"目录号: HY-14546
GPCR/G ProteinNeuronal Signaling-
Aripiprazole(Abilify)是人5-HT1A受体部分激动剂，Ki为4.2 nM。
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生物活性
Description
Aripiprazole(Abilify) is a human 5-HT1A receptor partial agonist with a Ki of 4.2 nM. IC50 Value: 4.2 nM(Ki)Target: 5-HT ReceptorAripiprazole is an atypical antipsychotic medication used for the treatment of schizophrenia. It has also recently received FDA approval for the treatment of acute manic and mixed episodes associated with bipolar disorder. Aripiprazole appears to mediate its antipsychotic effects primarily by partial agonism at the D2 receptor. In addition to partial agonist activity at the D2 receptor, aripiprazole is also a partial agonist at the 5-HT1A receptor, and like the other atypical antipsychotics, aripiprazole displays an antagonist profile at the 5-HT2A receptor. Aripiprazole has moderate affinity for histamine and alpha adrenergic receptors, and no appreciable affinity for cholinergic muscarinic receptors.
Clinical Trial
University of Medicine and Dentistry of New Jersey-Rutgers, The State University of New Jersey
Autism
May 2006
Otsuka Pharmaceutical Development & Commercialization, Inc.
Schizophrenia
April 2006
Phase 3
University Hospital Freiburg
Therapy-resistant Depression
June 2005
Phase 3
Otsuka Beijing Research Institute
Schizophrenia
May 31, 2017
Phase 3
CMG Pharmaceutical Co. Ltd
Schizophrenia
October 2015
Phase 1
San Francisco Department of Public Health-National Institute on Drug Abuse (NIDA)
Substance Abuse-HIV Infections
March 2009
Phase 2
Stanford University
Trichotillomania
July 2009
Otsuka Pharmaceutical Development & Commercialization, Inc.
Tourette's Disorder-Tic Disorder
January 2013
Phase 3
University of Maryland
Hyperprolactinemia
January 2011
University of Iowa-Bristol-Myers Squibb
Conduct Disorder
November 17, 2004
Phase 4
Indiana University School of Medicine-Bristol-Myers Squibb-Indiana University
Asperger's Disorder-Pervasive Developmental Disorder
January 2005
Phase 2
Yoo-Sook Joung-Korea Otsuka International Asia Arab-Samsung Medical Center
Autism
February 2014
Phase 4
Jamaica Hospital Medical Center-Bristol-Myers Squibb-Department of Psychiatry, Jamaica Hospital Medical Center-Research Division
Schizophrenia OCD-Obsessive Compulsive Disorder
March 2005
St. Luke's-Roosevelt Hospital Center-Bristol-Myers Squibb
Depressive Disorder, Major
March 2005
Phase 4
Drexel University College of Medicine-Drexel University
Autism
February 2004
Phase 2
Cambridge Health Alliance-Bristol-Myers Squibb
Autism-Asperger's Disorder-Pervasive Developmental Disorder
February 2006
Phase 2
Massachusetts General Hospital-Bristol-Myers Squibb
Psychotic Depression
June 2003
Phase 3
Otsuka Pharmaceutical Development & Commercialization, Inc.
Schizophrenia
July 2008
Phase 3
University of Malaya
Schizophrenia
May 2009
Phase 4
Otsuka Pharmaceutical Development & Commercialization, Inc.
Tourette's Disorder
August 2011
Phase 3
Indiana University School of Medicine-Indiana University
Fragile X Syndrome
April 2007
Phase 2
Abdi ?brahim Otsuka
Schizophrenia
April 2016
Phase 4
Otsuka Pharmaceutical Development & Commercialization, Inc.
Schizophrenia
July 2004
Phase 3
Otsuka Pharmaceutical Development & Commercialization, Inc.
Schizophrenia
January 2012
Phase 1
University of Texas Southwestern Medical Center-Bristol-Myers Squibb
Major Depressive Disorder
October 2005
Phase 4
Otsuka Pharmaceutical Development & Commercialization, Inc.
Schizophrenia
January 2012
Phase 3
University Hospitals Cleveland Medical Center-Bristol-Myers Squibb
Bipolar Disorder
April 2004
Phase 4
University of Pittsburgh-Bristol-Myers Squibb
Bipolar Disorder-Metabolic Syndrome
April 2008
Otsuka Pharmaceutical Development & Commercialization, Inc.
Schizophrenia
April 1998
Phase 3
Lawson Health Research Institute-Bristol-Myers Squibb
Postpartum Depression
June 2011
Phase 3
University of North Carolina, Chapel Hill-Bristol-Myers Squibb
Autistic Disorder-Asperger Syndrome-Autism Spectrum Disorder
January 2006
Phase 2
Seoul National University Hospital-Otsuka Pharmaceutical Co., Ltd.
Major Depressive Disorder
February 2012
Phase 4
Otsuka Pharmaceutical Development & Commercialization, Inc.
Healthy
August 2006
Phase 1
Otsuka Pharmaceutical Co., Ltd.
Schizophrenia
August 2010
Phase 3
National Taiwan University Hospital-National Science Council, Taiwan-Taoyuan Psychiatric Center, Ministry of Health and Welfare, Executive Yuan, R.O.C. Taiwan
DSM-IV Schizophrenia-Schizoaffective Disorder
August 2007
Phase 4
Pfizer
Pharmacokinetics-Cytochrome P-450 CYP2D6-CYP3A4 Protein, Human
August 2010
Phase 4
Otsuka Pharmaceutical Development & Commercialization, Inc.
Healthy
August 2006
Phase 1
Otsuka Pharmaceutical Development & Commercialization, Inc.-Covance
Schizophrenia
December 2008
Phase 3
Otsuka Pharmaceutical Development & Commercialization, Inc.
Schizophrenia
November 2007
Phase 1
University Hospitals Cleveland Medical Center-Bristol-Myers Squibb
Bipolar Disorder
August 2004
Phase 3
University of Oxford-National Institute for Health Research, United Kingdom
Hyperprolactinemia
April 2010
Phase 4
Seoul National University Hospital-Korea Otsuka Pharmaceutical Co., Ltd.
Schizophrenia
December 2005
Phase 4
Veterans Medical Research Foundation-Bristol-Myers Squibb
Diabetes
March 2009
Phase 4
University of North Carolina, Chapel Hill-Duke University-National Institute of Mental Health (NIMH)
Autism Spectrum Disorder
August 2009
Phase 4
University of Texas Southwestern Medical Center
Bipolar Disorder-Alcoholism-Alcohol Abuse
November 2016
Phase 3
University of North Carolina, Chapel Hill-Bristol-Myers Squibb
Schizophrenia-Schizoaffective Disorder-Schizophreniform Disorder-Mood Disorders
August 2005
Phase 4
Institute of Mental Health, Singapore
Antipsychotics Weight Gain
August 2016
Phase 4
Otsuka Pharmaceutical Development & Commercialization, Inc.-Otsuka America Pharmaceutical
