN-18) containing delta-antagonist and kappa-agonist pharmacophores bridges delta2 and kappa1 opioid receptor phenotypes. (2004) (104)
The FEMA GRAS assessment of trans-anethole used as a flavouring substance. Flavour and Extract Manufacturer's Association. (1999) (100)
Evidence for the interaction of morphine with kappa and delta opioid receptors to induce analgesia in beta-funaltrexamine-treated mice. (1987) (99)
Synthesis and pharmacologic characterization of an alkylating analogue (chlornaltrexamine) of naltrexone with ultralong-lasting narcotic antagonist properties. (1979) (98)
The FEMA GRAS assessment of cinnamyl derivatives used as flavor ingredients. (2004) (96)
Cocaine place preference is blocked by the δ-opioid receptor antagonist, naltrindole (1992) (95)
Role of spacer and address components in peptidomimetic delta opioid receptor antagonists related to naltrindole. (1991) (93)
The delta opioid receptor antagonist naltrindole attenuates both alcohol and saccharin intake in rats selectively bred for alcohol preference (1995) (90)
Affinity labels for opioid receptors. (1985) (90)
Nor-binaltorphimine decreases deprivation and opioid-induced feeding (1990) (88)
Involvement of delta 2 opioid receptors in the development of morphine dependence in mice. (1993) (86)
Edward E. Smissman-Bristol-Myers Squibb Award Address. The role of concepts in structure-activity relationship studies of opioid ligands. (1992) (84)
Molecular docking reveals a novel binding site model for fentanyl at the mu-opioid receptor. (2000) (81)
Relationships between stereostructure and pharmacological activities. (1970) (81)
Ligands that interact with putative MOR-mGluR5 heteromer in mice with inflammatory pain produce potent antinociception (2013) (79)
Stereochemical factors and receptor interactions associated with narcotic analgesics. (1966) (78)
Opioid agonist and antagonist bivalent ligands. The relationship between spacer length and selectivity at multiple opioid receptors. (1986) (78)
The FEMA GRAS assessment of pyrazine derivatives used as flavor ingredients. Flavor and Extract Manufacturers Association. (2002) (77)
7-Benzylidenenaltrexone (BNTX): A selective δ1 opioid receptor antagonist in the mouse spinal cord (1993) (76)
Bivalent ligands that target μ opioid (MOP) and cannabinoid1 (CB1) receptors are potent analgesics devoid of tolerance. (2013) (75)
Potent and selective indolomorphinan antagonists of the kappa-opioid receptor. (2000) (74)
5'-Guanidinonaltrindole, a highly selective and potent κ-opioid receptor antagonist (2000) (73)
Co-administration of morphine and oxycodone vaccines reduces the distribution of 6-monoacetylmorphine and oxycodone to brain in rats. (2012) (73)
Absence of conditioned place preference or reinstatement with bivalent ligands containing mu-opioid receptor agonist and delta-opioid receptor antagonist pharmacophores. (2007) (72)
Role of spinal mu opioid receptors in the development of morphine tolerance and dependence. (1984) (72)
Agonist and antagonist activities of ligands derived from naltrexone and oxymorphone. (1992) (72)
GRAS flavoring substances 18 (1996) (71)
An Oxycodone Conjugate Vaccine Elicits Drug-Specific Antibodies that Reduce Oxycodone Distribution to Brain and Hot-Plate Analgesia (2012) (70)
Opioid agonist and antagonist bivalent ligands as receptor probes. (1982) (70)
The FEMA GRAS Assessment of Lactones Used as Flavour Ingredients (1998) (69)
Contribution of the opioid system to alcohol aversion and alcohol drinking behavior. (1998) (69)
The δ2-opioid receptor antagonist naltriben reduces motivated responding for ethanol (1999) (69)
Mutational evidence for a common kappa antagonist binding pocket in the wild-type kappa and mutant mu[K303E] opioid receptors. (1998) (68)
Naltrindole 5'-isothiocyanate: a nonequilibrium, highly selective delta opioid receptor antagonist. (1990) (68)
Interaction of Bivalent Ligand KDN21 with Heterodimeric δ-κ Opioid Receptors in Human Embryonic Kidney 293 Cells (2005) (68)
Investigation of the selectivity of oxymorphone- and naltrexone-derived ligands via site-directed mutagenesis of opioid receptors: exploring the "address" recognition locus. (2001) (67)
Stereochemical requirements for receptor recognition of the mu-opioid peptide endomorphin-1. (2000) (67)
Opioid efficacy in a C6 glioma cell line stably expressing the delta opioid receptor. (1997) (66)
Stereochemical studies on medicinal agents. IV. Conformational analysis of ephedrine isomers and related compounds. (1967) (63)
The FEMA GRAS assessment of aliphatic and aromatic terpene hydrocarbons used as flavor ingredients. (2011) (63)
Endomorphin-1 potentiates HIV-1 expression in human brain cell cultures: implication of an atypical μ-opoid receptor (1999) (63)
Molecular simulation of dynorphin A-(1-10) binding to extracellular loop 2 of the kappa-opioid receptor. A model for receptor activation. (1997) (63)
Mediation of swim-stress antinociception by the opioid delta 2 receptor in the mouse. (1992) (61)
A selective delta 1 opioid receptor agonist derived from oxymorphone. Evidence for separate recognition sites for delta 1 opioid receptor agonists and antagonists. (1993) (61)
N-naphthoyl-β-naltrexamine (NNTA), a highly selective and potent activator of μ/κ-opioid heteromers (2011) (60)
Kappa opioid antagonist effects of the novel kappa antagonist 5′-guanidinonaltrindole (GNTI) in an assay of schedule-controlled behavior in rhesus monkeys (2002) (60)
The delta receptor is involved in sufentanil-induced respiratory depression--opioid subreceptors mediate different effects. (1992) (59)
Comparative antagonism by naltrexone and naloxone of μ, κ, and δ agonists☆ (1984) (59)
Improved assays for the assessment of ϰ- and δ-properties of opioid ligands (1982) (59)
Criteria for the safety evaluation of flavoring substances. The Expert Panel of the Flavor and Extract Manufacturers Association. (2005) (57)
An approach to the design of receptor-type-selective non-peptide antagonists of peptidergic receptors: delta opioid antagonists. (1991) (56)
Standard opioid agonists activate heteromeric opioid receptors: evidence for morphine and [d-Ala(2)-MePhe(4)-Glyol(5)]enkephalin as selective μ-δ agonists. (2010) (55)
A bivalent ligand (KDN-21) reveals spinal delta and kappa opioid receptors are organized as heterodimers that give rise to delta(1) and kappa(2) phenotypes. Selective targeting of delta-kappa heterodimers. (2004) (55)
Inhibition of Inflammatory and Neuropathic Pain by Targeting a Mu Opioid Receptor/Chemokine Receptor5 Heteromer (MOR-CCR5). (2015) (53)
Upregulation of HIV-1 expression in cocultures of chronically infected promonocytes and human brain cells by dynorphin. (1995) (53)
Reduced antinociception of opioids in rats and mice by vaccination with immunogens containing oxycodone and hydrocodone haptens. (2013) (53)
Stereostructure-activity relationship of opioid agonist and antagonist bivalent ligands. Evidence for bridging between vicinal opioid receptors. (1985) (53)
N-Demethylation of morphine and structurally related compounds with chloroformate esters. (1972) (53)
The FEMA GRAS assessment of furfural used as a flavour ingredient. Flavor and Extract Manufacturers' Association. (1997) (53)
Interaction of [D-Pen2,D-Pen5]enkephalin and [D-Ala2,Glu4]deltorphin with delta-opioid receptor subtypes in vivo. (1994) (53)
Selective kappa antagonist properties of nor-binaltorphimine in the rat MES seizure model. (1989) (52)
Allosteric Interactions between δ and κ Opioid Receptors in Peripheral Sensory Neurons (2012) (52)
Induced association of mu opioid (MOP) and type 2 cholecystokinin (CCK2) receptors by novel bivalent ligands. (2009) (52)
Spinal κ-opiate receptor involvement in the analgesia of pregnancy: effects of intrathecal nor-binaltorphimine, a κ-selective antagonist (1988) (52)
6.beta.-[N,N-Bis(2-chloroethyl)amino]-17-(cyclopropylmethyl)-4,5.alpha.-epoxy-3,14-dihydroxymorphinan (chloranaltrexamine), a potent opioid receptor alkylating agent with ultralong narcotic antagonist activity (1978) (52)
Stereospecific synthesis of the 6.alpha.- and 6.beta.-amino derivatives of naltrexone and oxymorphone (1980) (51)
Role of delta opioid receptors in the reinforcing and discriminative stimulus effects of cocaine in rhesus monkeys. (1995) (50)
Transformation of a κ-Opioid Receptor Antagonist to a κ-Agonist by Transfer of a Guanidinium Group from the 5‘- to 6‘-Position of Naltrindole (2001) (50)
The FEMA GRAS assessment of alicyclic substances used as flavour ingredients. (1996) (49)
kappa Opioid receptor selective affinity labels: electrophilic benzeneacetamides as kappa-selective opioid antagonists. (1994) (49)
The μ, κ and δ properties of various opioid agonists☆ (1986) (49)
Identity of the putative δ1-opioid receptor as a δ–κ heteromer in the mouse spinal cord (2003) (48)
Allylprodine analogues as receptor probes. Evidence that phenolic and nonphenolic ligands interact with different subsites on identical opioid receptors. (1981) (48)
Evidence for delta opioid receptor subtypes regulating adenylyl cyclase activity in rat brain. (1994) (48)
Kappa-opioid receptor agonist suppression of HIV-1 expression in CD4+ lymphocytes. (2001) (46)
Peptides as receptor selectivity modulators of opiate pharmacophores. (1986) (46)
Mediation of nitrous oxide analgesia in mice by spinal and supraspinal κ-opioid receptors (1990) (45)
Chloroxymorphamine, and opioid receptor site-directed alkylating agent having narcotic agonist activity. (1979) (45)
Enkephalin antinociception in mice is mediated by δ1- and δ2-opioid receptors in the brain and spinal cord, respectively (1993) (45)
Homology Modeling and Molecular Dynamics Simulations of the Mu Opioid Receptor in a Membrane–Aqueous System (2005) (44)
Antagonism by chlornaltrexamine of some effects of Δ9-tetrahydrocannabinol in rats (1981) (43)
Different receptor sites mediate opioid agonism and antagonism. (1983) (43)
The FEMA GRAS assessment of hydroxy- and alkoxy-substituted benzyl derivatives used as flavor ingredients. (2005) (43)
κ-Selective Opiate Antagonist Nor-Binaltorphimine Improves Outcome After Traumatic Spinal Cord Injury in Rats (1987) (43)
Clinically employed opioid analgesics produce antinociception via μ-δ opioid receptor heteromers in Rhesus monkeys. (2012) (42)
Cross-tolerance studies in the spinal cord of beta-FNA-treated mice provides further evidence for delta opioid receptor subtypes. (1991) (42)
Application of the message-address concept to the docking of naltrexone and selective naltrexone-derived opioid antagonists into opioid receptor models (1996) (42)
delta-Opioid receptor binding in mouse brain: evidence for heterogeneous binding sites. (1992) (41)
kappa-Opioid antagonist improves cellular bioenergetics and recovery after traumatic brain injury. (1991) (40)
Conformational analysis and automated receptor docking of selective arylacetamide-based kappa-opioid agonists. (1998) (39)
Gras flavoring substances (2000) (39)
Effects of β-funaltrexamine (β-FNA) on morphine dependence in rats and monkeys (1986) (39)
Targeting putative mu opioid/metabotropic glutamate receptor-5 heteromers produces potent antinociception in a chronic murine bone cancer model. (2014) (39)
Suppression by nor-binaltorphimine of kappa opioid-mediated diuresis in rats. (1988) (38)
The FEMA GRAS assessment of alpha,beta-unsaturated aldehydes and related substances used as flavor ingredients. (2008) (38)
Opioid receptor binding characteristics of the non-equilibrium μ antagonist, β-funaltrexamine (β-FNA)☆ (1985) (38)
Delta-opioid receptor antagonists attenuate motor activity induced by amphetamine but not cocaine. (1993) (37)
Stereochemical studies on medicinal agents. 23. Synthesis and biological evaluation of 6-amino derivatives of naloxone and naltrexone. (1977) (37)
Influence of Pseudoallylic Strain on the Conformational Preference of 4-Methyl-4-phenylpipecolic Acid Derivatives (1985) (37)
Research sectionThe FEMA GRAS assessment of furfural used as a flavour ingredient (1997) (36)
Synthesis of naltrexone-derived delta-opioid antagonists. Role of conformation of the delta address moiety. (1994) (36)
A bivalent ligand (KMN-21) antagonist for mu/kappa heterodimeric opioid receptors. (2009) (35)
From Models to Molecules: Opioid Receptor Dimers, Bivalent Ligands, and Selective Opioid Receptor Probes (2001) (35)
TENA, a selective kappa opioid receptor antagonist. (1985) (35)
Involvement of delta 2 opioid receptors in acute dependence on morphine in mice. (1993) (35)
Safety evaluation of natural flavour complexes. (2003) (34)
Only one pharmacophore is required for the kappa opioid antagonist selectivity of norbinaltorphimine. (1988) (34)
Binding of norbinaltorphimine (norBNI) congeners to wild-type and mutant mu and kappa opioid receptors: molecular recognition loci for the pharmacophore and address components of kappa antagonists. (2000) (34)
Synthesis and biological evaluation of phosphonamidate peptide inhibitors of enkephalinase and angiotensin-converting enzyme. (1985) (34)
Modulation of morphine antinociception by swim-stress in the mouse: involvement of supraspinal opioid delta-2 receptors. (1993) (34)
Interaction of bivalent ligand KDN21 with heterodimeric delta-kappa opioid receptors in human embryonic kidney 293 cells. (2005) (34)
The delta 2-opioid receptor antagonist naltriben reduces motivated responding for ethanol. (1999) (33)
Characterization of Opioid Receptors Modulating Neurogenic Contractions of Circular Muscle from Porcine Ileum and Evidence That δ- and κ-Opioid Receptors Are Coexpressed in Myenteric Neurons (2001) (33)
Role of the spacer in conferring kappa opioid receptor selectivity to bivalent ligands related to norbinaltorphimine. (1991) (33)
Bicyclic Bases. Synthesis of 2,5-Diazabicyclo[2.2.1]heptanes1 (1966) (33)
Cold water swim stress- and delta-2 opioid-induced analgesia are modulated by spinal gamma-aminobutyric acidA receptors. (1995) (32)
Stereochemical studies on medicinal agents. 20. Absolute configuration and analgetic potency alpha-promedol enantiomers. The role of the C-4 chiral center in conferring stereoselectivity in axial- and equatorial-phenyl prodine congeners. (1976) (32)
Pharmacological studies with an alkylating narcotic agonist, chloroxymorphamine, and antagonist, chlornaltrexamine. (1980) (32)
Delta opioid antagonist activity and binding studies of regioisomeric isothiocyanate derivatives of naltrindole: evidence for delta receptor subtypes. (1992) (31)
Naltrindole, an opioid delta receptor antagonist, blocks cocaine-induced facilitation of responding for rewarding brain stimulation. (1993) (30)
A highly selective delta 1-opioid receptor antagonist: 7-benzylidenenaltrexone. (1992) (30)
An immunocytochemical-derived correlate for evaluating the bridging of heteromeric mu-delta opioid protomers by bivalent ligands. (2013) (30)
The effect of selective opioid antagonists on butorphanol-induced feeding (1994) (29)
Putative Kappa Opioid Heteromers As Targets for Developing Analgesics Free of Adverse Effects (2014) (29)
Effects of the selective kappa opioid antagonist, nor-binaltorphimine, on electrically-elicited feeding in the rat. (1989) (29)
The FEMA GRAS assessment of phenethyl alcohol, aldehyde, acid, and related acetals and esters used as flavor ingredients. (2005) (29)
Supraspinal delta receptor subtype activity of heroin and 6-monoacetylmorphine in Swiss Webster mice. (1994) (28)
Synthesis and in vitro characterization of radioiodinatable benzodiazepines selective for type 1 and type 2 cholecystokinin receptors. (2009) (28)
Comparative antagonism by naltrexone and naloxone of mu, kappa, and delta agonists. (1984) (28)
Transformation of a kappa-opioid receptor antagonist to a kappa-agonist by transfer of a guanidinium group from the 5'- to 6'-position of naltrindole. (2001) (28)
5'-Guanidinonaltrindole, a highly selective and potent kappa-opioid receptor antagonist. (2000) (28)
Design and synthesis of naltrexone-derived affinity labels with nonequilibrium opioid agonist and antagonist activities. Evidence for the existence of different mu receptor subtypes in different tissues. (1984) (28)
The FEMA GRAS assessment of aromatic substituted secondary alcohols, ketones, and related esters used as flavor ingredients. (2007) (28)
Stereochemical studies on medicinal agents. 12. The distinction of enantiotopic groups in the interaction of 1-methyl-4-phenyl-4-propionoxypiperidine with analgetic receptors. (1973) (27)
Monophenylation of Morphinan-6-ones with Diphenyliodonium Iodide (1995) (27)
Evidence for a single functional opioid delta receptor subtype in the mouse isolated vas deferens. (1993) (26)
The δ opioid receptor agonist SNC80 selectively activates heteromeric μ-δ opioid receptors. (2012) (26)
7-Benzylidenenaltrexone (BNTX): a selective delta 1 opioid receptor antagonist in the mouse spinal cord. (1993) (26)
Structure-activity relationship of N17'-substituted norbinaltorphimine congeners. Role of the N17' basic group in the interaction with a putative address subsite on the kappa opioid receptor. (1994) (26)
Allosteric interactions between delta and kappa opioid receptors in peripheral sensory neurons (2011) (26)
Stereochemical studies on medicinal agents. V. Synthesis, configuration, and pharmacological activity of pipradrol enantiomers. (1968) (26)
MDAN-21: A Bivalent Opioid Ligand Containing mu-Agonist and Delta-Antagonist Pharmacophores and Its Effects in Rhesus Monkeys (2012) (26)
Cocaine place preference is blocked by the delta-opioid receptor antagonist, naltrindole. (1992) (25)
Safety assessment of ingested heterocyclic amines: initial report. (1993) (25)
Synthesis and opioid antagonist potencies of naltrexamine bivalent ligands with conformationally restricted spacers. (1986) (25)
Mu- and delta-opioid receptor-mediated inhibition of adenylate cyclase activity stimulated by released endogenous dopamine in rat neostriatal slices; demonstration of potent delta-agonist activity of bremazocine. (1989) (25)
Opioid receptor antagonists discriminate between presynaptic mu and delta receptors and the adenylate cyclase-coupled opioid receptor complex in the brain. (1992) (25)
Identity of the putative delta1-opioid receptor as a delta-kappa heteromer in the mouse spinal cord. (2003) (25)
Selective opioid antagonist effects on opioid-induced inhibition of release of norepinephrine in guinea pig cortex (1989) (25)
MECHANISM OF THE PRINS REACTION. STEREOASPECTS OF THE FORMATION OF 1,3-DIOXANES. (1965) (24)
Efficient Preparation of Polyfunctional a-Diketones from Carboxylic Acids (1986) (24)
A remarkable change of opioid receptor selectivity on the attachment of a peptidomimetic kappa address element to the delta antagonist, natrindole: 5'-[N2-alkylamidino)methyl]naltrindole derivatives as a novel class of kappa opioid receptor antagonists. (1993) (24)
Spinal δ2 but not δ1 opioid receptors are involved in intracereboventricular β-endorphin-induced antinociception in the mouse (1993) (24)
Arylacetamide-derived fluorescent probes: synthesis, biological evaluation, and direct fluorescent labeling of kappa opioid receptors in mouse microglial cells. (1996) (24)
Naloxone acts as a potent analgesic in transgenic mouse models of sickle cell anemia (2007) (24)
Lack of involvement of delta-1 opioid receptors in the development of physical dependence on morphine in mice. (1994) (24)
Molecular Basis for Binding and Subtype Selectivity of 1,4-Benzodiazepine Antagonist Ligands of the Cholecystokinin Receptor* (2012) (23)
Synthesis and kappa-opioid antagonist selectivity of a norbinaltorphimine congener. Identification of the address moiety required for kappa-antagonist activity. (1993) (23)
2-(3,4-Dichlorophenyl)-N-methyl-N-[(1S)-1-(3-isothiocyanatophenyl)-2-(1-pyrrolidinyl)ethyl]acetamide: an opioid receptor affinity label that produces selective and long-lasting kappa antagonism in mice. (1994) (23)
Isosteric replacement of acidic with neutral residues in extracellular loop-2 of the kappa-opioid receptor does not affect dynorphin A(1-13) affinity and function. (2000) (23)
α-Cyanation of Tertiary Amines (1980) (22)
Stereochemical studies on medicinal agents. VII. Absolute stereochemistry of methadol isomers and the role of the 6-methyl group in analgetic activity. (1969) (22)
Importance of C-6 chirality in conferring irreversible opioid antagonism to naltrexone-derived affinity labels. (1983) (22)
Relative Hydrolytic Rates of Certain Alkyl (b) dl-α-(2-Piperidyl)-phenylacetates (1961) (22)
N-benzylnaltrindoles as long-acting delta-opioid receptor antagonists. (1994) (22)
Stereochemical studies on medicinal agents. 13. Correlation of the solid-state conformations of 1,3,5-trimethyl- and 1,3-dimethyl-4-phenyl-4-propionoxypiperidine enantiomers with their absolute stereoselectivity at analgetic receptors. (1973) (21)
Synthesis and adrenoreceptor blocking action of aziridinium ions derived from phenoxybenzamine and dibenamine. (1976) (21)
A novel pyrrole synthesis via reaction of ketones with N-aminoimides (1986) (21)
The facility of formation of a .DELTA.6 bond in dihydromorphinone and related opiates (1989) (21)
Stereochemical studies on medicinal agents. VI. Bicyclic bases. Synthesis and pharmacology of epimeric bridged analogs of meperidine, 2-methyl-5-phenyl-5-carbethoxy-2-azabicyclo[2.2.1]heptane. (1968) (21)
Consequences of opioid receptor mutation on actions of univalent and bivalent kappa and delta ligands (2010) (21)
Heteromer Induction: An Approach to Unique Pharmacology? (2017) (20)
A bivalent compound targeting CCR5 and the mu opioid receptor treats inflammatory arthritis pain in mice without inducing pharmacologic tolerance (2018) (20)
Synthesis and evaluation of 1- and 2-substituted fentanyl analogues for opioid activity. (1983) (19)
Receptors for opioid peptides in the guinea-pig ileum. (1985) (19)
Bivalent ligand that activates mu opioid receptor and antagonizes mGluR5 receptor reduces neuropathic pain in mice (2017) (19)
Opioid agonist and antagonist activities of peripherally selective derivatives of naltrexamine and oxymorphamine. (1989) (19)
STEREOCHEMICAL STUDIES ON MEDICINAL AGENTS. I. ABSOLUTE CONFIGURATION OF CERTAIN ANALGESIC (-)-N-(2-(PHENALKYLMETHYLAMINO)PROPYL)PROPIONANILIDES. (1964) (19)
Opioid agonist and antagonist activities of morphindoles related to naltrindole. (1992) (19)
Bicyclic bases : Synthesis and nuclear magnetic resonance investigation of some chiral 2-oxa-5-azabicyclo[2.2.1]Heptane derivatives☆☆☆★ (1971) (18)
Reactivity of glutathione with a,-unsaturated ketone flavouring substances (1989) (18)
Hybrid bivalent ligands with opiate and enkephalin pharmacophores. (1987) (18)
Stereoisomeric ligands as opioid receptor probes (1978) (18)
Stereochemical studies on medicinal agents. 16. Conformational studies of methadone and isomethadone utilizing circular dichroism and proton magnetic resonance. (1974) (18)
Crystal structures of alpha- and beta-funaltrexamine: conformational requirement of the fumaramate moiety in the irreversible blockage of mu opioid receptors. (1986) (18)
Modulation of cell surface expression of nonactivated cholecystokinin receptors using bivalent ligand-induced internalization. (2010) (17)
Selectivity of δ- and κ-Opioid Ligands Depends on the Route of Central Administration in Mice (2007) (17)
Inhibition of substance P release from spinal cord tissue after pretreatment with capsaicin does not mediate the antinociceptive effect of capsaicin in adult mice (1997) (17)
Enkephalin antinociception in mice is mediated by delta 1- and delta 2-opioid receptors in the brain and spinal cord, respectively. (1993) (17)
Maintenance of acute morphine tolerance in mice by selective blockage of kappa opioid receptors with norbinaltorphimine. (1992) (17)
Stereochemical studies on medicinal agents. 8. Absolute stereochemistries of isomethadol isomers. (1970) (17)
Characterization of opioid receptors modulating neurogenic contractions of circular muscle from porcine ileum and evidence that delta- and kappa-opioid receptors are coexpressed in myenteric neurons. (2001) (16)
Affinity labels as tools for the identification of opioid receptor recognition sites. (2001) (16)
Stereochemical studies on medicinal agents. 18. Absolute configuration and analgetic potency of trimeperidine enatiomers. (1974) (16)
Comparison of Peptidic and Nonpeptidic δ-Opioid Agonists on Guanosine 5′-O-(3-[35S]thio)triphosphate ([35S]GTPγS) Binding in Brain Slices from Sprague-Dawley Rats (2005) (16)
Stereochemical studies on medicinal agents. 21. Investigation of the role of conformational factors in the action of diphenylpropylamines. Synthesis and analgetic potency of 5-methylmethadone diastereomers. (1976) (16)
Oxidation of oxyphenbutazone by sheep vesicular gland microsomes and lipoxygenase. (1975) (16)
Difference between μ-receptors in the guinea pig ileum and the mouse vas deferens (1983) (16)
Electrophilic N-benzylnaltrindoles as delta opioid receptor-selective antagonists. (1995) (16)
Methadone and heroin antinociception: predominant delta-opioid-receptor responses in methadone-tolerant mice. (2002) (16)
Pharmacological profiles of beta-funaltrexamine (beta-FNA) and beta-chlornaltrexamine (beta-CNA) on the mouse vas deferens preparation. (1982) (16)
NTI4F: a non-peptide fluorescent probe selective for functional delta opioid receptors (1998) (15)
2-azatricyclo[2.2.1.01,6]heptane: Synthesis and conversion to 2-azabicyclo[2.2.1]heptanes (1973) (15)
Pharmacological evidence for a 7-benzylidenenaltrexone-preferring opioid receptor mediating the inhibitory actions of peptidic delta- and mu-opioid agonists on neurogenic ion transport in porcine ileal mucosa. (2001) (15)
An explanation for the failure of aminomethanesulfonic acid to form sulfonamides. Acyl chloride-promoted generation of α-carboxamidoalkylating electrophiles. (1981) (15)
Spinal δ2-, but not δ1-, μ-, or κ-opioid receptors are involved in the tail-flick inhibition induced by β-endorphin from nucleus raphe obscurus in the pentobarbital-anesthetized rat (1995) (15)
Endogenous opioid peptides suppress cytokine-mediated upregulation of HIV-1 expression in the chronically infected promonocyte clone U1. (1995) (15)
Stereochemical studies on medicinal agents. 19. X-ray crystal structures of two (+/-)-allylprodine diastereomers. The role of the allyl group in conferring high stereoselectivity and potency at analgetic receptors. (1976) (15)
Stereochemical studies on medicinal agents. 10. The role of chirality in alpha-adrenergic receptor blockage by (plus)-and(minus)-phenoxybenzamine hydrochloride. (1971) (14)
Alkylation of opioid receptor subtypes by alpha-chlornaltrexamine produces concurrent irreversible agonistic and irreversible antagonistic activities. (1983) (14)
Reporter affinity labels: an o-phthalaldehyde derivative of beta-naltrexamine as a fluorogenic ligand for opioid receptors. (2000) (14)
Sterochemical studies on medicinal agents. 15. Absolute configurations and analgetic potencies of enantiomeric diastereomers of 3-allyl-1-methyl-4-phenyl-4-propionoxypiperidine. (1973) (14)
7-Spiroindanyl derivatives of naltrexone and oxymorphone as selective ligands for delta opioid receptors. (1997) (14)
Naphthalene dicarboxaldehyde as an electrophilic fluorogenic moiety for affinity labeling: application to opioid receptor affinity labels with greatly improved fluorogenic properties. (2002) (14)
Synthesis, X-ray crystallographic determination, and opioid activity of erythro-5-methylmethadone enantiomers. Evidence which suggests that mu and delta opioid receptors possess different stereochemical requirements. (1982) (14)
Opioid antagonist activity of naltrexone-derived bivalent ligands: importance of a properly oriented molecular scaffold to guide "address" recognition at kappa opioid receptors. (1996) (14)
Differential antagonism by naltrindole-5'-isothiocyanate on [3H]DSLET and [3H]DPDPE binding to striatal slices of mice. (1993) (13)
Synthesis and biological evaluation of a metazocine-containing enkephalinamide. Evidence for nonidentical roles of the tyramine moiety in opiates and opioid peptides. (1982) (13)
N,N-dialkylated leucine enkephalins as potential delta opioid receptor antagonists. (1987) (13)
The bivalent ligand MCC22 potently attenuates hyperalgesia in a mouse model of cisplatin-evoked neuropathic pain without tolerance or reward (2019) (13)
Synthesis and biological evaluation of 9,11-azo-13-oxa-15-hydroxyprostanoic acid, a potent inhibitor of platelet aggregation. (1979) (13)
Synthesis and evaluation of melphalan-containing N,N-dialkylenkephalin analogues as irreversible antagonists of the δ opioid receptor (1987) (13)
Design of peptidomimetic .delta. opioid receptor antagonists using the message-address concept [Erratum to document cited in CA112(25):235659s] (1990) (13)
Selective Nonpeptide Opioid Antagonists (1993) (13)
β-funaltrexamine (β-FNA) and neural tumor response in mice (1985) (13)
7'-Substituted amino acid conjugates of naltrindole. Hydrophilic groups as determinants of selective antagonism of delta 1 opioid receptor-mediated antinociception in mice. (1995) (13)
Synthesis of 7-arylmorphinans. Probing the "address" requirements for selectivity at opioid delta receptors. (1998) (13)
Potential nonequilibrium analgetic receptor inactivators. Synthesis and biological activities of N-acylanileridines. (1971) (13)
Aspartic acid conjugates of 2-(3,4-dichlorophenyl)-N-methyl-N-[(1S)-1(3-aminophenyl)-2-(1-pyrrolidi nyl) ethyl]acetamide: kappa opioid receptor agonists with limited access to the central nervous system. (1996) (13)
Stereochemistry of methadol diastereomers. (1966) (13)
Stereochemical studies on medicinal agents. 14. Relative stereochemistries and analgetic potencies of diastereomeric 3-allyl and 3-propyl derivatives of 1-methyl-4-phenyl-4-propionoxypiperidine. (1973) (12)
Pyrrolomorphinans as delta opioid receptor antagonists. The role of steric hindrance in conferring selectivity. (1997) (12)
Bicyclic bases : Synthesis, configuration, and NMR analysis of N-tosyl-2-thia-5-azabicyclo[2.2.1]heptane-2-oxides☆☆☆ (1971) (12)
Stereochemical studies on medicinal agents. 11. Metabolism and distribution of prodine isomers in mice. (1972) (11)
Relation between analgetic ED50 dose and time-course brain levels of N-alkylnormeperidine homologs (1976) (11)
Pharmacokinetics, metabolism, and urinary excretion of ( 3 H)alphaprodine in dogs. (1972) (11)
Absence of Asymmetric Induction in the Lithium Aluminum Hydride—d-Camphor Reduction of Ketones (1962) (11)
Bimorphinans as Highly Selective, Potent K Opioid Receptor Antagonists. (1987) (11)
The crystal structure of a bimorphinan with highly selective kappa opioid receptor antagonist activity (1987) (11)
Opioid receptor binding characteristics of the non-equilibrium mu antagonist, beta-funaltrexamine (beta-FNA). (1985) (11)
Possible contribution of a glutathione conjugate to the long-duration action of beta-funaltrexamine. (1993) (11)
A circular dichroism study of the interaction of sodium and potassium ions with methionine-enkephalin. (1976) (11)
Stereochemical studies on medicinal agents. 25. Absolute configuration and analgetic potency of beta-1,2-dimethyl-2-phenyl-4-(propionyloxy)piperidine enantiomers. (1982) (11)
7-Arylidenenaltrexones as Selective δ1 Opioid Receptor Antagonists (1998) (11)
Fluorescent N-benzylnaltrindole analogues as potential delta opioid receptor selective probes (1997) (11)
Investigation of phenolic bioisosterism in opiates: 3-sulfonamido analogues of naltrexone and oxymorphone. (2000) (11)
Targeting MOR-mGluR5 heteromers reduces bone cancer pain by activating MOR and inhibiting mGluR5 (2019) (11)
The design of delta-selective opioid receptor antagonists. (1993) (10)
Stereospecific synthesis of pseudocodeine: [2,3]-sigmatropic rearrangement using selenium intermediates (1998) (10)
An Analysis of the Conserved Residues between Halobacterial Retinal Proteins and G-Protein Coupled Receptors: Implications for GPCR Modeling (1996) (10)
Covalently induced activation of the delta opioid receptor by a fluorogenic affinity label, 7'-(phthalaldehydecarboxamido)naltrindole (PNTI). (2001) (10)
A κ Opioid Pharmacophore Becomes a Spinally Selective κ-δ Agonist When Modified with a Basic Extender Arm. (2011) (10)
Stereochemical studies on medicinal agents. 17. Synthesis, absolute configuration, and analgetic potency of enantiomeric diastereomers of 3-ethyl and 3-propyl derivatives of 1-methyl-4-phenyl-4-propionoxypiperidine. (1974) (10)
The mu, kappa and delta properties of various opioid agonists. (1986) (10)
9, 11-Azo-12-oxa-15-hydroxyprostanoic acid: a potent thromboxane synthetase inhibitor and a PGH2/TxA2 receptor antagonist. (1979) (10)
Morphine Tolerance in Mice Changes Response of Heroin from μ to δ Opioid Receptors (2000) (10)
Molecular modeling of the conformational and sodium ion binding properties of the oligosaccharide component of ganglioside GM1 (1994) (10)
Synthesis of Novel 6β,14-Epoxy-Bridged Opiates (1990) (10)
[Interaction of S-(+)-ketamine with opiate receptors. Effects on EEG, evoked potentials and respiration in awake dogs]. (1994) (10)
Characterization of Specific Opioid Binding Sites in Neural Membranes from the Myenteric Plexus of Porcine Small Intestine (2004) (10)
Isolation of selective 3H-chlornaltrexamine-bound complexes, possible opioid receptor components in brains of mice. (1980) (10)
Selectivity of delta- and kappa-opioid ligands depends on the route of central administration in mice. (2007) (10)
Potential nonequilibrium analgetic receptor inactivators. Further pharmacologic studies of N-acylanileridines. (1974) (10)
o-Naphthalenedicarboxaldehyde derivative of 7'-aminonaltrindole as a selective delta-opioid receptor affinity label. (2007) (10)
Spinal kappa-opiate receptor involvement in the analgesia of pregnancy: effects of intrathecal nor-binaltorphimine, a kappa-selective antagonist. (1988) (9)
Absolute stereochemistry and analgesic potency of prodine enantiomers. (1968) (9)
Irreversible blockage of opioid receptor types by ester homologues of beta-funaltrexamine. (1986) (9)
A convenient, general procedure for preparing specifically [3H]-labeled amines. Synthesis of [3H]-meperidine hydrochloride. (1973) (9)
X-ray crystal structure of the opioid ligand naltrexonazine. (1987) (9)
Bivalent ligand MCC22 potently attenuates nociception in a murine model of sickle cell disease (2018) (9)
Antagonism by chlornaltrexamine of some effects of delta 9-tetrahydrocannabinol in rats. (1981) (9)
Specific cross-linking of Lys233 and Cys235 in the mu opioid receptor by a reporter affinity label. (2005) (9)
Stereochemical Studies on Medicinal Agents III. Influence of Length of N-aralkyl Group on Configurational Selectivity of Receptors Toward Enantiomeric Basic Anilide Analgesics (1965) (9)
Pharmacology of highly selective, non-peptide delta opioid receptor antagonists (1990) (8)
Antagonism of morphine-induced behavioral suppression by opiate receptor alkylators (1982) (8)
Activity of N-methyl-alpha- and -beta-funaltrexamine at opioid receptors. (1986) (8)
Improved assays for the assessment of kappa- and delta-properties of opioid ligands. (1982) (8)
Opioid activity of spinally selective analogues of N-naphthoyl-β-naltrexamine in HEK-293 cells and mice. (2012) (8)
N1'‐(p‐[18F]Fluorobenzyl)naltrindole (p‐[18F]BNTI) as a potential PET imaging agent for DOP receptors (2006) (8)
Stereochemistry and innate immune recognition: (+)‐norbinaltorphimine targets myeloid differentiation protein 2 and inhibits toll‐like receptor 4 signaling (2019) (8)
Activities of morphinone and N-(cyclopropylmethyl)normorphinone at opioid receptors. (1984) (8)
Stereoselectivity of the Reduction of Naltrexone Oxime with Borane (1986) (8)
Opioid receptors (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database (2019) (8)
Combined Glia Inhibition and Opioid Receptor Agonism Afford Highly Potent Analgesics without Tolerance. (2018) (8)
Kappa-selective opiate antagonist nor-binaltorphimine improves outcome after traumatic spinal cord injury in rats. (1987) (7)
Linear free energy relationship among analgesic N-substituted phenylpiperidine derivatives. Method of detecting similar modes of molecular binding to common receptors. (1965) (7)
Opiate Dienes as Dienophiles in the Diels−Alder Reaction with 1-Cyano-o-quinodimethane (1998) (7)
Investigation of the structural requirements for the kappa-selective opioid receptor antagonist, 6 beta,6 beta'-[ethylenebis(oxyethyleneimino)]bis[17-(cyclopropylmethyl)- 4,5 alpha-epoxymorphinan-3,14-diol] (TENA). (1986) (7)
Binaltorphimine-related bivalent ligands and their .kappa. opioid receptor antagonist selectivity [Erratum to document cited in CA108(17):150771q] (1988) (7)
The State of the Journal at Its 50th Publication Volume (2007) (7)
Comparison of peptidic and nonpeptidic delta-opioid agonists on guanosine 5'-O-(3-[35S]thio)triphosphate ([35S]GTPgammaS) binding in brain slices from Sprague-Dawley rats. (2005) (7)
Long-acting agonist and antagonist activities of naltrexamine bivalent ligands in mice. (1990) (7)
3-Hydroxy-17-aralkylmorphinans as potential opiate receptor-site-directed alkylating agents. (1977) (7)
The FEMA GRAS assessment of lactones used as a flavour ingredients. The Flavor and Extract Manufacturers' Association. Generally recognized as safe. (1998) (7)
The δ1-opioid receptor antagonist, 7-benzylspiroindanylnaltrexone, prolongs renal allograft survival in a rat model (1998) (7)
Relative hydrolytic rates of certain alkyl (b) dl-alpha-(2-piperidyl)-phenylacetates. (1961) (6)
Chemical and nuclear magnetic resonance studies of 3,3-diphenyltetrahydrofuran derivatives (1969) (6)
STEREOCHEMICAL STUDIES ON MEDICINAL AGENTS. II. ABSOLUTE CONFIGURATION OF (--)-PHENAMPROMIDE. (1965) (6)
Synthesis and 124I‐labeling of m‐iodophenylpyrrolomorphinan as a potential PET imaging agent for delta opioid (DOP) receptors (2007) (6)
Mediation of nitrous oxide analgesia in mice by spinal and supraspinal kappa-opioid receptors. (1990) (6)
Spinal delta 2-, but not delta 1-, mu-, or kappa-opioid receptors are involved in the tail-flick inhibition induced by beta-endorphin from nucleus raphe obscurus in the pentobarbital-anesthetized rat. (1995) (6)
Stereoaspects of the Prins Reaction of Anethole1 (1962) (6)
Spinal Delta Opioid Receptor Subtype Activity of 6-monoacetylmorphine in Swiss Webster Mice (1997) (6)
Opioid agonist and antagonist activities of monofunctional nitrogen mustard analogues of beta-chlornaltrexamine. (1987) (6)
Stereochemical studies on medicinal agents. 9. Bicyclic bases. Synthesis and biological activities of epimeric quaternary derivatives of 2-oxa-5-azabicyclo [2.2.1]heptane. (1971) (6)
Erratum: 6β-[N,N-Bis(2-chloro-ethyl)amino]-17-(cyclopropylmethyl)-4,5α-epoxy- 3,14-dihydroxymorphinan (chlornaltrexamine), a potent opioid receptor alkylating agent with ultralong narcotic antagonist activity (Journal of Medicinal Chemistry (1978) 21, (598)) (1978) (6)
Effects of beta-funaltrexamine (beta-FNA) on morphine dependence in rats and monkeys. (1986) (6)
A convenient synthesis of 1‐methyl‐4‐oxopiṕecolic acid methyl ester (1983) (6)
Essentials of Molecular Pharmacology (1971) (6)
Facile intramolecular O-14−C-7 acetyl transfer in opiate 14-acetate esters (1990) (6)
14-Desoxy analogues of naltrindole and 7-spiroindanyloxymorphone: the role of the 14-hydroxy group at delta opioid receptors. (1998) (6)
A novel prostaglandin endoperoxide mimic, prostaglandin F2alpha acetal. (1977) (5)
Bieyclic bases . Synthesis and stereochemical studies of chiral 5‐substituted N‐tosyl‐2‐azabicyclo[2.2.1[ heptanes (1971) (5)
Difference between mu-receptors in the guinea pig ileum and the mouse vas deferens. (1983) (5)
Nonbonded13C-14N dipole-dipole interactions (1989) (5)
6β-(N,N-BIS(2-CHLOROETHYL)AMINO)-17-(CYCLOPROPYLMETHYL)-4,5α-EPOXY-3# ,14-DIHYDROXYMORPHINAN (CHLORANALTREXAMINE), A POTENT OPIOID RECEPTOR ALKYLATING AGENT WITH ULTRALONG NARCOTIC ANTAGONIST ACTIVITY (1978) (5)
Nonequilibrium opioid antagonist activity of 6,14-dideoxynaltrexone derivatives. (1987) (5)
Impact of recombinant DNA technology and molecular modeling on the practice of medicinal chemistry: Structure-activity analysis of opioid ligands (1999) (5)
7-spirobenzocyclohexyl derivatives of naltrexone, oxymorphone, and hydromorphone as selective opioid receptor ligands. (1997) (5)
DESIGN AND SYNTHESIS OF NALTREXONE-DERIVED AFFINITY LABELS WITH NONEQUILIBRIUM OPIOID AGONIST AND ANTAGONIST ACTIVITIES. EVIDENCE FOR THE EXISTENCE OF DIFFERENT μ RECEPTOR SUBTYPES IN DIFFERENT TISSUES (1985) (5)
Methadone conformation and opioid activity. (1983) (5)
The mixed antinociceptive agonist-antagonist activity of beta-endorphin(1-27) in mice. (1993) (5)
Investigation of 4-(3-hydroxyphenyl)-4-methylpipecolic acid as a conformationally restricted mimic of the tyrosyl residue of leucine-enkephalinamide. (1986) (5)
The Design of δ-Selective Opioid Receptor Antagonists. (1994) (5)
A simple, stereoselective synthesis of a prostaglandin endoperoxide analog (1976) (5)
Stereochemistry of isomethadol isomers (1966) (5)
Synthesis and Biological Activity of Analogues of β-Chlornaltrexamine and β-Funaltrexamine at Opioid Receptors (1986) (4)
My farewell to the Journal of Medicinal Chemistry. (2011) (4)
Morphine tolerance in mice changes response of heroin from mu to delta opioid receptors. (2000) (4)
Editorial - Ethical Guidelines to Publication of Chemical Research (1990) (4)
Molecular recognition at kappa opioid receptors (2001) (4)
DIPPA: An opioid receptor affinity label that produces selective and long-lasting κ antagonism in mice (1994) (4)
Translocation of ligand conformational free energy in receptor activation: a possible functional role of conformational isomerism in drug action. (1971) (4)
Stereochemistry of Cyanide Ion Addition to 3,4,5,6-Tetrahydropyridinium Derivatives (1983) (4)
Affinity labels as probes for opioid receptor types and subtypes. (1986) (4)
Combinatorial Chemistry Editorial Policy (1998) (4)
Synthesis and biological evaluation of 2.3-diazabicyclo[2.2.1]heptane derivatives as prostaglandin endoperoxide analogs. (1980) (4)
The crystal structure and molecular conformation of threo 5-methylmetadone in relation to opioid receptor binding (1984) (4)
Additions and Corrections - 6β[N,N-Bis(2-chloroethyl)amino]-17-(cyclopropylmethyl)-4,5α-epoxy-3,14-dihydroxymorphinan(Chlornaltrexamine), a Potent Opioid Receptor Alkylating Agent with Ultralong Narcotic Antagonist Activity (1978) (4)
A NOVEL PROSTAGLANDIN ENDOPEROXIDE MIMIC, PROSTAGLANDIN F2α ACETAL (1977) (4)
Differential antagonism of DSLET and DPDPE by novel delta opioid receptor antagonists (1990) (4)
Spinal delta 2 but not delta 1 opioid receptors are involved in intracerebroventricular beta-endorphin-induced antinociception in the mouse. (1993) (4)
Irreversible binding of [3H]β-funaltremaxine to brain slices of morphine-tolerant and -dependent mice (1988) (4)
FBNTI, a DOR-selective antagonist that allosterically activates MOR within a MOR-DOR heteromer. (2020) (4)
2000 Alfred Burger Award Address in Medicinal Chemistry. From Models to Molecules: Opioid Receptor Dimers, Bivalent Ligands, and Selective Opioid Receptor Probes. (2001) (4)
Synthesis and physico‐chemical properties of (R, S)‐6‐ditrideuteriomethylamino‐4,4‐diphenylheptan‐3‐one hydrochloride (methadone‐d6) (1985) (4)
Boron tribromide-catalyzed rearrangement of 7,7-diphenylhydromorphone to 6,7-diphenylmorphine: A novel conversion of ketones to allylic alcohols (1996) (4)
Stereochemical requirements for receptor recognition of the μ-opioid peptide endomorphin-1: Biological activity, NMR and conformational analysis of D-amino acid substituted analogs (2002) (3)
A guinea pig ileum preparation devoid of functional κ receptors: A new in vitro pharmacologic assay for μ-opioid ligands (1997) (3)
A novel route for functionalization of the bridgehead C-2 position of benzomorphans (1981) (3)
IMPORTANCE OF CARBON 6 CHIRALITY IN CONFERRING IRREVERSIBLE OPIOID ANTAGONISM TO NALTREXONE-DERIVED AFFINITY LABELS (1984) (3)
Modulation of musculoskeletal hyperalgesia by brown adipose tissue activity in mice (2016) (3)
The delta1-opioid receptor antagonist, 7-(benzospiroindanyl)naltrexone [correction of 7-benzylspiroindanylnaltrexone], prolongs renal allograft survival in a rat model. (1998) (3)
Persistent binding of fatty acyl derivatives of naltrexamine to opioid receptors. (1991) (3)
Erratum: The σ1-opioid receptor antagonist, 7-benzylspiroindanylnaltrexone, prolongs renal allograft survival in a rat model (European Journal of Pharmacology 354 (1998) (R3-R5) PII: S0014299998004774) (1998) (3)
Bicyclic bases. Stereoselective synthesis of exo‐ and endo‐N‐benzyl‐6‐hydroxy‐2‐azabicyclo[2.2.1]heptane (1972) (3)
Comparison of peptidic and nonpeptidic delta-opioid agonists on [ 35 S ] GTP γ S binding in brain slices from Sprague-Dawley rats (2004) (3)
Linear free energy relationship among analgesic N-substituted phenylpiperidine derivatives. Method of detecting similar modes of molecular binding to common receptors. (1965) (3)
Erratum: Design of peptidomimetic δ opioid receptor antagonists using the message-address concept (Journal of Medicinal Chemistry (1990) Volume 33 (1714)) (1990) (3)
CORRELATION OF OPIATE RECEPTOR AFFINITY WITH ANALGETIC EFFECTS OF MEPERIDINE HOMOLOGS (1977) (3)
The use of mu opioid receptors in the mouse vas deferens for the study of opiate tolerance. (1989) (3)
The bivalent ligand approach in the design of highly selective opioid receptor antagonists. (1990) (3)
NARCOTIC ANTAGONISTIC POTENCY OF BIVALENT LIGANDS WHICH CONTAIN β-NALTREXAMINE. EVIDENCE FOR SIMULTANEOUS OCCUPATION OF PROXIMAL RECOGNITION SITES (1982) (3)
Interaction of [ D-Pen 2 , 0-PenS ] enkephalin and [ DAla 2 , Glu 4 ] deltorphin with-opioid receptor subtypes in vivo (2002) (3)
The bivalent ligand, MMG22, reduces neuropathic pain after nerve injury without the side effects of traditional opioids. (2020) (3)
Effect of opioid receptor ligands on the μ-S196A knock-in and μ knockout mouse vas deferens (2003) (3)
Synthesis and delta-opioid receptor antagonist activity of a naltrindole analogue with a regioisomeric indole moiety. (1994) (3)
ACTIVITIES OF MORPHINONE AND N-(CYCLOPROPYLMETHYL)NORMORPHINONE AT OPIOID RECEPTORS (1985) (2)
Crystal Structures of α- and β-Funaltrexamine: Conformational Requirement of the Fumaramate Moiety in the irreversible Blockage of μ Opioid Receptors. (1986) (2)
beta-Funaltrexamine (beta-FNA) and neural tumor response in mice. (1985) (2)
Resolution and absolute configuration of (+)‐α‐anilinopropionic acid (1964) (2)
6beta-[N,N-Bis(2-chloroethyl)amino]-17-(cyclopropylmethyl)-4,5alpha-epoxy-3,14-dihydroxymorphinan(chlornaltrexamine) a potent opioid receptor alkylating agent with ultralong narcotic antagonist actitivty. (1978) (2)
Binding characteristics of the specific μ antagonist β-FNA, the fumaramate methyl ester derivative of naltrexone (1981) (2)
Editorial - Expansion of the Perspective Series (1993) (2)
Revision of purity criteria for tested compounds. (2009) (2)
A guinea pig ileum preparation devoid of functional kappa receptors: a new in vitro pharmacologic assay for mu-opioid ligands. (1997) (2)
Reactivity of glutathione with alpha, beta-unsaturated ketone flavouring substances. (1989) (2)
3-HYDROXY-17-ARALKYLMORPHINANS AS POTENTIAL OPIATE RECEPTOR-SITE-DIRECTED ALKYLATING AGENTS (1977) (2)
Targeting the brain's immune system: a psychopharmacological approach to central nervous system infections. (2001) (2)
GRAS Flavoring Substances The 21 st publication by the Expert Panel of the Flavor and Extract Manufacturers Association on recent progress in the consideration of flavoring ingredients generally recognized as safe under the Food Additives Amendment (2003) (2)
Opioid receptors in GtoPdb v.2021.3 (2021) (2)
Investigation of the Structural Requirements for the K-Selective Opioid Receptor Antagonist, 6β,6β′-[Ethylenebis(oxyethyleneimino)]bis[17-(cyclopropylmethyl)-4,5-epoxymorphinan-3,14-diol] (TENA). (1986) (1)
Synthesis and pharmacological evaluation of an 8 beta-bis(2-chloroethyl)amino opiate as a nonequilibrium opioid receptor probe. (1984) (1)
STEREOCHEMICAL STUDIES ON MEDICINAL AGENTS PART 15, ABSOLUTE CONFIGURATIONS AND ANALGETIC POTENCIES OF ENANTIOMERIC DIASTEREOMERS OF 3‐ALLYL‐1‐METHYL‐4‐PHENYL‐4‐PROPIONOXYPIPERIDINE (1973) (1)
STRUCTURE-ACTIVITY RELATIONSHIP STUDY OF AFFINITY LABELS THAT ARE SPECIFIC FOR μ OPIOID RECEPTORS (1981) (1)
Synthesis and biological activity of analogues of beta-chlornaltrexamine and beta-funaltrexamine at opioid receptors. (1986) (1)
Synthesis and activity profiles of bivalent [Leu5]enkephalin-α-oxymorphamine hybrid opioid receptor ligands (1988) (1)
STEREOCHEMICAL STUDIES ON MEDICINAL AGENTS. 23. SYNTHESIS AND BIOLOGICAL EVALUATION OF 6-AMINO DERIVATIVES OF NALOXONE AND NALTREXONE (1977) (1)
SYNTHESIS AND EVALUATION OF 1- AND 2-SUBSTITUTED FENTANYL ANALOGS FOR OPIOID ACTIVITY (1983) (1)
Identification of Helical Packing Motifs Common to Bacteriorhodopsin and G Protein-Coupled Receptors (1996) (1)
Stereochemistry of the Cyclization of the Half-Esters of Diarylitaconic Acid (1961) (1)
Melphalan-containing N,N-dialkylenkephalin analogs as potential irreversible antagonists of the delta opioid receptor. (1986) (1)
Transfer of fatty acyl groups from membrane phosphatides to opiate ligands (1989) (1)
Editorial - Communications to the Editor: A Vehicle for the Rapid Publication of Reports of Unusual Significance and Comtemporary Interest. (1992) (1)
Role of the spinal cord in the development of opiate tolerance and dependence. (1987) (1)
STEREOSTRUCTURE-ACTIVITY RELATIONSHIP OF OPIOID AGONIST AND ANTAGONIST BIVALENT LIGANDS. EVIDENCE FOR BRIDGING BETWEEN VICINAL OPIOID RECEPTORS (1985) (1)
Delta-selective ligands related to naltrindole (2003) (1)
Could DAA modulate norepinephrine storage function (1987) (1)
Journal of Medicinal Chemistry: Editorial (1990) (1)
ALLYLPRODINE ANALOGS AS RECEPTOR PROBES. EVIDENCE THAT PHENOLIC AND NONPHENOLIC LIGANDS INTERACT WITH DIFFERENT SUBSITES ON IDENTICAL OPIOID RECEPTORS (1981) (1)
Boron Tribromide Catalyzed Rearrangement of 7,7-Diphenylhydromorphone to 6,7-Diphenylmorphine: A Novel Conversion of Ketones to Allylic Alcohols. (1996) (1)
7-Benzylidenenaltrexone (BNTX), a highly selective δ1 antagonist, the first clear evidence for δ receptor subtypes based on binding (1993) (1)
USE OF THE NOVEL OPIATE, β-FUNALTREXAMINE (β-FNA) IN THE ELUCIDATION OF RECEPTOR TYPES INVOLVED IN OPIATE-MEDIATED RESPIRATORY DEPRESSION (1981) (1)
Relationship between analgetic ED50 dose and time-course brain levels N-alkylnormeperidine homologues. (1976) (1)
Medicinal chemistry: 1989 and beyond. (1989) (1)
SYNTHESIS, X-RAY CRYSTALLOGRAPHIC DETERMINATION, AND OPIOID ACTIVITY OF ERYTHRO-5-METHYLMETHADONE ENANTIOMERS. EVIDENCE WHICH SUGGESTS THAT μ AND Δ OPIOID RECEPTORS POSSESS DIFFERENT STEREOCHEMICAL REQUIREMENTS (1982) (1)
The absolute antipodal activity of analgesics in the basic anilide series. (1962) (1)
DIFFERENT RECEPTOR SITES MEDIATE OPIOID AGONISM AND ANTAGONISM (1984) (1)
Additions and Correction. Stereo-chemical Studies on Medicinal Agents. 12. The Distinction of Enantiotopic Groups in the Interaction of 1-Methyl-4-phenyl-4-propionoxypiperidine with Analgetic Receptors. (1973) (1)
Irreversible binding of [3H]beta-funaltrexamine to brain slices of morphine-tolerant and -dependent mice. (1988) (1)
Corrigendum to: ''The FEMA GRAS assessment of a,b-unsaturated aldehydes and related substances used as flavor ingredients" [Food and Chemical Toxicology 46 (2008) 2935-2967] (DOI:10.1016/j.fct.2008.06.082) (2009) (1)
A flexible policy concerning purity criteria for published target compounds. (1999) (1)
Editorial - The Journal of Medicinal Chemistry Becomes a Biweekly Publication in 1992 (1991) (0)
Editorial - Expediting Publication of Communications to the Editor (1990) (0)
Stereochemical Studies on Medicinal Agents. 24 Correlation of the Solid‐State Conformations of 4‐Phenylpiperidine Analgetic With the Torsional Relationship Between the Phenyl Group and Piperidine Ring in Solution, a Circular Dichroism Study (2010) (0)
Synthesis of [3H]DIPPA: A potent irreversible antagonist selective for the κ opioid receptor (1995) (0)
SYNTHESIS AND PHARMACOLOGIC CHARACTERIZATION OF AN ALKYLATING ANALOG CHLORNALTREXAMINE, OF NALTREXONE WITH ULTRALONG-LASTING NARCOTIC ANTAGONIST PROPERTIES (1979) (0)
GUT-SELECTIVE OPIATES ( 75 ) Inventor : (2017) (0)
SYNTHESIS AND BIOLOGICAL EVALUATION OF PHOSPHONAMIDATE PEPTIDE INHIBITORS OF ENKEPHALINASE AND ANGIOTENSIN-CONVERTING ENZYME (1985) (0)
Isolation of kappa opioid receptor with an aminoethyl-nor-binaltorphimine (AE-norBNI) affinity column. (1990) (0)
a-Cyanation of Tertiary Amines (1981) (0)
STEREOCHEMICAL STUDIES ON MEDICINAL AGENTS PART 16, CONFORMATIONAL STUDIES OF METHADONE AND ISOMETHADONE UTILIZING CIRCULAR AND PROTON MAGNETIC RESONANCE (1974) (0)
Panel Discussion: New Problems that Should be Addressed in the Next Ten Years (1999) (0)
New format for references (1991) (0)
RESOLUTION AND ABSOLUTE CONFIGURATION OF (+)-ALPHA-ANILINOPROPIONIC ACID. (1964) (0)
A CIRCULAR DICHROISM STUDY OF THE INTERACTION OF SODIUM AND POTASSIUM IONS WITH METHIONINE ENKEPHALIN (1977) (0)
Specificity of in vivo opiate antagonism by chlornaltrexamine (1980) (0)
STEREOCHEMICAL STUDIES ON MEDICINAL AGENTS. 20. ABSOLUTE CONFIGURATION AND ANALGETIC POTENCY OF α-PROMEDOL ENANTIOMERS. THE ROLE OF THE C-4 CHIRAL CENTER IN CONFERRING STEREOSELECTIVITY IN AXIAL- AND EQUATORIAL-PHENYLPRODINE CONGENERS (1977) (0)
SYNTHESIS AND BIOLOGICAL EVALUATION OF 2,3-DIAZABICYCLO(2.2.1)HEPTANE DERIVATIVES AS PROSTAGLANDIN ENDOPEROXIDE ANALOGS (1981) (0)
STEREOCHEMICAL STUDIES ON MEDICINAL AGENTS. 21. INVESTIGATION OF THE ROLE OF CONFORMATIONAL FACTORS IN THE ACTION OF DIPHENYLPROPYLAMINES. SYNTHESIS AND ANALGETIC POTENCY OF 5-METHYLMETHADONE DIASTEREOMERS (1977) (0)
BICYCLISCHE BASEN, STEREOSELEKTIVE SYNTH. VON EXO- UND ENDO-N-BENZYL-6-HYDROXY-2-AZA-BICYCLO(2,2,1)HEPTAN (1972) (0)
Synthesis and Biological Activity of Analogues of β-Chlornaltrexamine and β-Funaltrexamine at Opioid Receptors. (1987) (0)
STEREOCHEMICAL STUDIES ON MEDICINAL AGENTS PART 17, SYNTHESIS, ABSOLUTE CONFIGURATION, AND ANALGETIC POTENCY OF ENANTIOMERIC DIASTEREOMERS OF 3-ETHYL AND 3-PROPYL DERIVATIVES OF 1-METHYL-4-PHENYL-4-PROPIONOXYPIPERIDINE (1974) (0)
7-Arylidenenaltrexones as selective delta1 opioid receptor antagonists. (1998) (0)
Affinity Labels as Tools for the Identification of Opioid Receptor Recognition Sites (2001) (0)
909 – CHLORNALTREXAMINE, A NEW, POTENT, ULTRA-LONG ACTING NARCOTIC ANTAGONIST (1978) (0)
Interview with Philip Portoghese (2012) (0)
Opioid Agonist and Antagonist Activities of Monofunctional Nitrogen Mustard Analogues (I) of β-Chlornaltrexamine. (1987) (0)
Accelerated Electronic Publication (1997) (0)
Influence of Pseudoallylic Strain on the Conformational Preference of 4-Methyl- 4-phenylpipecolic Acid Derivatives. (1986) (0)
An ultra-long lasting narcotic antagonist, chlornaltrexamine: Effects in vitro and in vivo (1978) (0)
Ultralong lasting single-dose tolerance to chloroxymorphamine (COA), an opioid receptor alkylating agonist (1979) (0)
The 20th publication by the Expert Panel of the Flavor and Extract Manufacturers Association on recent progress in the consideration of flavoring ingredients generally recognized as safe under the Food Additives Amendment (2001) (0)
The Role of Conformation and Configuration in the Interaction of 4-Phenylpiperidines with Analgetic Receptors (1974) (0)
SYNTHESES OF DELTA OPIOID ANTAGONISTS AND THEIR STRUCTURE ACTIVITY RELATIONSHIPS (1990) (0)
β-FNA-insensitive, opioid peptide preferring receptors in the guinea pig ileum (GPI) (1985) (0)
Irreversible Blockage of Opioid Receptor Types by Ester Homologues of β-Funaltrexamine. (1987) (0)
The role of conformation and configuration in the interaction of 4 phenylpiperidine derivatives with analgetic receptor (1974) (0)
Internalization of Two Distinct Receptors in Response to Occupation with a Bivalent Ligand Incorporating a Single Stimulus for Internalization (2010) (0)
Additional file 1: of A bivalent compound targeting CCR5 and the mu opioid receptor treats inflammatory arthritis pain in mice without inducing pharmacologic tolerance (2018) (0)
Opioid Efficacy in a C 6 Glioma Cell Line Stably Expressing the Delta Opioid Receptor 1 (1997) (0)
A Novel Pyrrole Synthesis via Reaction of Ketones with N-Aminoimides. (1987) (0)
The Absolute Configuration of (-)-N-[2-(Methylbenzylamino)-propyl]-propionanilide (1962) (0)
Synthesis and evaluation of melphalan-containing N,N-dialkylenkephalin analogues as irreversible antagonists of the delta opioid receptor. (1987) (0)
A CONVENIENT SYNTHESIS OF 1-METHYL-4-OXOPIPECOLIC ACID METHYL ESTER (1983) (0)
Comparison of Peptidic and Nonpeptidic (cid:1) -Opioid Agonists on Guanosine 5 (cid:1) - O -(3-[ 35 S]thio)triphosphate ([ 35 S]GTP (cid:2) S) Binding in Brain Slices from Sprague-Dawley Rats (2005) (0)
Prostaglandins: the once-a-month birth control pill of the future. (1972) (0)
SYNTHESIS AND BIOLOGICAL EVALUATION OF A METAZOCINE-CONTAINING ENKEPHALINAMIDE. EVIDENCE FOR NONIDENTICAL ROLES OF THE TYRAMINE MOIETY IN OPIATES AND OPIOI PEPTIDES (1983) (0)
Selectivity at the μ opiate receptor: the structures of α and β-funaltrexamine (1984) (0)
Morphine Tolerance In Mice Changes Response of Heroin From μ To δ Opioid Receptors (44520) (2000) (0)
Editorial - Subsidizing Color Graphics (1992) (0)
Chemical tools in opioid research. (1992) (0)
Activity of N-Methyl-α- and -β-funaltrexamine at Opioid Receptors. (1987) (0)
Stereoselectivity of the Reduction of Naltrexone Oxime with Borane. (1986) (0)
POTENTIAL NONEQUILIBRIUM ANALGETIC RECEPTOR INACTIVATORS, FURTHER PHARMACOLOGIC STUDIES OF N-ACYLANILERIDINES (1975) (0)
Efficient Preparation of Polyfunctional α-Diketones from Carboxylic Acids. (1986) (0)
Medicinal chemistry as we start the next millennium (1997) (0)
SYNTHESIS AND ADRENORECEPTOR BLOCKING ACTION OF AZIRIDINIUM IONS DERIVED FROM PHENOXYBENZAMINE AND DIBENAMINE (1976) (0)
Selectivity of opioid agonists and antagonists for the various opioid receptor types. (1985) (0)
STEREOCHEMICAL STUDIES ON MEDICINAL AGENTS PART 18, ABSOLUTE CONFIGURATION AND ANALGETIC POTENCY OF TRIMEPERIDINE ENANTIOMERS (1975) (0)
SYNTHESIS AND BIOLOGICAL EVALUATION OF 9,11-AZO-13-OXA-15-HYDROXYPROSTANOIC ACID, A POTENT INHIBITOR OF PLATELET AGGREGATION (1980) (0)
MMG22 Potently Blocks Hyperalgesia in Cisplatin-treated Mice (2023) (0)
Effect of opioid receptor ligands on the mu-S196A knock-in and mu knockout mouse vas deferens. (2003) (0)
Editorial - Reinstatement of Notes as a Manuscript Class (1992) (0)
Editorial - Expedited Articles: A New Category for the Rapid Dissemination of Cutting-Edge Research (1993) (0)
Franklin Robinson memorial symposium on medicinal chemistry in drug abuse research (1995) (0)
A vehicle for the rapid publication of reports of unusual significance and contemporary interest (1992) (0)
2‐AZATRICYCLO(2,2,1,0(1,6))HEPTANE, SYNTHESIS AND CONVERSION TO AZABICYCLO(2,2,1)HEPTANES (1973) (0)
Targeting Putative Mu Opioid/Chemokine Receptor Type 5 Heteromers Potently Attenuates Nociception in a Murine Model of Sickle Cell Disease (2015) (0)

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