Ziprasidone HCl

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

Ziprasidone HCl Chemical Structure

Molecular Weight(MW): 449.4

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

Size Price Stock Quantity  
In DMSO USD 90 In stock
USD 70 In stock
USD 170 In stock
USD 370 In stock
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Cited by 2 Publications

1 Customer Review

  • a, Quantification of sterol levels in OPCs (oligodendrocyte progenitor cells) treated with the indicated molecules at 2 μM.

    Nature, 2018, 560(7718):372-376. Ziprasidone HCl purchased from Selleck.

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Biological Activity

Description Ziprasidone HCl 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

Solubility (25°C)

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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 449.4
Formula

C21H21ClN4OS·HCl

CAS No. 122883-93-6
Storage powder
in solvent
Synonyms CP-88059

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03837860 Not yet recruiting Opioid Abuse Unspecified|Opioid Dependence The University of Texas Health Science Center at San Antonio March 31 2019 Early Phase 1
NCT03837860 Not yet recruiting Opioid Abuse Unspecified|Opioid Dependence The University of Texas Health Science Center at San Antonio March 31 2019 Early Phase 1
NCT03768726 Recruiting Bipolar Disorder Pfizer December 21 2018 Phase 3
NCT03781115 Recruiting Schizophrenia University of Arizona|Sidney R. Baer Jr. Foundation December 2018 Phase 1
NCT03768726 Recruiting Bipolar Disorder Pfizer December 21 2018 Phase 3
NCT03781115 Recruiting Schizophrenia University of Arizona|Sidney R. Baer Jr. Foundation December 2018 Phase 1

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