Home Neuronal Signaling 5-HT Receptor antagonist - Dopamine Receptor antagonist Ziprasidone HCl For research use only.

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

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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 lnformation & 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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