Ziprasidone HCl

Licensed by Pfizer Catalog No.S1444 Synonyms: CP-88059

For research use only.

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

CAS No. 122883-93-6

Selleck's Ziprasidone HCl has been cited by 5 Publications

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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

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 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]

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 90 mg/mL
(200.26 mM)
Water Insoluble
Ethanol Insoluble

Chemical Information

Molecular Weight 449.4
Formula

C21H21ClN4OS·HCl

CAS No. 122883-93-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CN(CCN1CCC2=C(C=C3C(=C2)CC(=O)N3)Cl)C4=NSC5=CC=CC=C54.Cl

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01245348 Completed Genetic: SULT4A1-1 genetic test Schizophrenia|Bipolar Disorder Medco Health Solutions Inc.|SureGene LLC December 2010 --
NCT01714011 Completed Drug: Ziprasidone|Drug: Aripiprazole Schizophrenia University of Malaya May 2009 Phase 4
NCT00835107 Completed Drug: ziprasidone hydrochloride|Drug: placebo Depression Bipolar Queen''s University|Providence Health & Services|Pfizer|MDS Pharma Services February 2009 Phase 4
NCT00676429 Completed Drug: Ziprasidone Hydrochloride|Drug: Placebo Conduct Disorder|Oppositional Defiant Disorder University Hospital Freiburg|Pfizer July 2006 Phase 2
NCT00148564 Completed Drug: olanzapine|Drug: Ziprasidone Schizophrenia Charite University Berlin Germany March 2004 Phase 4

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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.

Handling Instructions

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