Ziprasidone Hydrochloride Monohydrate

Supplier Creative Peptides
Product # 10-101-129
CAS # 138982-67-9
Pricing Inquire
LabelingTarget
  • 5-hydroxytryptamine Receptor;
  • Dopamine Receptor
Synonyms CP-88059; 5-(2-(4-(1,2-Benzisothiazol-3-yl)piperazinyl)ethyl)-6-chlorooxindole · HCl · H2O
MolecularFormula C21H21ClN4OS·ClH·H2O
MolecularWeight 467.42
Source Synthetic
Explanation Ziprasidone (marketed as Geodon, Zeldox and Zipwell) was the fifth atypical antipsychotic to gain approval (February 2001) in the United States.
Application Ziprasidone hydrochloride monohydrate is approved by the U.S. Food and Drug Administration (FDA) for the treatment of schizophrenia, acute mania and mixed states associated with bipolar disorder. Ziprasidone is also used off-label for depression, bipolar maintenance and PTSD.
Activity Antagonist
BiologicalActivity Ziprasidone (CP 88059) hydrochloride monohydrate, an antipsychotic agent, is an orally active combined 5-HT (serotonin) and dopamine receptor antagonist. Ziprasidone hydrochloride monohydrate has high affinity for rat (Ki: 3.4 nM)/human (2.5 nM) 5-HT1A receptors, 5-HT2A (0.42 nM), and dopamine D2 receptors (4.8 nM). Ziprasidone hydrochloride monohydrate is an inhibitor of norepinephrine reuptake.
Target 5-HT Receptor
Reference
  • In the current work the kinetics of dehydration of ziprasidone hydrochloride monohydrate was studied by nonisothermal thermogravimetry. Ziprasidone hydrochloride monohydrate was heated from 30 to 150° with a heating rate of 5° per min under nitrogen gas atmosphere and weight loss data were collected. Powder X-ray difraction was used to characterize the solid before and after dehydration. The well accepted Coats-Redfern model fitting approach was applied to the thermogravimetry data for the kinetic analysis. Thirteen solid state reaction models were studied; among them one-dimensional diffusion model was found to be the best fit model for this reaction with an excellent correlation 0.9994. The Arrhenius parameters, activation energy, and pre-exponential factor were determined, the values were found to be 28 k.cal/mol and 9.53×1013 sec-1, respectively.
  • Ravikiran, A., Arthanareeswari, M., Kamaraj, P., & Praveen, C. (2013). Nonisothermal kinetics analysis of the dehydration of ziprasidone hydrochloride monohydrate by thermogravimetry. Indian journal of pharmaceutical sciences, 75(3), 361.
  • The findings of this study indicate that mild-to-moderate impairment of renal function does not result in clinically significant alteration of ziprasidone pharmacokinetics and therefore does not necessitate dose adjustment.
  • Aweeka, F., Jayesekara, D., Horton, M., Swan, S., Lambrecht, L., Wilner, K. D., ... & Turncliff, R. Z. (2000). The pharmacokinetics of ziprasidone in subjects with normal and impaired renal function. British journal of clinical pharmacology, 49(S1), 27-33.
AreasOfInterest Neurological Disease
Functions
  • Potassium channel regulator activity;
  • Virus receptor activity
Disease
  • Mixed bipolar I disorder
  • Schizophrenia
  • Bipolar disorder in remission
Organism Human
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