"目录号: HY-14542A
GPCR/G ProteinNeuronal Signaling-
Ziprasidone(CP88059)盐酸盐是5-HT和多巴胺受体拮抗剂，有抗精神病活性。
5-HT ReceptorDopamine Receptor
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生物活性
Description
Ziprasidone Hcl(CP-88059 Hcl) is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects of antipsychotic activity.Target: 5-HT receptor; Dopamine receptorZiprasidone (hydrochloride) is the salt form of ziprasidone, which possesses an in vitro 5-HT2A/dopamine D2 receptor affinity ratio higher than any clinically available antipsychotic agent. In vivo, ziprasidone antagonizes 5-HT2A receptor-induced head twitch with 6-fold higher potency than for blockade of d-amphetamine-induced hyperactivity, a measure of central dopamine D2 receptor antagonism. Ziprasidone also has high affinity for the 5-HT1A, 5-HT1D and 5-HT2C receptor subtypes, which may further enhance its therapeutic potential [1]. Ziprasidone sulfoxide and sulfone were the major metabolites in human serum. The affinities of the sulfoxide and sulfone metabolites for 5-HT2 and D2 receptors are low with respect to ziprasidone, and are thus unlikely to contribute to its antipsychotic effects [2]. Ziprasidone was associated with significant differential adverse effects relative to placebo in BPM, BPD, and schizophrenia with no significant difference in weight gain in all 3 groups. Self-reported somnolence was increased across the 3 conditions. Subjects with BPM were more vulnerable to EPS than those with BPD or schizophrenia [3].Clinical indications: Bipolar I disorder; Bipolar disorder; Mania; SchizophreniaFDA Approved Date: February 2001
Clinical Trial
Yang Fude-Pfizer-Beijing HuiLongGuan Hospital
Schizophrenia
October 2016
Phase 4
Dr. Reddy's Laboratories Limited
Healthy
November 2004
Phase 1
Dr. Reddy's Laboratories Limited
Healthy
November 2004
Phase 1
Soonchunhyang University Hospital-Pfizer
Schizophrenia-Schizoaffective Disorder
September 2010
Phase 4
Queen's University-Providence Health & Services-Pfizer-MDS Pharma Services
Depression, Bipolar
February 2009
Phase 4
Manhattan Psychiatric Center-Pfizer
Schizophrenia-Schizoaffective Disorder
September 2003
Phase 2-Phase 3
Massachusetts General Hospital-Cambridge Health Alliance-University of Connecticut-Vanderbilt University-Psychiatric Medicine Associates, L.L.C.-Cedars-Sinai Medical Center
Major Depressive Disorder
March 2008
Phase 2
University of Malaya
Schizophrenia
May 2009
Phase 4
Pfizer
Bipolar Disorder
July 2010
Phase 3
University of Texas Southwestern Medical Center-Stanley Medical Research Institute-Pfizer-Children's Medical Center Dallas
Bipolar Disorder
February 2007
Phase 4
Pfizer
Schizophrenia
October 2007
The University of Texas Health Science Center at San Antonio
Schizophrenia-Schizoaffective Disorder-Bipolar Disorder
August 2007
Massachusetts General Hospital-Pfizer
Generalized Anxiety Disorder-Bipolar Disorder
February 2006
Phase 4
Donald C. Goff, MD-Pfizer-Massachusetts General Hospital
Schizophrenia
January 2006
Phase 3
Pfizer
Schizophrenia and Disorders With Psychotic Features
December 2008
Phase 4
Drexel University College of Medicine-Drexel University
Autism
February 2002
Phase 2
University Hospitals Cleveland Medical Center-Pfizer
Medication Adherence-Bipolar Disorder
January 2011
Phase 4
Pfizer
Schizoaffective Disorder-Schizophrenia
December 2003
Phase 4
Pfizer
Schizophrenia-Bipolar Disorder-Schizoaffective Disorder
December 2003
Phase 2
University of North Carolina, Chapel Hill-Pfizer-National Institute of Mental Health (NIMH)
Schizophrenia
December 2002
Phase 2
The Medical Research Network-Liebowitz, Michael R., M.D.-Pfizer
Bipolar II Disorder-Major Depressive Episode
February 2005
Phase 4
Bronx Psychiatric Center-Pfizer-Buffalo Psychiatric Center-Rochester Psychiatric Center
Schizophrenia-Schizoaffective Disorder
May 2005
Phase 4
Tufts Medical Center-Duke University-University of South Carolina
Depression-Bipolar Disorder
February 2010
Phase 4
Stanford University-Pfizer
Bipolar Disorder
January 2007
Phase 4
Pfizer
Affective Psychosis, Bipolar-Mania-Manic-Depressive Psychosis
April 2007
Pfizer
Schizophrenia
March 2002
Phase 3
Pfizer
Bipolar Disorder-Depression, Bipolar
October 2007
Phase 3
Northwell Health
Schizophrenia
June 2002
Pfizer
Schizophrenia-Schizoaffective Disorder
November 2006
Phase 4
New York State Psychiatric Institute-Pfizer
Schizophreniform Disorder-Schizoaffective Disorder-Psychosis-Depressive Disorder, Major-Bipolar Disorder
May 2006
Phase 3
Duke University-Pfizer
Social Anxiety Disorder
November 2004
Phase 2
Pfizer
Bipolar Mania-Bipolar Disorder
December 2005
Phase 3
Pfizer
Schizophrenia-Schizoaffective Disorder
September 2004
Phase 3
Pfizer
Pyschotic Disorders
August 2003
Phase 4
Pfizer
Schizophrenia-Schizoaffective Disorder
October 2003
Phase 4
Pfizer
Schizophrenia-Mania-Delusional Disorder-Acute Exacerbation of Psychosis
July 2003
Phase 4
Creighton University-Pfizer
Posttraumatic Stress Disorder-Post-Traumatic Stress Disorder-PTSD
December 2002
Phase 4
Pfizer
Schizophrenia
September 2008
Phase 3
Pfizer
Schizophrenia
June 2006
Phase 3
Pfizer
Bipolar Disorder
July 2010
Phase 3
University Hospital Freiburg-Pfizer
Conduct Disorder-Oppositional Defiant Disorder
July 2006
Phase 2
Massachusetts General Hospital-University of Alabama at Birmingham
Major Depressive Disorder
July 2008
Phase 2
Fundació Institut de Recerca de l'Hospital de la Santa Creu i Sant Pau-Ministry of Health, Spain-REM-TAP Network-Pfizer
Borderline Personality Disorder
March 2004
Phase 2
Pfizer
Bipolar Disorder-Schizophrenia
June 2005
Yale University
Psychosis Prodrome
March 2008
Phase 2
VA Palo Alto Health Care System-Pfizer-University of South Florida-Lindner Center of HOPE
Bipolar Disorder-Panic Disorder-Generalized Anxiety Disorder
April 2010
Phase 4
Pfizer
Schizophrenia
April 2006
Phase 3
Pfizer
Acute Ma
