"目录号: HY-14545
GPCR/G ProteinNeuronal Signaling-
Amisulpride(DAN 2163)是多巴胺拮抗剂，对D2和D3受体的Ki分别为2.8 nM和3.2 nM。
Dopamine Receptor
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Chlorpromazine hydrochloride-Brexpiprazole-Haloperidol-Cabergoline-Clozapine-Cariprazine hydrochloride-L-DOPA-Perphenazine-Dopamine hydrochloride-Oxidopamine hydrobromide-Sertindole-B-HT 920-Azaperone-Fluphenazine dihydrochloride-Iloperidone-
生物活性
Description
Amisulpride(DAN 2163) is an antipsychotic drug, which is a selective dopamine antagonist (Ki=2.8 nM D2 receptor; Ki=3.2 nM D3 receptor).Target: D2/D3 receptorAmisulpride is an atypical antipsychotic used to treat psychosis in schizophrenia and episodes of mania in bipolar disorder. In small doses it is also used to treat depression. Amisulpride functions primarily as a D2 and D3 receptor antagonist. It has high affinity for these receptors with dissociation constants of 2.8 nM and 3.2 nM, respectively [1]. At low doses (< or = 10 mg/kg) amisulpride preferentially blocks presynaptic dopamine autoreceptors that control dopamine synthesis and release in the rat, whereas at higher doses (40-80 mg/kg) postsynaptic dopamine D2 receptor occupancy and antagonism is apparent. In contrast, haloperidol is active in all of these paradigms within the same dose range. Amisulpridepreferentially inhibits in vivo binding of the D2/D3 antagonist [3H]raclopride to the limbic system (ID50 = 17 mg/kg) in comparison to the striatum (ID50 = 44 mg/kg) of the rat, increases striatal and limbic tissue 3,4-dihydroxyphenylacetic acid levels with similar potency and efficacy, and preferentially increases extracellular 3,4-dihydroxyphenylacetic acid levels in the nucleus accumbens when compared to the striatum [1]. Clinical indications: Schizophrenia; Bipolar disorder; Dysthymia; FDA Approved Date: February 2002Toxicity: Insomnia; Hypersalivation; Hyperprolactinaemia; Nausea; Vomiting [2]
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Seoul National University Hospital
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Schizophrenia
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University of Zurich
Addiction
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Technische Universität München
Schizophrenia-Schizoaffective Disorder-Schizophreniform Disorder
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University of Cologne
Schizophrenia
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Phase 2
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Chonbuk National University Hospital
Normal Volunteers
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Taipei Veterans General Hospital, Taiwan-National Science Council, Taiwan
Tardive Dyskinesia-Neurocognitive Function
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Phase 4
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Rene Kahn-King's College London-Technische Universität München-University of Manchester-Ludwig-Maximilians - University of Munich-UMC Utrecht
Schizophrenia-Schizophreniform Disorder-Schizoaffective Disorder
May 2011
Phase 4
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Central Institute of Mental Health, Mannheim-University of Cologne
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Phase 1
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Merck Sharp & Dohme Corp.
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Technische Universität München
Schizophrenia-Schizophrenia and Disorders With Psychotic Features-Schizoaffective Disorders
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Dementia-Depression-Schizophrenia-Psychosomatic Disorders-Anxiety Disorders
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CHA University-Handok Pharmaceuticals Co., Ltd.
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January 2014
Phase 4
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Phase 4
NCT01615185
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Phase 4
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Imperial College London-University of Manchester-University College, London
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Phase 4
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