Functional Selectivity and Classical Concepts of Quantitative Pharmacology

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1994 • 2,935 citations

Structural basis of glutamate recognition by a dimeric metabotropic glutamate receptor

2000 • 1,197 citations

Principles for modulation of the nuclear receptor superfamily

2004 • 1,165 citations

Magic shotguns versus magic bullets: selectively non-selective drugs for mood disorders and schizophrenia

2004 • 1,111 citations

Progressive Multifocal Leukoencephalopathy after Natalizumab Therapy for Crohn's Disease

2005 • 1,062 citations

Pharmacologic Analysis of Drug Receptor Interaction

1988 • 936 citations

Aripiprazole, A Novel Atypical Antipsychotic Drug with a Unique and Robust Pharmacology

2003 • 918 citations

G Protein-Coupled Receptor Allosterism and Complexing

2002 • 910 citations

Aripiprazole, a Novel Antipsychotic, Is a High-Affinity Partial Agonist at Human Dopamine D2 Receptors

2002 • 896 citations

H1-Receptor Antagonists

1994 • 757 citations

Organization of the G Protein-coupled Receptors Rhodopsin and Opsin in Native Membranes

2003 • 591 citations

Morphine Activates Opioid Receptors without Causing Their Rapid Internalization

1996 • 536 citations

Effector Pathway-Dependent Relative Efficacy at Serotonin Type 2A and 2C Receptors: Evidence for Agonist-Directed Trafficking of Receptor Stimulus

1998 • 502 citations

Role for G protein-coupled receptor kinase in agonist-specific regulation of μ-opioid receptor responsiveness

1998 • 501 citations

The Human Polyomavirus, JCV, Uses Serotonin Receptors to Infect Cells

2004 • 456 citations

Nephrogenic Diabetes Insipidus

2001 • 432 citations

Functional Dissociation of μ Opioid Receptor Signaling and Endocytosis

1999 • 422 citations

Interactions of the Novel Antipsychotic Aripiprazole (OPC-14597) with Dopamine and Serotonin Receptor Subtypes

1999 • 407 citations

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

1997 • 378 citations

Morphine-activated opioid receptors elude desensitization by β-arrestin

1998 • 374 citations

Nephrogenic Syndrome of Inappropriate Antidiuresis

2005 • 364 citations

Functionally Different Agonists Induce Distinct Conformations in the G Protein Coupling Domain of the β2Adrenergic Receptor

2001 • 361 citations

Structural views of the ligand-binding cores of a metabotropic glutamate receptor complexed with an antagonist and both glutamate and Gd ³⁺

2002 • 337 citations

Regulation of Opioid Receptor Trafficking and Morphine Tolerance by Receptor Oligomerization

2002 • 335 citations

Sequential Binding of Agonists to the β2 Adrenoceptor

2003 • 333 citations

Agonist-selective endocytosis of mu opioid receptor by neurons in vivo.

1996 • 327 citations

mu-Opioid receptor internalization: opiate drugs have differential effects on a conserved endocytic mechanism in vitro and in the mammalian brain.

1998 • 323 citations

Dopamine Partial Agonists

2004 • 321 citations

New Concepts in Drug Discovery: Collateral Efficacy and Permissive Antagonism

2005 • 313 citations

Constitutive Activity of the Serotonin2C Receptor InhibitsIn VivoDopamine Release in the Rat Striatum and Nucleus Accumbens

2004 • 301 citations

Crosstalk in G protein-coupled receptors: Changes at the transmembrane homodimer interface determine activation

2005 • 282 citations

Paradoxical trafficking and regulation of 5-HT2A receptors by agonists and antagonists

2001 • 281 citations

Transcriptome Fingerprints Distinguish Hallucinogenic and Nonhallucinogenic 5-Hydroxytryptamine 2A Receptor Agonist Effects in Mouse Somatosensory Cortex

2003 • 279 citations

Structure-based Analysis of GPCR Function: Evidence for a Novel Pentameric Assembly between the Dimeric Leukotriene B4 Receptor BLT1 and the G-protein

2003 • 270 citations

7-(4-[4-(2,3-Dichlorophenyl)-1-piperazinyl]butyloxy)-3,4-dihydro-2(1H)-quinolinone (OPC-14597), a new putative antipsychotic drug with both presynaptic dopamine autoreceptor agonistic activity and postsynaptic D2 receptor antagonistic activity.

1995 • 268 citations

Closed state of both binding domains of homodimeric mGlu receptors is required for full activity

2004 • 267 citations

μ-Opioid Receptor Internalization: Opiate Drugs Have Differential Effects on a Conserved Endocytic MechanismIn Vitroand in the Mammalian Brain

1998 • 265 citations

The Dopamine Receptors

1997 • 260 citations

Probing the β2 Adrenoceptor Binding Site with Catechol Reveals Differences in Binding and Activation by Agonists and Partial Agonists

2005 • 260 citations

Constitutive arrestin-mediated desensitization of a human vasopressin receptor mutant associated with nephrogenic diabetes insipidus

2000 • 235 citations

μ Opioid Receptor Phosphorylation, Desensitization, and Ligand Efficacy

1997 • 218 citations

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

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Finding New Tricks For Old Drugs: An Efficient Route For Public-Sector Drug Discovery

2005 • 216 citations

Serotonin stimulates phospholipase A2 and the release of arachidonic acid in hippocampal neurons by a type 2 serotonin receptor that is independent of inositolphospholipid hydrolysis.

1990 • 215 citations

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

1965 • 207 citations

Regulation of serotonin2 (5-HT2) receptors labeled with [3H]spiroperidol by chronic treatment with the antidepressant amitriptyline.

1980 • 207 citations

Antagonist-stimulated internalization of the G protein-coupled cholecystokinin receptor.

1997 • 198 citations

Aripiprazole has Functionally Selective Actions at Dopamine D2 Receptor-Mediated Signaling Pathways

2006 • 188 citations

Nephrogenic diabetes insipidus. A V2 vasopressin receptor unable to stimulate adenylyl cyclase

1993 • 185 citations

Three-dimensional representations of G protein-coupled receptor structures and mechanisms

2002 • 173 citations

A concept for G protein activation by G protein-coupled receptor dimers: the transducin/rhodopsin interface

2004 • 171 citations

Trans-10,11-dihydroxy-5,6,6a,7,8,12b-hexahydrobenzo[a]phenanthridine: a highly potent selective dopamine D1 full agonist

1990 • 171 citations

μ-Opioid Receptors: Ligand-Dependent Activation of Potassium Conductance, Desensitization, and Internalization

2002 • 168 citations

A small region of the beta-adrenergic receptor is selectively involved in its rapid regulation.

1991 • 166 citations

Clozapine and other 5-hydroxytryptamine-2A receptor antagonists alter the subcellular distribution of 5-hydroxytryptamine-2A receptors in vitro and in vivo

1999 • 166 citations

Activation-independent Parathyroid Hormone Receptor Internalization Is Regulated by NHERF1 (EBP50)

2003 • 164 citations

Ligand-induced rearrangement of the dimeric metabotropic glutamate receptor 1α

2004 • 163 citations

The Dynamin-dependent, Arrestin-independent Internalization of 5-Hydroxytryptamine 2A (5-HT2A) Serotonin Receptors Reveals Differential Sorting of Arrestins and 5-HT2A Receptors during Endocytosis

2001 • 158 citations

Serotonin 5-Hydroxytryptamine_2AReceptor-Coupled Phospholipase C and Phospholipase A₂Signaling Pathways Have Different Receptor Reserves

2003 • 155 citations

Characterization of Agonist Stimulation of cAMP-Dependent Protein Kinase and G Protein-Coupled Receptor Kinase Phosphorylation of the β₂-Adrenergic Receptor Using Phosphoserine-Specific Antibodies

2004 • 151 citations

RNA‐editing of the 5‐HT_2C receptor alters agonist‐receptor‐effector coupling specificity

2001 • 139 citations

"Dopamine System Stabilizers, Aripiprazole, and the Next Generation of Antipsychotics, Part 1: "Goldilocks" Actions at Dopamine Receptors

2001 • 138 citations

Multiple mechanisms of serotonergic signal transduction

1987 • 133 citations

Dopamine System Stabilizers, Aripiprazole, and the Next Generation of Antipsychotics, Part 2: Illustrating Their Mechanism of Action

2001 • 129 citations

C5a Receptor Activation

1999 • 124 citations

Functional Selectivity of Dopamine Receptor Agonists. I. Selective Activation of Postsynaptic Dopamine D₂Receptors Linked to Adenylate Cyclase

2002 • 121 citations

Conserved Helix 7 Tyrosine Acts as a Multistate Conformational Switch in the 5HT2C Receptor

2002 • 119 citations

A complex signaling cascade links the serotonin_2A receptor to phospholipase A₂ activation: the involvement of MAP kinases

2003 • 117 citations

Partial Dopamine Agonists and Dopaminergic Stabilizers, in the Treatment of Psychosis

2002 • 116 citations

Supersensitivity to opioids following the chronic blockade of endorphin action by naloxone

1979 • 109 citations

beta-Adrenergic receptor kinase. Activity of partial agonists for stimulation of adenylate cyclase correlates with ability to promote receptor phosphorylation.

1988 • 106 citations

Dihydrexidine, a novel selective high potency full dopamine D-1 receptor agonist

1989 • 106 citations

Differential Activation of Gq/11 and Gi₃Proteins at 5-Hydroxytryptamine_2CReceptors Revealed by Antibody Capture Assays: Influence of Receptor Reserve and Relationship to Agonist-Directed Trafficking

2002 • 106 citations

The elusive nature of intrinsic efficacy

1998 • 102 citations

Rapid agonist-induced internalization of the 5-hydroxytryptamine2A receptor occurs via the endosome pathway in vitro.

1996 • 102 citations

Chronic treatment with dopamine receptor antagonists: behavioral and pharmacologic effects on D1 and D2 dopamine receptors

1988 • 101 citations

Dihydrexidine, a novel full efficacy D1 dopamine receptor agonist.

1992 • 100 citations

Partial agonist properties of the antipsychotics SSR181507, aripiprazole and bifeprunox at dopamine D2 receptors: G protein activation and prolactin release

2006 • 90 citations

Mass Spectrometric Analysis of Agonist Effects on Posttranslational Modifications of the β-2 Adrenoceptor in Mammalian Cells

2005 • 89 citations

Functional Selectivity of D₂Receptor Ligands in a Chinese Hamster Ovary hD_2LCell Line: Evidence for Induction of Ligand-Specific Receptor States

2004 • 86 citations

Functional Selectivity of Dopamine Receptor Agonists. II. Actions of Dihydrexidine in D_2LReceptor-Transfected MN9D Cells and Pituitary Lactotrophs

2002 • 82 citations

Inverse agonism: theory and practice

1995 • 80 citations

Three-dimensional structure of an invertebrate rhodopsin and basis for ordered alignment in the photoreceptor membrane 1 1Edited by D. Rees

2001 • 74 citations

Molecular Basis of Partial Agonism: Orientation of Indoleamine Ligands in the Binding Pocket of the Human Serotonin 5-HT2A Receptor Determines Relative Efficacy

2003 • 73 citations

A pathophysiological paradigm for the therapy of psychiatric disease

2005 • 73 citations

Chronic mianserin treatment decreases 5-HT2 receptor binding without altering 5-HT2 receptor mRNA levels

1991 • 68 citations

Pleiotropic Behavior of 5‐HT_2A and 5‐HT_2C Receptor Agonists

1998 • 67 citations

Differential Activation of Adenylate Cyclase and Receptor Internalization by Novel Dopamine D₁ Receptor Agonists

2005 • 66 citations

The assessment of antagonist potency under conditions of transient response kinetics

1999 • 65 citations

Conformational Analysis of D₁ Dopamine Receptor Agonists: Pharmacophore Assessment and Receptor Mapping

1996 • 65 citations

Rapid Desensitization of the Serotonin_2C Receptor System: Effector Pathway and Agonist Dependence

2002 • 61 citations

Mechanisms of Ligand-Induced Desensitization of the 5-Hydroxytryptamine_2AReceptor

2002 • 61 citations

Serotonin 5‐HT_2A receptor activation induces 2‐arachidonoylglycerol release through a phospholipase c‐dependent mechanism

2006 • 59 citations

Constitutive Activation and Endocytosis of the Complement Factor 5a Receptor: Evidence for Multiple Activated Conformations of a G Protein‐Coupled Receptor

2002 • 53 citations

5-HT2A receptor-stimulated phosphoinositide hydrolysis in the stimulus effects of hallucinogens

2002 • 52 citations

Conformational analysis and molecular modeling of 1-phenyl-, 4-phenyl-, and 1-benzyl-1,2,3,4-tetrahydroisoquinolines as D1 dopamine receptor ligands

1989 • 50 citations

Dynamic mechanisms of non-classical antagonism by competitive AT1 receptor antagonists

2000 • 45 citations

Quantitative Information Management for the Biochemical Computation of Cellular Networks

2004 • 41 citations

Regulation of 5-HT2A receptor mRNA levels and binding sites in rat frontal cortex by the agonist DOI and the antagonist mianserin

2000 • 38 citations

Differences in conformational properties of the second intracellular loop (IL2) in 5HT2C receptors modified by RNA editing can account for G protein coupling efficiency

2001 • 38 citations

Differential phospholipase C activation by phenylalkylamine serotonin 5‐HT_2A receptor agonists

2005 • 37 citations

beta-Adrenergic-receptor kinase

1997 • 37 citations

Mianserin‐Induced Down‐Regulation of Human 5‐Hydroxytryptamine_2A and 5‐Hydroxytryptamine_2C Receptors Stably Expressed in the Human Neuroblastoma Cell Line SH‐SY5Y

1997 • 34 citations

The structure and dynamics of GPCR oligomers: a new focus in models of cell-signaling mechanisms and drug design.

2005 • 34 citations

Hallucinogen actions on 5-HT receptors reveal distinct mechanisms of activation and signaling by G protein-coupled receptors

2005 • 33 citations

Biomedical Applications of Computer Modeling

2000 • 31 citations

Kenakin replies

1995 • 26 citations

Use of fluorescence spectroscopy to study conformational changes in the β2-adrenoceptor

2002 • 26 citations

Locomotor inhibition, yawning and vacuous chewing induced by a novel dopamine D2 post-synaptic receptor agonist

1997 • 24 citations

Therapeutic targeting of α4-integrins in chronic inflammatory diseases: tipping the scales of risk towards benefit?

2005 • 24 citations

Dopamine receptor subtypes : from basic science to clinical application

1998 • 24 citations

An evaluation of the ability of a series of full alpha-1 adrenoceptor agonists to release internal calcium in venous smooth muscle.

1985 • 19 citations

Synthesis and pharmacological evaluation of substituted naphth[1,2,3- de ]isoquinolines (dinapsoline analogues) as D 1 and D 2 dopamine receptor ligands

2003 • 18 citations

Molecular Drug Design and Dopamine Receptors

1997 • 15 citations

From the Static to the Dynamic

2000 • 6 citations

Chapter 1. Promise and progress of central G-protein coupled receptor modulators for obesity treatments

2002 • 6 citations