The delta-opioid receptor: molecular pharmacology, signal transduction, and the determination of drug efficacy.

Relationship between the inhibition constant (KI) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction

1973 • 12,522 citations

G PROTEINS: TRANSDUCERS OF RECEPTOR-GENERATED SIGNALS

1987 • 6,374 citations

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

1975 • 3,780 citations

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

Opiate Receptor: Demonstration in Nervous Tissue

1973 • 2,364 citations

Isolation and structure of the endogenous agonist of opioid receptor-like ORL1 receptor

1995 • 1,887 citations

Orphanin FQ: A Neuropeptide That Activates an Opioidlike G Protein-Coupled Receptor

1995 • 1,800 citations

Regulation of noradrenaline release by presynaptic receptor systems

1977 • 1,482 citations

Molecular and Cellular Basis of Addiction

1997 • 1,324 citations

Opioid-receptor mRNA expression in the rat CNS: anatomical and functional implications

1995 • 1,267 citations

Cloning of a Delta Opioid Receptor by Functional Expression

1992 • 1,225 citations

A mutation-induced activated state of the beta 2-adrenergic receptor. Extending the ternary complex model.

1993 • 1,213 citations

Anatomy of CNS opioid receptors

1988 • 1,178 citations

The Many Faces of G Protein Signaling

1998 • 1,137 citations

A MODIFICATION OF RECEPTOR THEORY

1956 • 1,126 citations

Receptor-effector coupling by G proteins

1990 • 1,117 citations

Operational models of pharmacological agonism

1983 • 1,062 citations

ORL1, a novel member of the opioid receptor family

1994 • 1,060 citations

Stereospecific Binding of the Potent Narcotic Analgesic [ ³ H]Etorphine to Rat-Brain Homogenate

1973 • 1,055 citations

The GTP-binding protein, Go9 regulates neuronal calcium channels

1987 • 910 citations

Psychotomimesis Mediated by κ Opiate Receptors

1986 • 822 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

Stereospecific Interaction Between Narcotic Analgesics and a Synaptic Plasma Membrane Fraction of Rat Cerebral Cortex

1973 • 650 citations

Pharmacological characterization of the cloned kappa-, delta-, and mu-opioid receptors.

1994 • 630 citations

Principles of Drug Action: The Basis of Pharmacology.

1975 • 616 citations

Mu and delta receptors belong to a family of receptors that are coupled to potassium channels.

1987 • 616 citations

Cloning and functional comparison of kappa and delta opioid receptors from mouse brain.

1993 • 614 citations

Molecular cloning and tissue distribution of a putative member of the rat opioid receptor gene family that is not a μ, δ or κ opioid receptor type

1994 • 593 citations

On the reaction of cells and of nerve‐endings to certain poisons, chiefly as regards the reaction of striated muscle to nicotine and to curari

1905 • 581 citations

Pharmacological Mechanisms of Opioid Analgesics

1993 • 559 citations

Opiate Receptor Binding of Agonists and Antagonists Affected Differentially by Sodium

1974 • 554 citations

Morphine receptors as regulators of adenylate cyclase activity.

1975 • 529 citations

COMPARISON OF DISSOCIATION CONSTANTS AND OF RELATIVE EFFICACIES OF SELECTED AGONISTS ACTING ON PARASYMPATHETIC RECEPTORS*

1967 • 517 citations

Opiate receptor knockout mice define μ receptor roles in endogenous nociceptive responses and morphine-induced analgesia

1997 • 511 citations

Specific uncoupling by islet-activating protein, pertussis toxin, of negative signal transduction via alpha-adrenergic, cholinergic, and opiate receptors in neuroblastoma x glioma hybrid cells.

1983 • 493 citations

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

1976 • 467 citations

Opioid receptor-coupled second messenger systems

1991 • 466 citations

Cloning and pharmacological characterization of a rat μ opioid receptor

1993 • 460 citations

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

1989 • 453 citations

In vitro autoradiography of receptor-activated G proteins in rat brain by agonist-stimulated guanylyl 5'-[gamma-[35S]thio]-triphosphate binding.

1995 • 450 citations

Modulation by mu-opioid agonists of guanosine-5'-O-(3-[35S]thio)triphosphate binding to membranes from human neuroblastoma SH-SY5Y cells.

1995 • 441 citations

Cloning and pharmacological characterization of a rat kappa opioid receptor.

1993 • 422 citations

Roles of mu, delta and kappa opioid receptors in spinal and supraspinal mediation of gastrointestinal transit effects and hot-plate analgesia in the mouse.

1984 • 417 citations

mu opiate receptor: cDNA cloning and expression.

1993 • 405 citations

cDNA cloning and regional distribution of a novel member of the opioid receptor family

1994 • 404 citations

Nociceptin/orphanin FQ and the opioid receptor-like ORL1 receptor

1997 • 387 citations

Recent advances in molecular recognition and signal transduction of active peptides: Receptors for opioid peptides

1995 • 386 citations

cDNA Cloning of an orphan opiate receptor gene family member and its splice variant

1994 • 379 citations

Morphine-like drugs inhibit the stimulation by E prostaglandins of cyclic AMP formation by rat brain homogenate

1974 • 373 citations

The family of G‐protein‐coupled receptors

1995 • 369 citations

ICI 174864: A highly selective antagonist for the opioid Δ-receptor

1984 • 361 citations

Molecular biology of opioid receptors

1993 • 358 citations

Molecular biology of the opioid receptors: structures, functions and distributions

1995 • 345 citations

Molecular cloning, tissue distribution and chromosomal localization of a novel member of the opioid receptor gene family

1994 • 333 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

The Rate of Action of Drugs on Cells

1937 • 319 citations

Application of the message-address concept in the design of highly potent and selective non-peptide .delta. opioid receptor antagonists

1988 • 298 citations

CREB (cAMP Response Element-Binding Protein) in the Locus Coeruleus: Biochemical, Physiological, and Behavioral Evidence for a Role in Opiate Dependence

1997 • 298 citations

Pharmacological characterization in vivo of the novel opiate, beta-funaltrexamine.

1982 • 296 citations

Human μ opiate receptor

1994 • 286 citations

Primary structures and expression from cDNAs of rat opioid receptor δ‐and μ‐subtypes

1993 • 277 citations

The classification of seven transmembrane receptors in recombinant expression systems.

1996 • 271 citations

Molecular Characterization of Opioid Receptors

1990 • 266 citations

An aspartate conserved among G-protein receptors confers allosteric regulation of alpha 2-adrenergic receptors by sodium.

1990 • 266 citations

Opiate-dependent modulation of adenylate cyclase.

1977 • 265 citations

Differential antagonism of opioid delta antinociception by [D-Ala2,Leu5,Cys6]enkephalin and naltrindole 5'-isothiocyanate: evidence for delta receptor subtypes.

1991 • 265 citations

Molecular pharmacology of the opioid receptors

1995 • 255 citations

Molecular cloning of a rat κ opioid receptor reveals sequence similarities to the μ and δ opioid receptors

1993 • 254 citations

Isolation of a novel cDNA encoding a putative membrane receptor with high homology to the cloned μ, δ, and κ opioid receptors

1994 • 254 citations

δ-opioid-receptor-mediated inhibition of adenylate cyclase is transduced specifically by the guanine-nucleotide-binding protein Gi2

1990 • 252 citations

IMPORTANT CONCEPTS OF RECEPTOR THEORY

1982 • 251 citations

G proteins and regulation of adenylyl cyclase

1995 • 250 citations

Opiate Analgesia: Evidence for Mediation by a Subpopulation of Opiate Receptors

1980 • 249 citations

Molecular Cloning of a Novel G Protein‐Coupled Receptor Related to the Opiate Receptor Family

1995 • 249 citations

Principles of Drug Action

1990 • 243 citations

Structure/function relationship of proteins belonging to the family of receptors coupled to GTP‐binding proteins

1991 • 241 citations

Receptor Occupancy and Tissue Response

1956 • 238 citations

Cloning and expression of a cDNA for the rat k‐opioid receptor

1993 • 234 citations

Differential stereochemical requirements of mu vs. delta opioid receptors for ligand binding and signal transduction: development of a class of potent and highly delta-selective peptide antagonists.

1992 • 233 citations

Bivalent ligands and the message-address concept in the design of selective opioid receptor antagonists

1989 • 232 citations

Lack of antinociceptive cross-tolerance between [D-Pen2, D-Pen5]enkephalin and [D-Ala2]deltorphin II in mice: evidence for delta receptor subtypes.

1991 • 231 citations

Molecular biology and pharmacology of cloned opioid receptors ¹

1995 • 231 citations

The reaction between acetyl choline and muscle cells

1926 • 230 citations

The irreversible narcotic antagonistic and reversible agonistic properties of the fumaramate methyl ester derivative of naltrexone

1981 • 229 citations

kappa-Opioid receptor in humans: cDNA and genomic cloning, chromosomal assignment, functional expression, pharmacology, and expression pattern in the central nervous system.

1995 • 228 citations

Deltorphin, a novel amphibian skin peptide with high selectivity and affinity for δ opioid receptors

1989 • 227 citations

Binding affinity and selectivity of opioids at mu, delta and kappa receptors in monkey brain membranes.

1994 • 226 citations

Novel opiate binding sites selective for benzomorphan drugs.

1981 • 225 citations

Quantitative autoradiographic mapping of μ-, δ- and κ-opioid receptors in knockout mice lacking the μ-opioid receptor gene

1997 • 224 citations

Agonist-dependent phosphorylation of the mouse delta-opioid receptor: involvement of G protein-coupled receptor kinases but not protein kinase C.

1995 • 222 citations

Affinity and intrinsic activity in the theory of competitive inhibition. I. Problems and theory.

1954 • 216 citations

Discrete mapping of brain mu and delta opioid receptors using selective peptides: Quantitative autoradiography, species differences and comparison with kappa receptors

1989 • 207 citations

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

1965 • 207 citations

Probes for Narcotic Receptor Mediated Phenomena. 19. Synthesis of (+)-4-[(.alpha.R)-.alpha.-((2S,5R)-4-Allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl]-N,N-diethylbenzamide (SNC 80): A Highly Selective, Nonpeptide .delta. Opioid Receptor Agonist

1994 • 203 citations

Coupling of opiate receptors to adenylate cyclase: requirement for Na+ and GTP.

1979 • 200 citations

Molecular cloning and expression of a rat κ opioid receptor

1993 • 198 citations

Chronic Opioid Treatment Induces Adenylyl Cyclase V Superactivation

1996 • 198 citations

Specificity of opioids towards the μ-, δ- and ϵ-opiate receptors

1979 • 194 citations

Activity of the δ-Opioid Receptor Is Partially Reduced, Whereas Activity of the κ-Receptor Is Maintained in Mice Lacking the μ-Receptor

1998 • 193 citations

Selective loss of δ opioid analgesia and binding by antisense oligodeoxynucleotides to a δ opioid receptor

1994 • 192 citations

Mutagenesis of the beta2-Adrenergic Receptor: How Structure Elucidates Function

1992 • 192 citations

Functional Coupling of the δ‐, μ‐, and κ‐Opioid Receptors to Mitogen‐Activated Protein Kinase and Arachidonate Release in Chinese Hamster Ovary Cells

1996 • 189 citations

ADP-ribosylation of adenylate cyclase by pertussis toxin. Effects on inhibitory agonist binding.

1984 • 189 citations

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

1992 • 182 citations

SNC 80, a selective, nonpeptidic and systemically active opioid delta agonist.

1995 • 181 citations

Selective Natrexone-Derived Opioid Receptor Antagonists

1992 • 173 citations

Mapping of opioid receptors using antisense oligodeoxynucleotides: correlating their molecular biology and pharmacology

1995 • 170 citations

Role of mu and delta receptors in the supraspinal and spinal analgesic effects of [D-Pen2, D-Pen5] enkephalin in the mouse

1988 • 169 citations

Direct dependence studies in rats with agents selective for different types of opioid receptor.

1988 • 166 citations

Genomic structure analysis of promoter sequence of a mouse mu opioid receptor gene.

1994 • 166 citations

The relationship between muscarinic receptor occupancy and adenylate cyclase inhibition in the rabbit myocardium.

1985 • 161 citations

Structural and functional relationships of heterotrimeric G‐proteins

1995 • 160 citations

G Proteins and Opioid Receptor-Mediated Signalling

1997 • 159 citations

Opioid Receptor Types and Subtypes: The delta Receptor as a Model

1996 • 156 citations

Measurement of guanine nucleotide-binding protein activation by A1 adenosine receptor agonists in bovine brain membranes: stimulation of guanosine-5'-O-(3-[35S]thio)triphosphate binding.

1993 • 154 citations

Role of Aromatic Transmembrane Residues of the δ-Opioid Receptor in Ligand Recognition

1996 • 154 citations

Determinants of alpha 2-adrenergic receptor activation of G proteins: evidence for a precoupled receptor/G protein state.

1994 • 149 citations

A novel, potent and selective nonpeptidic delta opioid receptor agonist BW373U86.

1993 • 149 citations

Demonstration and Characterization of Opiate Inhibition of the Striatal Adenylate Cyclase

1981 • 149 citations

A single residue, aspartic acid 95, in the delta opioid receptor specifies selective high affinity agonist binding.

1993 • 146 citations

Cardiac muscarinic cholinergic receptor binding is regulated by Na+ and guanyl nucleotides.

1980 • 140 citations

Opioid δ-receptor involvement in supraspinal and spinal antinociception in mice

1987 • 139 citations

Pharmacology and regulation of the neuronal dopamine transporter

1997 • 139 citations

Autoradiographic analysis of mu1, mu2, and delta opioid binding in the central nervous system of C57BL/6BY and CXBK (opioid receptor-deficient) mice

1985 • 137 citations

Cerebral delta opioid receptors mediate analgesia but not the intestinal motility effects of intracerebroventricularly administered opioids.

1984 • 136 citations

The antagonism of acetyl choline by atropine

1926 • 133 citations

Pharmacological characterization of the epsilon-opiate receptor.

1981 • 133 citations

Antinociceptive profile of biphalin, a dimeric enkephalin analog.

1993 • 133 citations

The human delta-opioid receptor: genomic organization, cDNA cloning, functional expression, and distribution in human brain.

1994 • 131 citations

Inhibition of the ω-conotoxin-sensitive calcium current by distinct G proteins

1992 • 128 citations

cAMP‐dependent reversal of opioid‐ and prostaglandin‐mediated depression of the isolated respiratory network in newborn rats

1997 • 127 citations

The μ-opioid receptor is necessary for [d-Pen2,d-Pen5]enkephalin-induced analgesia

1997 • 126 citations

Identification of a human delta opioid receptor: Cloning and expression

1994 • 125 citations

Naloxone sensitive orphanin FQ-induced analgesia in mice

1996 • 125 citations

Opioid mu, delta, and kappa receptor-induced activation of phospholipase C-beta 3 and inhibition of adenylyl cyclase is mediated by Gi2 and G(o) in smooth muscle.

1996 • 124 citations

The Cloning and Chromosomal Mapping of Two Novel Human Opioid-Somatostatin-like Receptor Genes, GPR7 and GPR8, Expressed in Discrete Areas of the Brain

1995 • 124 citations

Opioid Modulation of Extracellular Signal‐Regulated Protein Kinase Activity Is Ras‐Dependent and Involves G_βγ Subunits

1998 • 121 citations

Pharmacology characterization of guanine nucleotide exchange reactions in membranes from Cho cells stably transfected with human muscarinic receptors m1–m4

1993 • 121 citations

Double-enkephalins—Synthesis, activity on guinea-pig ileum, and analgesic effect

1982 • 121 citations

Binding selectivity profiles for ligands of multiple receptor types: Focus on opioid receptors

1987 • 120 citations

An antisense oligodeoxynucleotide to the delta opioid receptor (DOR-1) inhibits morphine tolerance and acute dependence in mice

1996 • 119 citations

Cyclic adenosine monophosphate antagonism of morphine analgesia.

1973 • 119 citations

Opioids mobilize calcium from inositol 1,4,5-trisphosphate-sensitive stores in NG108-15 cells

1994 • 117 citations

Structure and Chromosomal Mapping of Genes for the Mouse κ-Opioid Receptor and an Opioid Receptor Homologue (MOR-C)

1994 • 116 citations

Regulation of Multiple Effectors by the Cloned δ‐Opioid Receptor: Stimulation of Phospholipase C and Type II Adenylyl Cyclase

1995 • 116 citations

Differential blockade of opioid analgesia by antisense oligodeoxynucleotides directed against various G protein alpha subunits.

1996 • 115 citations

Blockade of morphine analgesia by an antisense oligodeoxynucleotide against the mu receptor

1994 • 110 citations

Metkephamid, a Systemically Active Analog of Methionine Enkephalin with Potent Opioid δ-Receptor Activity

1981 • 110 citations

Pharmacological characterization of orphanin FQ/nociceptin and its fragments.

1997 • 110 citations

Dual excitatory and inhibitory effects of opioids on intracellular calcium in neuroblastoma x glioma hybrid NG108-15 cells.

1992 • 108 citations

Isolation of a Human κ Opioid Receptor cDNA from Placenta

1994 • 108 citations

Functional role and sequence analysis of a lymphocyte orphan opioid receptor

1995 • 107 citations

Cannabinoid receptor stimulation of guanosine-5′-O-(3-[35S]thio)triphosphate binding in rat brain membranes

1996 • 107 citations

Thr353, Located within the COOH-terminal Tail of the ´ Opiate Receptor, Is Involved in Receptor Down-regulation

1996 • 105 citations

cDNA cloning and pharmacological characterization of an opioid receptor with high affinities for κ‐subtype‐selective ligands

1993 • 102 citations

The conserved aspartate residue in the third putative transmembrane domain of the delta-opioid receptor is not the anionic counterpart for cationic opiate binding but is a constituent of the receptor binding site.

1996 • 102 citations

In vivo injection of antisense oligodeoxynucleotides to G alpha subunits and supraspinal analgesia evoked by mu and delta opioid agonists.

1995 • 101 citations

Cloning of a human κ opioid receptor from the brain

1995 • 100 citations

Involvement of Trp-284, Val-296, and Val-297 of the Human δ-Opioid Receptor in Binding of δ-Selective Ligands

1996 • 100 citations

Differential blockade of morphine and morphine-6β-glucuronide analgesia by antisense oligodeoxynucleotides directed against MOR-1 and G-protein α subunits in rats

1995 • 98 citations

A Chimeric Study of the Molecular Basis of Affinity and Selectivity of the κ and the δ Opioid Receptors.

1995 • 98 citations

Opiate binding to membrane preparations of neuroblastoma X glioma hybrid cells NG108-15: Effects of ions and nucleotides

1978 • 97 citations

Molecular cloning and in situ hybridization histochemistry for rat μ-opioid receptor

1994 • 95 citations

G-protein antisense oligodeoxyribonucleotides and μ-opioid supraspinal antinociception

1994 • 91 citations

Agonists and antagonists bind to different domains of the cloned kappa opioid receptor.

1994 • 87 citations

Studies on mu and delta opioid receptor selectivity utilizing chimeric and site-mutagenized receptors.

1995 • 85 citations

UNEXPECTED ANTAGONISM IN THE RAT VAS DEFERENS BY BENZOMORPHANS WHICH ARE AGONISTS IN OTHER PHARMACOLOGICAL TESTS

1981 • 80 citations

Agonist activation of p42 and p44 mitogen-activated protein kinases following expression of the mouse δ opioid receptor in Rat-1 fibroblasts: effects of receptor expression levels and comparisons with G-protein activation

1996 • 80 citations

Evidence for two subtypes of δ opioid receptors in rat brain

1991 • 79 citations

Characterization and Distribution of a Cloned Rat μ‐Opioid Receptor

1995 • 76 citations

Characterization of the cloned human mu opioid receptor.

1995 • 76 citations

DAMGO, a μ‐opioid receptor selective agonist, distinguishes between μ‐ and δ‐opioid receptors around their first extracellular loops

1995 • 76 citations

On the role of extracellular loops of opioid receptors in conferring ligand selectivity

1995 • 76 citations

Interactions of ligands with morphine and enkephalin receptors are differentially affected by guanine nucleotide.

1981 • 74 citations

Treatment with antisense oligodeoxynucleotide to the opioid δ receptor selectively inhibits δ2-agonist antinociception

1994 • 72 citations

Blockade of U50,488H analgesia by antisense oligodeoxynucleotides to a κ-opioid receptor

1994 • 71 citations

Properties and localization of beta-endorphin receptor in rat brain.

1979 • 71 citations

Cyclic penicillamine containing enkephalin analogs display profound delta receptor selectivities

1983 • 70 citations

Primary structure and functional expression of a guinea pig kappa opioid (dynorphin) receptor.

1994 • 68 citations

Can supraspinal δ-opioid receptors mediate antinociception?

1988 • 66 citations

Antisense strategies in neurobiology

1997 • 66 citations

Antinociceptive effects of the selective non-peptidic δ-opioid receptor agonist TAN-67 in diabetic mice

1995 • 65 citations

Plasticity: Implications for opioid and other pharmacological interventions in specific pain states

1997 • 64 citations

δ‐Opioids Stimulate Inositol 1,4,5‐Trisphosphate Formation, and so Mobilize Ca²⁺ from Intracellular Stores, in Undifferentiated NG108‐15 Cells

1996 • 63 citations

Mutation of a conserved serine in TM4 of opioid receptors confers full agonistic properties to classical antagonists.

1996 • 62 citations

Examination of the involvement of supraspinal and spinal mu and delta opioid receptors in analgesia using the mu receptor deficient CXBK mouse.

1988 • 62 citations

Development of conformationally constrained linear peptides exhibiting a high affinity and pronounced selectivity for .delta. opioid receptors

1988 • 62 citations

Pertussis toxin differentially reduces the efficay of opioids to produce supraspinal analgesia in the mouse

1988 • 61 citations

Effect of pertussis toxin treatment on the down-regulation of opiate receptors in neuroblastoma X glioma NG108-15 hybrid cells.

1985 • 60 citations

Mapping the receptor domains critical for the binding selectivity of δ-opioid receptor ligands

1996 • 59 citations

G protein regulation of receptor signalling

1988 • 58 citations

delta Opioid receptor subtypes activate inositol-signaling pathways in the production of antinociception.

1998 • 57 citations

Characterization of [3H]naltrindole binding to delta opioid receptors in rat brain

1992 • 55 citations

Selective inhibition of [D-ALA2, GLU4]deltrophin antinociception by supraspinal, but not spinal, administration of an antisense oligodeoxynucleotide to an opioid delta receptor

1994 • 55 citations

Endomorphin-1 and endomorphin-2 are partial agonists at the human μ-opioid receptor

1998 • 55 citations

Delta but not mu-opioid receptors in the spinal cord are involved in antinociception induced by beta-endorphin given intracerebroventricularly in mice.

1990 • 54 citations

Evidence for the Existence of the β-Endorphin-Sensitive “ε-Opioid Receptor” in the Brain: The Mechanisms of ε-Mediated Antinociception

1998 • 54 citations

Antisense oligodeoxynucleotide to a δ-opioid receptor selectivily blocks the spinal antinociception induced by δ-, but not μ- or κ-opioid receptor agonists in the mouse

1994 • 54 citations

Opioid-induced stimulation of fetal respiratory activity by [D-Ala2]deltorphin I

1993 • 53 citations

Pertussis toxin abolishes the antinociception mediated by opioid receptors in rat spinal cord

1987 • 53 citations

Antibodies to the cloned mu-opioid receptor detect various molecular weight forms in areas of mouse brain.

1995 • 53 citations

Opioid regulation of mucosal ion transport in the mouse isolated jejunum.

1990 • 52 citations

Multiple affinity states of opiate receptor in neuroblastoma x glioma NG108-15 hybrid cells. Opiate agonist association rate is a function of receptor occupancy.

1985 • 51 citations

Antisense knockouts: molecular scalpels for the dissection of signal transduction

1994 • 50 citations

Interaction of [d-Pen2, d-Pen5]enkephalin and [d-Ala2, Glu4]deltorphin with δ-opioid receptor subtypes in vivo

1994 • 50 citations

Opioids at low concentration decrease openings of K+ channels in sensory ganglion neurons

1991 • 49 citations

Modulation of Protein Kinase C and cAMP-Dependent Protein Kinase by δ-Opioid

1997 • 48 citations

Genomic Structure of the Mouse δ Opioid Receptor Gene

1995 • 48 citations

Analgesic activity of a novel bivalent opioid peptide compared to morphine via different routes of administration

1991 • 48 citations

Bivalent opioid peptide analogues with reduced distances between pharmacophores

1987 • 48 citations

Opioids acting through delta receptors elicit a transient increase in the intracellular free calcium concentration in dorsal root ganglion-neuroblastoma hybrid ND8-47 cells.

1994 • 47 citations

Identification of the critical domains of the delta-opioid receptor involved in G protein coupling using site-specific synthetic peptides.

1996 • 47 citations

Molecular cloning and expression of a δ‐opioid recetpor from rat brain

1994 • 46 citations

Evidence for delta opioid receptor subtypes regulating adenylyl cyclase activity in rat brain

1994 • 46 citations

Delta-1 opioid receptor-mediated antinociceptive properties of a nonpeptidic delta opioid receptor agonist, (-)TAN-67, in the mouse spinal cord.

1997 • 45 citations

GX/Z Is Regulated by μ But Not δ Opioid Receptors in the Stimulation of the Low K_m GTPase Activity in Mouse Periaqueductal Grey Matter

1997 • 45 citations

An antisense oligodeoxynucleotide to μ-opioid receptors inhibits μ-opioid receptor agonist-induced analgesia in rats

1995 • 44 citations

Effects of a highly selective nonpeptide δ opioid receptor agonist, TAN-67, on morphine-induced antinociception in mice

1995 • 43 citations

[35S]GTPγS binding: A tool to evaluate functional activity of a cloned opioid receptor transiently expressed in COS cells

1996 • 42 citations

Antisense oligodeoxynucleotide treatment to the brain cannabinoid receptor inhibits antinociception

1996 • 42 citations

Intracerebroventricular treatment with an antisense oligodeoxynucleotide to κ-opioid receptors inhibited κ-agonist-induced analgesia in rats

1994 • 42 citations

Human delta opioid receptor: functional studies on stably transfected Chinese hamster ovary cells after acute and chronic treatment with the selective nonpeptidic agonist SNC-80.

1996 • 41 citations

Structure-activity relationship of biphalin. The synthesis and biological activities of new analogues with modifications in positions 3 and 4

1997 • 40 citations

Benzomorphan sites are ligand recognition sites of putative epsilon-receptors.

1984 • 40 citations

A CONFORMATIONAL ANALYSIS FOR LEUCINE‐ENKEPHALIN USING ACTIVITY AND BINDING DATA OF SYNTHETIC ANALOGUES

1977 • 38 citations

The third extracellular loop of the human delta-opioid receptor determines the selectivity of delta-opioid agonists.

1996 • 38 citations

Binding of 3H-β-endorphin in rat brain

1982 • 37 citations

GX/Z and Gi2 transducer proteins on μ/δ opioid-mediated supraspinal antinociception

1993 • 37 citations

The stereochemical requirements of the novel δ-opioid selective dipeptide antagonist TMT-Tic

1997 • 37 citations

Differentiation between rat brain and mouse vas deferens δ opioid receptors

1990 • 36 citations

Properties of TAN-67, a nonpeptide δ-opioid receptor agonist, at cloned human δ-and μ-opioid receptors

1995 • 36 citations

A single residue, Lys108, of the delta-opioid receptor prevents the mu-opioid-selective ligand [D-Ala2,N-MePhe4,Gly-ol5]enkephalin from binding to the delta-opioid receptor.

1996 • 36 citations

Effect of Cyclic AMP on Morphine Analgesia Tolerance and Physical Dependence

1972 • 36 citations

Molecular Biology of Opioid Receptors

1996 • 35 citations

The δ‐Opioid Receptor Regulates Activity of Ryanodine Receptors in the Human Neuroblastoma Cell Line SK‐N‐BE

1996 • 35 citations

μ and δ opioid agonists at low concentrations decrease voltage-dependent K+ currents in F11 neuroblastoma × DRG neuron hybrid cells via cholera toxin-sensitive receptors

1993 • 32 citations

Differential regulation of adenylyl cyclase activity by mu and delta opioids in rat caudate putamen and nucleus accumbens.

1993 • 32 citations

Relative efficacies of δ-opioid receptor agonists at the cloned human δ-opioid receptor

1997 • 32 citations

The mathematics of drug-receptor interactions

1966 • 30 citations

Activation of δ-Opioid Receptors Inhibits Neuronal-Like Calcium Channels and Distal Steps of Ca²⁺-Dependent Secretion in Human Small-Cell Lung Carcinoma Cells

1996 • 30 citations

Dual regulation by μ, δ and κ opioid receptor agonists of K+ conductance of DRG neurons and neuroblastoma × DRG neuron hybrid F11 cells

1995 • 30 citations

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

1976 • 29 citations

Human delta opioid receptor: a stable cell line for functional studies of opioids.

1995 • 28 citations

delta-Opioid receptor activates cAMP phosphodiesterase activities in neuroblastoma x glioma NG108-15 hybrid cells.

1993 • 28 citations

Antisense oligodeoxynucleotide to the Gi2 protein alpha subunit sequence inhibits an opioid-induced increase in the intracellular free calcium concentration in ND8-47 neuroblastoma x dorsal root ganglion hybrid cells.

1995 • 27 citations

Coupling of the Cloned μ‐Opioid Receptor with the ω‐Conotoxin‐Sensitive Ca²⁺ Current in NG108‐15 Cells

1995 • 26 citations

δ-opioid supraspinal antinociception in mice is mediated by G13 transducer proteins

1993 • 25 citations

Antisense oligodeoxynucleotides against μ- or κ-opioid receptors block agonist-induced body temperature changes in rats

1995 • 24 citations

Syntheses of Non-Peptidic Delta Opioid Agonists and Their Structure Activity Relationships.

1994 • 24 citations

Multiple states of opioid receptors may modulate adenylate cyclase in intact neuroblastoma X glioma hybrid cells.

1985 • 24 citations

Antagonism of Morphine Analgesia by Adenine, Adenosine, and Adenine Nucleotides

1973 • 24 citations

Pretreatment with pertussis toxin differentially modulates morphine- and beta-endorphin-induced antinociception in the mouse.

1996 • 23 citations

Intracerebroventricular injection of antibodies directed against Gsα enhances the supraspinal antinociception induced by morphine, β-endorphin and clonidine in mice

1992 • 23 citations

Delta opioid receptor down-regulation is independent of functional G protein yet is dependent on agonist efficacy.

1998 • 22 citations

Antisense oligodeoxynucleotide to a δ-opioid receptor given intrathecally blocks i.c.v. administered β-endorphin-induced antinociception in the mouse

1994 • 22 citations

A new type of Ca-channel modulation by a novel class of 1,4-dihydropyridines

1996 • 22 citations

Autoradiographic comparison of [3H]DPDPE and [3H]DSLET binding: evidence for distinct δ1 and δ2 opioid receptor populations in rat brain

1996 • 22 citations

Opioid agonist binding affinity is increased by magnesium in the presence of guanosine diphosphate but decreased by magnesium in the presence of guanyl-5'-yl imidodiphosphate.

1994 • 22 citations

[3H]Naltrindole: a potent and selective ligand for labeling δ-opioid receptors

1993 • 22 citations

Multiple opioid receptors and GTP-binding proteins.

1991 • 22 citations

δ-Opioid receptor: the third extracellular loop determines naltrindole selectivity

1996 • 20 citations

Metkephamid (Tyr-D-Ala-Gly-Phe-N(Me)Met-NH2), a potent opioid peptide: Receptor binding and analgesic properties

1982 • 20 citations

Effect of chronic D-Ala,2 D-Leu5-enkephalin or pertussis toxin treatment on the high-affinity state of delta opioid receptor in neuroblastoma x glioma NG108-15 hybrid cells.

1991 • 20 citations

Dissimilar efficacy of opioids to produce μ-mediated analgesia: Role of Gx/z and G12 transducer proteins

1994 • 20 citations

An examination of the relationship between μ-opioid antinociceptive efficacy and G-protein coupling using pertussis and cholera toxins

1997 • 19 citations

Cyclic AMP mediates mu and delta, but not kappa opioid analgesia in the spinal cord of the rat

1993 • 18 citations

Opioid‐Induced Increase in [Ca²⁺]_i in ND8‐47 Neuroblastoma × Dorsal Root Ganglion Hybrid Cells Is Mediated Through G Protein‐Coupled δ‐Opioid Receptors and Desensitized by Chronic Exposure to Opioid

1995 • 18 citations

A Gi2α antisense oligonucleotide differentiates morphine antinociception, constipation and acute dependence in mice

1995 • 18 citations

Studies on the structural prerequisites for the activation of the beta-endorphin receptor on the rat vas deferens.

1982 • 18 citations

In vivo evidence for the selectivity of ICI 154129 for the delta-opioid receptor

1985 • 16 citations

Cyclic AMP, morphine, met-enkephalin and neuronal firing.

1981 • 15 citations

Stimulation of spinal δ-opioid receptors in mice selectively enhances the attenuation of δ-opioid receptor-mediated antinociception by antisense oligodeoxynucleotide

1995 • 15 citations

Enhanced analgesic activity of D-Ala2 enkephalinamides following D-isomer substitutions at position five

1978 • 15 citations

Treatment with Antisense Oligodeoxynucleotide to a Conserved Sequence of Opioid Receptors Inhibits Antinociceptive Effects of Delta Subtype Selective Ligands

1995 • 15 citations

Regulation of δ‐Opioid Receptor mRNA Levels by Receptor‐Mediated and Direct Activation of the Adenylyl Cyclase‐Protein Kinase A Pathway

1997 • 14 citations

Improved Models for Pharmacological Null Experiments: Calculation of Drug Efficacy at Recombinant D1A Dopamine Receptors Stably Expressed in Clonal Cell Lines

1996 • 14 citations

The Carboxyl Terminus of Mouse δ-Opioid Receptor Is Not Required for Agonist-Dependent Activation

1997 • 13 citations

Trp²⁸⁴ of the Human δ Opioid Receptor is Required for SNC121 Binding but Not Binding of pCl-DPDPE, Deltorphin II or Naltrindole

1995 • 12 citations

Use of antisense oligodeoxynucleotide to determine δ-opioid receptor involvement in [d-Ala2]deltorphin II-induced locomotor hyperactivity

1996 • 12 citations

Analgesia following local injection of dibutyryl cyclic nucleotides at sites in the rat CNS

1981 • 12 citations

Steroid-monoamine feedback interactions in discrete brain regions using as a model the monosodium glutamate (MSG)-lesioned rat

1984 • 12 citations

Pretreatment with pertussis toxin blocks morphine-but not β-endorphin-induced antinociception in the mouse

1995 • 11 citations

Pretreatment with β-endorphin facilitates the attenuation of δ-opioid receptor-mediated antinociception caused by δ-opioid receptor antisense oligodeoxynucleotide

1995 • 11 citations

Phosphorylation of cyclic AMP response element-binding protein and induction of c-fos gene expression on withdrawal from chronic treatment with carbachol in NG108-15 cells.

1995 • 11 citations

In vivo treatment with antisense oligodeoxynucleotide to κ-opioid receptors inhibited κ-agonist-induced analgesia in rats

1994 • 7 citations

Expression of functional trk protooncogene in human monocytes

1994 • 2 citations