Current status of inverse agonism at serotonin2A (5-HT2A) and 5-HT2C receptors
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References (140)
Classification of typical and atypical antipsychotic drugs on the basis of dopamine D-1, D-2 and serotonin2 pKi values.
1989 • 1,313 citations
A mutation-induced activated state of the beta 2-adrenergic receptor. Extending the ternary complex model.
1993 • 1,213 citations
International Union of Pharmacology. XV. Subtypes of gamma-aminobutyric acidA receptors: classification on the basis of subunit structure and receptor function.
1998 • 1,204 citations
Hallucinogens
2004 • 1,077 citations
Functional Selectivity and Classical Concepts of Quantitative Pharmacology
2006 • 1,076 citations
Regulation of serotonin-2C receptor G-protein coupling by RNA editing
1997 • 985 citations
G Protein-Coupled Receptor Allosterism and Complexing
2002 • 910 citations
DESENSITIZATION OF G PROTEIN–COUPLED RECEPTORS AND NEURONAL FUNCTIONS
2004 • 829 citations
Identification of a serotonin/glutamate receptor complex implicated in psychosis
2008 • 757 citations
Behavioural and pharmacological characterisation of the elevated “zero-maze” as an animal model of anxiety
1994 • 702 citations
Conformational complexity of G-protein-coupled receptors
2007 • 675 citations
The Role of Serotonin in Antipsychotic Drug Action
1999 • 672 citations
Constitutive activity of G-protein-coupled receptors: cause of disease and common property of wild-type receptors
2002 • 606 citations
Pharmacologic mechanisms of serotonergic regulation of dopamine neurotransmission
2006 • 586 citations
Serotonin receptors in the human brain—III. Autoradiographic mapping of serotonin-1 receptors
1987 • 569 citations
How receptors talk to trimeric G proteins
1997 • 562 citations
Serotonin model of schizophrenia: emerging role of glutamate mechanisms
2000 • 520 citations
SB 242084, a Selective and Brain Penetrant 5-HT 2C Receptor Antagonist
1997 • 519 citations
Antagonists with negative intrinsic activity at delta opioid receptors coupled to GTP-binding proteins.
1989 • 519 citations
5-Hydroxytryptamine 2A serotonin receptors in the primate cerebral cortex: Possible site of action of hallucinogenic and antipsychotic drugs in pyramidal cell apical dendrites
1998 • 510 citations
The two-state model of receptor activation
1995 • 492 citations
Serotonin function in anxiety
1987 • 467 citations
Molecular Basis of Receptor/G-Protein-Coupling Selectivity
1998 • 444 citations
Inverse, protean, and ligand‐selective agonism: matters of receptor conformation
2001 • 403 citations
RNA Editing of the Human Serotonin 5-Hydroxytryptamine 2C Receptor Silences Constitutive Activity
1999 • 353 citations
Serotonin receptors in the human brain—IV. Autoradiographic mapping of serotonin-2 receptors
1987 • 342 citations
Serotonin2C receptors tonically suppress the activity of mesocortical dopaminergic and adrenergic, but not serotonergic, pathways: A combined dialysis and electrophysiological analysis in the rat
2000 • 333 citations
Serotonin 5-HT2A receptors are expressed on pyramidal cells and interneurons in the rat cortex
1997 • 324 citations
5-HT2C receptor agonists: pharmacological characteristics and therapeutic potential.
1998 • 324 citations
5‐HT1 agonists reduce 5‐hydroxytryptamine release in rat hippocampus in vivo as determined by brain microdialysis
1989 • 322 citations
FUNCTIONAL AND STRUCTURAL COMPLEXITY OF SIGNAL TRANSDUCTION VIA G-PROTEIN-COUPLED RECEPTORS
1997 • 321 citations
Noradrenergic and Serotonergic Function in Posttraumatic Stress Disorder
1997 • 317 citations
Constitutive Activity of the Serotonin2C Receptor InhibitsIn VivoDopamine Release in the Rat Striatum and Nucleus Accumbens
2004 • 301 citations
An operational model of pharmacological agonism: the effect of E/[A] curve shape on agonist dissociation constant estimation
1985 • 295 citations
m-Chlorophenylpiperazine as a probe of serotonin function
1991 • 291 citations
5-HT1A and 5-HT2A Receptor mRNAs and Binding Site Densities Are Differentially Altered in Schizophrenia
1996 • 287 citations
Anxiogenic-like effects of mCPP and TFMPP in animal models are opposed by 5-HT1C receptor antagonists
1989 • 285 citations
Structural Instability of a Constitutively Active G Protein-coupled Receptor
1997 • 285 citations
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
2004 • 247 citations
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
2002 • 190 citations
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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