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Current status of inverse agonism at serotonin2A (5-HT2A) and 5-HT2C receptors

Data up to Jan 2025

Published2008
Citations109
References140

Total Citations Per Year

Abstract

References (140)

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Serotonin2C receptors tonically suppress the activity of mesocortical dopaminergic and adrenergic, but not serotonergic, pathways: A combined dialysis and electrophysiological analysis in the rat

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Serotonin 5-HT2A receptors are expressed on pyramidal cells and interneurons in the rat cortex

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

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m-Chlorophenylpiperazine as a probe of serotonin function

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5-HT1A and 5-HT2A Receptor mRNAs and Binding Site Densities Are Differentially Altered in Schizophrenia

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5-Hydroxytryptamine2-Family Receptors (5-Hydroxytryptamine2A, 5-Hydroxytryptamine2B, 5-Hydroxytryptamine2C) Where Structure Meets Function

1998 • 280 citations

Serotonin 5-HT2C Receptors as a Target for the Treatment of Depressive and Anxious States: Focus on Novel Therapeutic Strategies

2005 • 276 citations

The classification of seven transmembrane receptors in recombinant expression systems.

1996 • 271 citations

Constitutively active 5-hydroxytryptamine2C receptors reveal novel inverse agonist activity of receptor ligands.

1994 • 249 citations

Anxiety-like effects induced by acute fluoxetine, sertraline or m-CPP treatment are reversed by pretreatment with the 5-HT2C receptor antagonist SB-242084 but not the 5-HT1A receptor antagonist WAY-100635

2001 • 249 citations

5-HT2 Receptors

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Role of 5-HT2C receptors in the control of central dopamine function

2001 • 236 citations

Partial agonists, full agonists, antagonists: dilemmas of definition

1993 • 234 citations

Selective Abnormalities of Prefrontal Serotonergic Receptors in Schizophrenia

1993 • 234 citations

Selective blockade of serotonin-2C/2B receptors enhances mesolimbic and mesostriatal dopaminergic function: a combined in vivo electrophysiological and microdialysis study

1999 • 220 citations

Ultrastructural localization of serotonin2A receptors in the middle layers of the rat prelimbic prefrontal cortex

2003 • 209 citations

Altered G Protein‐Coupling Functions of RNA Editing Isoform and Splicing Variant Serotonin2C Receptors

2000 • 195 citations

A three-state receptor model of agonist action

1997 • 192 citations

Role of the Serotonin 5-HT2A Receptor in Learning

2003 • 192 citations

Differential Actions of Antiparkinson Agents at Multiple Classes of Monoaminergic Receptor. III. Agonist and Antagonist Properties at Serotonin, 5-HT1 and 5-HT2, Receptor Subtypes

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5-hydroxytryptamine2A receptor inverse agonists as antipsychotics.

2001 • 190 citations

Neuroendocrine Effects ofM-Chlorophenylpiperazine, a Serotonin Agonist, in Humans

1985 • 181 citations

Serotonin 5‐HT2C Receptor RNA Editing Alters Receptor Basal Activity

1999 • 180 citations

Evidence for a Model of Agonist-induced Activation of 5-Hydroxytryptamine 2A Serotonin Receptors That Involves the Disruption of a Strong Ionic Interaction between Helices 3 and 6

2002 • 177 citations

Inverse agonist activity of atypical antipsychotic drugs at human 5-hydroxytryptamine2C receptors.

2000 • 169 citations

RNA editing of the 5-HT2C receptor is reduced in schizophrenia

2001 • 165 citations

5-HT2 receptors exert a state-dependent regulation of dopaminergic function: studies with MDL 100,907 and the amphetamine analogue, 3,4-methylenedioxymethamphetamine

1992 • 160 citations

Serotonin2 (5-HT2) receptor binding in the frontal cortex of schizophrenic patients

1991 • 154 citations

Serotonin2C receptor localization in GABA neurons of the rat medial prefrontal cortex: Implications for understanding the neurobiology of addiction

2007 • 153 citations

Agonist-independent regulation of constitutively active G-protein-coupled receptors

1998 • 150 citations

Messenger RNA Editing of the Human Serotonin 5-HT2C Receptor

1999 • 149 citations

Serotonin 2C receptors within the basolateral amygdala induce acute fear-like responses in an open-field environment

2003 • 146 citations

Inverse agonism and the regulation of receptor number

1997 • 142 citations

WAY-163909 [(7bR,10aR)-1,2,3,4,8,9,10,10a-Octahydro-7bH-cyclopenta-[b][1,4]diazepino[6,7,1hi]indole]: A Novel 5-Hydroxytryptamine 2C Receptor-Selective Agonist with Preclinical Antipsychotic-Like Activity

2006 • 142 citations

Inverse agonist actions of typical and atypical antipsychotic drugs at the human 5-hydroxytryptamine(2C) receptor.

2001 • 141 citations

Influence of the 5-HT2C receptor antagonist, SB-242084, in tests of anxiety

2002 • 139 citations

A guide to RNA editing.

1997 • 139 citations

Pharmacological characterization of 8‐OH‐DPAT‐induced inhibition of rat hippocampal 5‐HT release in vivo as measured by microdialysis

1989 • 137 citations

Anxiogenic-like effects of fluprazine and eltoprazine in the mouse elevated plus-maze

1992 • 133 citations

mCPP-induced anxiety in the light-dark box in rats - a new method for screening anxiolytic activity

1998 • 133 citations

Signal transduction differences between 5-hydroxytryptamine type 2A and type 2C receptor systems.

1994 • 130 citations

Attenuation of haloperidol‐induced catalepsy by a 5‐HT2C receptor antagonist

1999 • 129 citations

Anxiogenic effects of m-CPP in patients with panic disorder: Comparison to caffeine's anxiogenic effects

1991 • 128 citations

Mechanisms of inverse agonism at G-protein-coupled receptors

2002 • 124 citations

RNA Editing of the Human Serotonin 5-HT2CReceptor Alters Receptor-mediated Activation of G13Protein

2001 • 105 citations

Inverse Agonist and Neutral Antagonist Actions of Antidepressants at Recombinant and Native 5-Hydroxytryptamine2CReceptors: Differential Modulation of Cell Surface Expression and Signal Transduction

2007 • 101 citations

Lysergic acid diethylamide and [−]-2,5-dimethoxy-4-methylamphetamine increase extracellular glutamate in rat prefrontal cortex

2004 • 100 citations

SB-243213; a selective 5-HT2C receptor inverse agonist with improved anxiolytic profile: lack of tolerance and withdrawal anxiety

2001 • 99 citations

Novel actions of inverse agonists on 5-HT2C receptor systems.

1999 • 98 citations

Creation of a constitutively activated state of the 5-hydroxytryptamine2A receptor by site-directed mutagenesis: inverse agonist activity of antipsychotic drugs.

1998 • 93 citations

Selective destruction of brain serotonin neurons by 5,7-dihydroxytryptamine increases responding for a conditioned reward

1999 • 91 citations

5-HT2A receptor density is decreased in the at-risk mental state

2007 • 91 citations

Agonist-induced modulation of inverse agonist efficacy at the beta 2-adrenergic receptor.

1996 • 90 citations

Ritanserin potentiates the stimulatory effects of raclopride on neuronal activity and dopamine release selectively in the mesolimbic dopaminergic system

1995 • 90 citations

Identification and Characterization of RNA Editing Events within the 5‐HT2C Receptora

1998 • 89 citations

Evidence for the existence of serotonin type-2 receptors on cholinergic terminals in rat cortex

1985 • 88 citations

Stimulation of serum cortisol and prolactin secretion in humans by MK-212, a centrally active serotonin agonist

1988 • 86 citations

RNA Editing

1996 • 85 citations

Central Serotonin2C Receptor: From Physiology to Pathology

2006 • 84 citations

Serotonergic regulation of associative learning

1995 • 83 citations

Behavioral effects of systemically administered MK-212 are prevented by ritanserin microinfusion into the basolateral amygdala of rats exposed to the elevated plus-maze

2005 • 82 citations

Apparent Loss-of-Function Mutant GPCRs Revealed as Constitutively Desensitized Receptors

2002 • 79 citations

Messenger RNA Editing of the Human Serotonin 5-HT2C Receptor

1999 • 79 citations

The 5‐HT2A receptor antagonist M100,907 prevents extracellular glutamate rising in response to NMDA receptor blockade in the mPFC

2004 • 78 citations

The effects of 5-HT1B characterizing agents in the mouse elevated plus-maze

1990 • 78 citations

Differential Regulation of Rat 5-HT2A and 5-HT2C Receptors after Chronic Treatment with Clozapine, Chlorpromazine and Three Putative Atypical Antipsychotic Drugs

1995 • 77 citations

Serotonin Induces EPSCs Preferentially in Layer V Pyramidal Neurons of the Frontal Cortex in the Rat

2000 • 75 citations

The Human B1 Bradykinin Receptor Exhibits High Ligand-independent, Constitutive Activity

2001 • 74 citations

Evidence for accelerated desensitisation of 5-HT2C receptors following combined treatment with fluoxetine and the 5-HT1A receptor antagonist, WAY 100,635, in the rat

2000 • 74 citations

Region‐dependent regulation of mesoaccumbens dopamine neurons in vivo by the constitutive activity of central serotonin2C receptors

2006 • 72 citations

Effect of SB 200646A, a 5-HT2C/5-HT2B receptor antagonist, in two conflict models of anxiety

1995 • 72 citations

Increased basal phosphorylation of the constitutively active serotonin 2C receptor accompanies agonist-mediated desensitization.

1995 • 70 citations

Anxiogenic-like effects of mCPP microinfusions into the amygdala (but not dorsal or ventral hippocampus) in mice exposed to elevated plus-maze

2007 • 70 citations

Agonist‐Induced Phosphoinositide Hydrolysis in Choroid Plexus

1986 • 69 citations

Differences in rapid desensitization of 5-hydroxytryptamine2A and 5-hydroxytryptamine2C receptor-mediated phospholipase C activation.

2001 • 66 citations

5-Hydroxytryptamine2C Receptor Contribution to m-Chlorophenylpiperazine and N-Methyl-β-carboline-3-carboxamide-Induced Anxiety-Like Behavior and Limbic Brain Activation

2006 • 64 citations

Rapid Desensitization of the Serotonin2C Receptor System: Effector Pathway and Agonist Dependence

2002 • 61 citations

Activation of Presynaptic 5-Hydroxytryptamine 2A Receptors Facilitates Excitatory Synaptic Transmission via Protein Kinase C in the Dorsolateral Septal Nucleus

2002 • 59 citations

A voxel-by-voxel analysis of [18F]setoperone PET data shows no substantial serotonin 5-HT2A receptor changes in schizophrenia

2000 • 53 citations

Abnormalities in 5-HT2A receptor mRNA expression in frontal cortex of chronic elderly schizophrenics with varying histories of neuroleptic treatment

2000 • 51 citations

Discriminative stimulus effects of m-chlorophenylpiperazine as a model of the role of serotonin receptors in anxiety

2003 • 50 citations

A Conservative, Single-Amino Acid Substitution in the Second Cytoplasmic Domain of the Human Serotonin2CReceptor Alters Both Ligand-Dependent and -Independent Receptor Signaling

2007 • 50 citations

Effects of imipramine and serotonin-2 agonists and antagonists on serotonin-2 and beta-adrenergic receptors following noradrenergic or serotonergic denervation

1989 • 49 citations

Constitutive Activity of G-Protein Coupled Receptors: Emphasis on Serotonin Receptors

2002 • 47 citations

Effects of serotonin 5-HT 2A/2C antagonists on associative learning in the rabbit

1998 • 47 citations

Activation of 5‐HT2 receptors enhances the release of acetylcholine in the prefrontal cortex and hippocampus of the rat

2004 • 45 citations

Therapeutic Potential of 5-HT2C Receptor Antagonists in the Treatment of Anxiety Disorders

2003 • 42 citations

Forebrain serotonin depletion facilitates the acquisition and performance of a conditional visual discrimination task in rats

1999 • 40 citations

Selective remodeling of rabbit frontal cortex: relationship between 5-HT 2A receptor density and associative learning

2004 • 37 citations

Effects of LSD, Ritanserin, 8-OH-DPAT, and Lisuride on Classical Conditioning in the Rabbit

1998 • 35 citations

Differential Effects of Forebrain 5‐Hydroxytryptamine Depletions on Pavlovian Aversive Conditioning to Discrete and Contextual Stimuli in the Rat

1995 • 34 citations

The physiological significance of constitutive receptor activity

2005 • 34 citations

Effect of serotonin depletion on 5-HT2A-mediated learning in the rabbit: evidence for constitutive activity of the 5-HT2A receptor in vivo

2005 • 31 citations

Selective and divergent regulation of cortical 5-HT(2A) receptors in rabbit.

2001 • 29 citations

5-HT 2C receptor mediation of unconditioned escape behaviour in the unstable elevated exposed plus maze

2002 • 27 citations

Development of functionally selective agonists as novel therapeutic agents

2006 • 26 citations

Intraventricular 5,7-dihydroxytryptamine lesions disrupt acquisition of working memory task rules but not performance once learned

2003 • 21 citations

Dissociable effects of the 5-HT2 antagonist mianserin on associative learning and performance in the rabbit

2000 • 19 citations

Regulation of 5-HT1A and 5-HT1B receptor systems by phospholipid signaling cascades

2001 • 19 citations

5-HT 2C Receptor Agonists: Pharmacological Characteristics and Therapeutic Potential

1998 • 16 citations

The Time-Course for Up- and Down-Regulation of the Cortical 5-Hydroxytryptamine (5-HT)2A Receptor Density Predicts 5-HT2A Receptor-Mediated Behavior in the Rabbit

2007 • 15 citations

Prenalterol as a Selective Cardiostimulant

1985 • 15 citations

Prenalterol as a selective cardiostimulant: differences between organ and receptor selectivity.

1985 • 15 citations

Serotonergic depletion increases conditioned suppression to background stimuli in the rat

2001 • 13 citations

5-HT-2 Receptors

2007 • 12 citations

5-HT2C SEROTONIN RECEPTORS: CELLULAR LOCALIZATION AND CONTROL OF DOPAMINERGIC PATHWAYS IN THE RAT BRAIN

2007 • 1 citations

Deleted Work

1955 • 0 citations

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Current status of inverse agonism at serotonin2A (5-HT2A) and 5-HT2C receptors (2008) – Pharmacology & Therapeutics | Metascience Observatory Explorer