Ziprasidone hydrochloride

"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

NCT02935998

Yang Fude-Pfizer-Beijing HuiLongGuan Hospital

Schizophrenia

October 2016

Phase 4

NCT01581866

Dr. Reddy's Laboratories Limited

Healthy

November 2004

Phase 1

NCT01581879

Dr. Reddy's Laboratories Limited

Healthy

November 2004

Phase 1

NCT01198353

Soonchunhyang University Hospital-Pfizer

Schizophrenia-Schizoaffective Disorder

September 2010

Phase 4

NCT00835107

Queen's University-Providence Health & Services-Pfizer-MDS Pharma Services

Depression, Bipolar

February 2009

Phase 4

NCT00395031

Manhattan Psychiatric Center-Pfizer

Schizophrenia-Schizoaffective Disorder

September 2003

Phase 2-Phase 3

NCT00555997

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

NCT01714011

University of Malaya

Schizophrenia

May 2009

Phase 4

NCT01113541

Pfizer

Bipolar Disorder

July 2010

Phase 3

NCT00622739

University of Texas Southwestern Medical Center-Stanley Medical Research Institute-Pfizer-Children's Medical Center Dallas

Bipolar Disorder

February 2007

Phase 4

NCT00579670

Pfizer

Schizophrenia

October 2007

NCT00538642

The University of Texas Health Science Center at San Antonio

Schizophrenia-Schizoaffective Disorder-Bipolar Disorder

August 2007

NCT00374543

Massachusetts General Hospital-Pfizer

Generalized Anxiety Disorder-Bipolar Disorder

February 2006

Phase 4

NCT00403546

Donald C. Goff, MD-Pfizer-Massachusetts General Hospital

Schizophrenia

January 2006

Phase 3

NCT00748566

Pfizer

Schizophrenia and Disorders With Psychotic Features

December 2008

Phase 4

NCT00208559

Drexel University College of Medicine-Drexel University

Autism

February 2002

Phase 2

NCT01293825

University Hospitals Cleveland Medical Center-Pfizer

Medication Adherence-Bipolar Disorder

January 2011

Phase 4

NCT00649064

Pfizer

Schizoaffective Disorder-Schizophrenia

December 2003

Phase 4

NCT00650611

Pfizer

Schizophrenia-Bipolar Disorder-Schizoaffective Disorder

December 2003

Phase 2

NCT01006551

University of North Carolina, Chapel Hill-Pfizer-National Institute of Mental Health (NIMH)

Schizophrenia

December 2002

Phase 2

NCT00237666

The Medical Research Network-Liebowitz, Michael R., M.D.-Pfizer

Bipolar II Disorder-Major Depressive Episode

February 2005

Phase 4

NCT00458211

Bronx Psychiatric Center-Pfizer-Buffalo Psychiatric Center-Rochester Psychiatric Center

Schizophrenia-Schizoaffective Disorder

May 2005

Phase 4

NCT01168674

Tufts Medical Center-Duke University-University of South Carolina

Depression-Bipolar Disorder

February 2010

Phase 4

NCT00472641

Stanford University-Pfizer

Bipolar Disorder

January 2007

Phase 4

NCT00454883

Pfizer

Affective Psychosis, Bipolar-Mania-Manic-Depressive Psychosis

April 2007

NCT00139737

Pfizer

Schizophrenia

March 2002

Phase 3

NCT00483548

Pfizer

Bipolar Disorder-Depression, Bipolar

October 2007

Phase 3

NCT00225498

Northwell Health

Schizophrenia

June 2002

NCT00406315

Pfizer

Schizophrenia-Schizoaffective Disorder

November 2006

Phase 4

NCT00421954

New York State Psychiatric Institute-Pfizer

Schizophreniform Disorder-Schizoaffective Disorder-Psychosis-Depressive Disorder, Major-Bipolar Disorder

May 2006

Phase 3

NCT00215150

Duke University-Pfizer

Social Anxiety Disorder

November 2004

Phase 2

NCT00280566

Pfizer

Bipolar Mania-Bipolar Disorder

December 2005

Phase 3

NCT00645229

Pfizer

Schizophrenia-Schizoaffective Disorder

September 2004

Phase 3

NCT00645320

Pfizer

Pyschotic Disorders

August 2003

Phase 4

NCT00650429

Pfizer

Schizophrenia-Schizoaffective Disorder

October 2003

Phase 4

NCT00644800

Pfizer

Schizophrenia-Mania-Delusional Disorder-Acute Exacerbation of Psychosis

July 2003

Phase 4

NCT00208208

Creighton University-Pfizer

Posttraumatic Stress Disorder-Post-Traumatic Stress Disorder-PTSD

December 2002

Phase 4

NCT00723606

Pfizer

Schizophrenia

September 2008

Phase 3

NCT00265382

Pfizer

Schizophrenia

June 2006

Phase 3

NCT01124877

Pfizer

Bipolar Disorder

July 2010

Phase 3

NCT00676429

University Hospital Freiburg-Pfizer

Conduct Disorder-Oppositional Defiant Disorder

July 2006

Phase 2

NCT00633399

Massachusetts General Hospital-University of Alabama at Birmingham

Major Depressive Disorder

July 2008

Phase 2

NCT00635921

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

NCT01053429

Pfizer

Bipolar Disorder-Schizophrenia

June 2005

NCT00635700

Yale University

Psychosis Prodrome

March 2008

Phase 2

NCT01172652

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

NCT00257192

Pfizer

Schizophrenia

April 2006

Phase 3

NCT00329108

Pfizer

Acute Ma

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