Ziprasidone HCl

Synonyms: CP-88059

Ziprasidone HCl (CP-88059) is a novel and potent dopamine and serotonin (5-HT) receptor antagonist, used in the treatment of schizophrenia and bipolar disorder.

Ziprasidone HCl Chemical Structure

Ziprasidone HCl Chemical Structure

CAS: 122883-93-6

Selleck's Ziprasidone HCl has been cited by 5 Publications

1 Customer Review

Purity & Quality Control

Batch: S144401 DMSO] 90 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.01%
99.01

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Biological Activity

Description Ziprasidone HCl (CP-88059) is a novel and potent dopamine and serotonin (5-HT) receptor antagonist, used in the treatment of schizophrenia and bipolar disorder.
Targets
5-HT receptor [1] Dopamine receptor [1]
In vitro
In vitro Ziprasidone has high affinity for human 5-HT receptors and for human dopamine D(2) receptors. Ziprasidone is a 5-HT(1A) receptor agonist and an antagonist at 5-HT(2A), 5-HT(2C) and 5-HT(1B/1D) receptors. Ziprasidone inhibits neuronal uptake of 5-HT and norepinephrine comparable to the antidepressant imipramine. [1] Ziprasidone blocks wild-type hERG current in a voltage- and concentration-dependent manner with IC(50) of 120nM in stably transfected HEK-293 cells. Ziprasidone shows minimal tonic block of hERG current estimated during a depolarizing voltage (-20 or +30mV) or evaluated by the envelope of tails test (+30mV). Ziprasidone significantly increases the time constant of the slow component of hERG current deactivation (at -50mV). [2]
In Vivo
In vivo Ziprasidone exhibits less potent block of wild-type hERG current with IC(50) of 2.8 mM in Xenopus oocytes. [2] Ziprasidone suppresses the significant increases in food intake produced by olanzapine, indicating that it has an intrinsic protective mechanism against drug-induced increases in food intake in rats. [3] Ziprasidone results in a notable increase in NGF and ChAT immunoreactivity in the dentate gyrus (DG), CA1, and CA3 areas of the hippocampus of rats. [4] Ziprasidone dose-dependently slows raphe unit activity (ED50 = 300 mg/kg i.v.) as does the atypical antipsychotics clozapine (ED50 = 250 mg/kg i.v.) and olanzapine (ED50 = 1000 mg/kg i.v.) in anesthetized rats. [5]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01245348 Completed
Schizophrenia|Bipolar Disorder
Medco Health Solutions Inc.|SureGene LLC
December 2010 --
NCT01714011 Completed
Schizophrenia
University of Malaya
May 2009 Phase 4
NCT00835107 Completed
Depression Bipolar
Queen''s University|Providence Health & Services|Pfizer|MDS Pharma Services
February 2009 Phase 4
NCT00676429 Completed
Conduct Disorder|Oppositional Defiant Disorder
University Hospital Freiburg|Pfizer
July 2006 Phase 2
NCT00148564 Completed
Schizophrenia
Charite University Berlin Germany
March 2004 Phase 4

Chemical Information & Solubility

Molecular Weight 449.4 Formula

C21H21ClN4OS·HCl

CAS No. 122883-93-6 SDF Download Ziprasidone HCl SDF
Smiles C1CN(CCN1CCC2=C(C=C3C(=C2)CC(=O)N3)Cl)C4=NSC5=CC=CC=C54.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 90 mg/mL ( (200.26 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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