From Models to Molecules: Opioid Receptor Dimers, Bivalent Ligands, and Selective Opioid Receptor Probes

The effects of morphine- and nalorphine- like drugs in the nondependent and morphine-dependent chronic spinal dog.

1976 • 2,883 citations

Endogenous opioid peptides: multiple agonists and receptors

1977 • 2,494 citations

A potent and selective endogenous agonist for the µ-opiate receptor

1997 • 1,306 citations

Requirement of Rigid-Body Motion of Transmembrane Helices for Light Activation of Rhodopsin

1996 • 1,159 citations

G-protein-coupled receptor heterodimerization modulates receptor function

1999 • 1,146 citations

Pharmacologic Analysis of Drug Receptor Interaction

1988 • 936 citations

Bis-penicillamine enkephalins possess highly improved specificity toward delta opioid receptors.

1983 • 737 citations

International Union of Pharmacology. XII. Classification of opioid receptors.

1996 • 704 citations

Analogues of β-LPH61–64 posessing selective agonist activity at μ-opiate receptors

1981 • 503 citations

Deltorphins: a family of naturally occurring peptides with high affinity and selectivity for delta opioid binding sites.

1989 • 453 citations

ACTH: A SHORT INTRODUCTORY REVIEW*

1977 • 389 citations

Agonists induce conformational changes in transmembrane domains III and VI of the beta 2 adrenoceptor

1997 • 378 citations

Synthetic Analgesics: Stereochemical Considerations

1954 • 331 citations

Differential antagonism of delta opioid agonists by naltrindole and its benzofuran analog (NTB) in mice: evidence for delta opioid receptor subtypes.

1991 • 330 citations

Design of peptidomimetic .delta. opioid receptor antagonists using the message-address concept

1990 • 251 citations

A New Concept on the Mode of Interaction of Narcotic Analgesics with Receptors

1965 • 207 citations

Mutation of a Highly Conserved Aspartic Acid in the β₂Adrenergic Receptor: Constitutive Activation, Structural Instability, and Conformational Rearrangement of Transmembrane Segment 6

1999 • 203 citations

Constitutive Activation of the β2 Adrenergic Receptor Alters the Orientation of Its Sixth Membrane-spanning Segment

1997 • 186 citations

A highly selective δ1-opioid receptor antagonist: 7-benzylidenenaltrexone

1992 • 182 citations

Selective Natrexone-Derived Opioid Receptor Antagonists

1992 • 173 citations

Opioids and Their Complicated Receptor Complexes

2000 • 165 citations

Expression cloning of an insect diuretic hormone receptor. A member of the calcitonin/secretin receptor family.

1994 • 146 citations

Binaltorphimine-related bivalent ligands and their .kappa. opioid receptor antagonist selectivity

1988 • 137 citations

Domain swapping in G-protein coupled receptor dimers

1998 • 127 citations

Oligomerisation of G-protein-coupled receptors

2001 • 124 citations

Narcotic antagonistic potency of bivalent ligands which contain .beta.-naltrexamine. Evidence for simultaneous occupation of proximal recognition sites

1982 • 121 citations

Dimeric tetrapeptide enkephalins display extraordinary selectivity for the δ opiate receptor

1982 • 112 citations

Differential binding domains of peptide and non-peptide ligands in the cloned rat kappa opioid receptor.

1994 • 105 citations

Human kappa opiate receptor second extracellular loop elevates dynorphin's affinity for human mu/kappa chimeras

1994 • 99 citations

Role of spacer and address components in peptidomimetic .delta.-opioid receptor antagonists related to naltrindole

1991 • 97 citations

Opiate (Enkephalin) Receptors of Neuroblastoma Cells: Occurrence in Clusters on the Cell Surface

1979 • 96 citations

Potent and Selective Indolomorphinan Antagonists of the Kappa-Opioid Receptor

2000 • 95 citations

Opioid agonist and antagonist bivalent ligands. The relationship between spacer length and selectivity at multiple opioid receptors

1986 • 88 citations

Pharmacologic analysis of drug-receptor interaction (2nd edition): Edited by T Kenakin. (Pp 468; $113.50.) New York: Reven Press, 1993. ISBN 0-7817-0065-5

1995 • 80 citations

Determination of the Amino Acid Residue Involved in [3H]β-Funaltrexamine Covalent Binding in the Cloned Rat µ Opioid Receptor

1996 • 80 citations

Molecular Simulation of Dynorphin A-(1−10) Binding to Extracellular Loop 2 of the κ-Opioid Receptor. A Model for Receptor Activation

1997 • 78 citations

Investigation of the Selectivity of Oxymorphone- and Naltrexone-Derived Ligands via Site-Directed Mutagenesis of Opioid Receptors: Exploring the ‘Address' Recognition Locus

2001 • 78 citations

Application of the message-address concept to the docking of naltrexone and selective naltrexone-derived opioid antagonists into opioid receptor models

1996 • 76 citations

Opioid agonist and antagonist bivalent ligands as receptor probes

1982 • 76 citations

Mutational Evidence for a Common κ Antagonist Binding Pocket in the Wild-Type κ and Mutant μ[K303E] Opioid Receptors

1998 • 75 citations

Analysis of selective binding epitopes for the kappa-opioid receptor antagonist nor-binaltorphimine.

1995 • 74 citations

Structural requirements for specific recognition of mu or delta opiate receptors.

1981 • 73 citations

The Search for a Better Analgesic

1973 • 73 citations

A selective .delta.1 opioid receptor agonist derived from oxymorphone. Evidence for separate recognition sites for .delta.1 opioid receptor agonists and antagonists

1993 • 72 citations

Dimeric enkephalins display enhanced affinity and selectivity for the delta opiate receptor.

1982 • 62 citations

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 • 61 citations

Peptides as receptor selectivity modulators of opiate pharmacophores

1986 • 58 citations

Discovery of a Novel Class of Substituted Pyrrolooctahydroisoquinolines as Potent and Selective δ Opioid Agonists, Based on an Extension of the Message−Address Concept

1997 • 56 citations

Stereostructure-activity relationship of opioid agonist and antagonist bivalent ligands. Evidence for bridging between vicinal opioid receptors

1985 • 56 citations

7-Aminoquinolines. A novel class of agents active against herpes viruses

1988 • 52 citations

Role of the spacer in conferring .kappa. opioid receptor selectivity to bivalent ligands related to norbinaltorphimine

1991 • 51 citations

Stereochemical studies on medicinal agents. 31. Only one pharmacophore is required for the .kappa. opioid antagonist selectivity of norbinaltorphimine

1988 • 47 citations

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 • 44 citations

Different receptor sites mediate opioid agonism and antagonism

1983 • 43 citations

Synthesis of naltrexone-derived .delta.-opioid antagonists. Role of conformation of the .delta. address moiety

1994 • 41 citations

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 • 35 citations

Synthesis and opioid antagonist potencies of naltrexamine bivalent ligands with conformationally restricted spacers

1986 • 32 citations

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 • 32 citations

Comments on the optical and radio detection of black hole explosions

1977 • 30 citations

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 • 30 citations

Pharmacology identification of two related pentapeptides from the brain with potent opiate agonist activity

1976 • 29 citations

Synthesis and .kappa.-opioid antagonist selectivity of a norbinaltorphimine congener. Identification of the address moiety required for .kappa.-antagonist activity

1993 • 28 citations

Isosteric Replacement of Acidic with Neutral Residues in Extracellular Loop-2 of the κ-Opioid Receptor Does Not Affect Dynorphin A(1−13) Affinity and Function

2000 • 24 citations

Stereochemical Factors Related to the Potency of Anticholinergic Psychotomimetic Drugs

1965 • 23 citations

Pyrrolomorphinans as δ Opioid Receptor Antagonists. The Role of Steric Hindrance in Conferring Selectivity

1997 • 21 citations

3-Phenoxypyridine 1-oxides as anticonvulsant agents

1988 • 20 citations

7-Spiroindanyl Derivatives of Naltrexone and Oxymorphone as Selective Ligands for δ Opioid Receptors

1997 • 19 citations

Opioid Antagonist Activity of Naltrexone-Derived Bivalent Ligands: Importance of a Properly Oriented Molecular Scaffold To Guide “Address” Recognition at κ Opioid Receptors

1996 • 15 citations

Synthesis and biological activity of analogs of .beta.-chlornaltrexamine and .beta.-funaltrexamine at opioid receptors

1986 • 11 citations