"目录号: HY-14545A
GPCR/G ProteinNeuronal Signaling-
Amisulpride(DAN 2163)盐酸盐是多巴胺拮抗剂，对D2和D3受体的Ki分别为2.8 nM和3.2 nM。
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生物活性
Description
Amisulpride Hcl(DAN 2163 Hcl) 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 hydrochloride 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 hydrochloride 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 hydrochloride 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. Amisulpride hydrochloride preferentially 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]
Clinical Trial
CHA University-Handok Pharmaceuticals Co., Ltd.
Schizophrenia-Schizophreniform Disorder
January 2014
Phase 4
Sanofi
Schizophrenia
November 2012
Phase 4
Kaohsiung Kai-Suan Psychiatric Hospital
Schizophrenia
January 2008
Phase 4
Imperial College London-University of Manchester-University College, London
Schizophrenia
September 2011
Phase 4
National Health Research Institutes, Taiwan
Treatment-resistant Schizophrenia
May 2006
Phase 4
Geha Mental Health Center
Schizophrenia-Treatment Resistant Disorders
October 2011
Sanofi
Schizophrenia
May 2005
Phase 4
Sanofi
Schizophrenia
June 2005
Phase 4
Heinrich-Heine University, Duesseldorf
Schizophrenia-Schizoaffective Disorder
June 2012
Phase 4
Sanofi
Schizophrenia
February 2004
Phase 4
Mclean Hospital-National Institute of Mental Health (NIMH)
Major Depressive Disorder (MDD)
February 2012
Central Institute of Mental Health, Mannheim-Sanofi
Schizophrenia-Diabetes-Insulin Resistance
May 2004
Sanofi
Bipolar Disorder
May 2004
Phase 2
Beersheva Mental Health Center-Tirat Carmel Mental Health Center
Clozapine-induced Hypersalivation
November 2008
Phase 3
Birte Glenthoj-Glostrup University Hospital, Copenhagen-Rigshospitalet, Denmark-Institute of Psychiatry, London-UMC Utrecht-Copenhagen Hospital Corporation-University of Copenhagen
Schizophrenia-Schizophreniform Disorder-Schizoaffective Disorder
May 2011
Mclean Hospital-National Institute of Mental Health (NIMH)-Massachusetts General Hospital
Major Depressive Disorder (MDD)-History of Childhood Sexual Abuse (CSA)
November 2012
Acacia Pharma Ltd
Healthy
November 2013
Phase 1
Sanofi
Schizophrenia
September 2008
Phase 4
National Taiwan University Hospital-Yu-Li Veterans Hospital-Yu-Li Hospital
Metabolic Syndrome X
November 2009
University of Cologne-German Federal Ministry of Education and Research-German Research Network On Schizophrenia-Sanofi-Synthelabo-Department of Psychiatry University of Bonn-Heinrich-Heine University, Duesseldorf-Ludwig-Maximilians - University of Munich
Schizophrenia-Psychoses
January 2001
Phase 4
University of Jena-Sanofi
Schizophrenia
January 2003
Phase 4
Sunovion
Schizophrenia
March 2014
Phase 1
GlaxoSmithKline
Obsessive-Compulsive Disorder
August 2006
Phase 1
Seoul National University Hospital
Schizophrenia
September 2016
Haukeland University Hospital-Helse Vest
Schizophrenia-Psychotic Disorders
October 2011
Phase 4
University of Copenhagen-Glostrup University Hospital, Copenhagen-Rigshospitalet, Denmark-Institute of Psychiatry, London-UMC Utrecht-Copenhagen Hospital Corporation
Schizophrenia
December 2008
University of Zurich
Addiction
February 2014
Technische Universität München
Schizophrenia-Schizoaffective Disorder-Schizophreniform Disorder
December 2009
University of Cologne
Schizophrenia
October 2002
Phase 2
Chonbuk National University Hospital
Normal Volunteers
March 2009
Taipei Veterans General Hospital, Taiwan-National Science Council, Taiwan
Tardive Dyskinesia-Neurocognitive Function
January 2003
Phase 4
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
Central Institute of Mental Health, Mannheim-University of Cologne
Schizophrenia
January 2013
Phase 1
Merck Sharp & Dohme Corp.
Bipolar Disorder
April 1, 2013
Technische Universität München
Schizophrenia-Schizophrenia and Disorders With Psychotic Features-Schizoaffective Disorders
November 2014
Phase 4
Hannover Medical School
Dementia-Depression-Schizophrenia-Psychosomatic Disorders-Anxiety Disorders
January 2015
Phase 3
CHA University-Handok Pharmaceuticals Co., Ltd.
Schizophrenia-Schizophreniform Disorder
January 2014
Phase 4
Sanofi
Schizophrenia
November 2012
Phase 4
Kaohsiung Kai-Suan Psychiatric Hospital
Schizophrenia
January 2008
Phase 4
Imperial College London-University of Manchester-University College, London
Schizophrenia
September 2011
Phase 4
National Health Research Institutes, Taiwan
Treatment-resistant Schizophrenia
May 2006
Phase 4
Geha Mental Health Center
Schizophrenia-Treatment Resistant Disorders
October 2011
Sanofi
Schizophrenia
May 2005
Phase 4
Sanofi
Schizophrenia
June 2005
Phase 4
Heinrich-Heine University, Duesseldorf
Schizophrenia-Schizoaffective Disorder
June 2012
Phase 4
Sanofi
Schizophrenia
February 2004
Phase 4
Mclean Hospital-National Institute of Mental Health (NIMH)
Major Depressive Disorder (MDD)
February 2012
