Licensed by Pfizer Catalog No.S1444 Synonyms: CP-88059
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.
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|Description||Ziprasidone HCl is a novel and potent dopamine and serotonin (5-HT) receptor antagonist, used in the treatment of schizophrenia and bipolar disorder.|
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.  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). 
|In vivo||Ziprasidone exhibits less potent block of wild-type hERG current with IC(50) of 2.8 mM in Xenopus oocytes.  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.  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.  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. |
-  Schmidt AW, et al. Eur J Pharmacol, 2001, 425(3), 197-201.
-  Su Z, et al. Biochem Pharmacol, 2006, 71(3), 278-286.
-  Kirk SL, et al. Eur J Pharmacol, 2004, 505(1-3), 253-254.
|In vitro||DMSO||90 mg/mL (200.26 mM)|
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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|
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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