Ziprasidone (marketed as Geodon, Zeldox and Zipwell) was the fifth atypical antipsychotic to gain approval (February 2001) in the United States.
CAT No: 10-101-129
CAS No:146939-27-7 (net), 138982-67-9 (hydrochloride monohydrate)
Synonyms/Alias:CP-88059; 5-(2-(4-(1,2-Benzisothiazol-3-yl)piperazinyl)ethyl)-6-chlorooxindole · HCl · H2O
Ziprasidone Hydrochloride Monohydrate is a synthetic small-molecule compound classified as a benzisothiazolylpiperazine derivative, widely recognized for its role as a potent antagonist at dopamine D2 and serotonin 5-HT2A receptors. Its distinct pharmacological profile, including high affinity for multiple neurotransmitter receptors, makes it a valuable tool in neuropharmacological research and receptor-binding studies. Researchers utilize this compound to investigate central nervous system pathways, neurotransmitter regulation, and molecular mechanisms underlying neuropsychiatric conditions. Its well-characterized receptor interactions and physicochemical stability further support its relevance in experimental and analytical applications across neuroscience and pharmacology.
Receptor Binding Studies: Ziprasidone Hydrochloride Monohydrate is extensively used in receptor binding assays to elucidate the affinity and selectivity of ligands for dopamine and serotonin receptors. Its established binding characteristics provide a reliable reference for competitive binding experiments, allowing researchers to benchmark new compounds or investigate receptor-ligand interactions in various tissue preparations and cell-based systems. These studies are critical for mapping receptor pharmacology and characterizing the functional consequences of receptor modulation.
Neurotransmitter Pathway Analysis: The compound is instrumental in probing the functional dynamics of dopaminergic and serotonergic signaling pathways. By serving as a selective antagonist in in vitro and ex vivo models, it enables the dissection of neurotransmitter-mediated responses and the identification of downstream molecular targets. This application is particularly valuable in exploring the mechanisms of neurotransmitter release, receptor cross-talk, and synaptic plasticity, contributing to a deeper understanding of neural circuit regulation.
Pharmacodynamic Profiling: In preclinical research, Ziprasidone Hydrochloride Monohydrate is employed to assess the pharmacodynamic properties of novel neuroactive agents. It is frequently included in comparative studies designed to evaluate the efficacy, potency, and receptor specificity of new chemical entities. By providing a well-characterized reference point, it supports the development of structure-activity relationships and informs the optimization of lead compounds targeting central nervous system receptors.
Analytical Method Development: The compound serves as a standard or control in the development and validation of analytical methods, such as high-performance liquid chromatography (HPLC) and mass spectrometry protocols. Its defined chemical structure and stability make it suitable for calibration, quantitation, and quality control in the analysis of complex biological matrices. This application is essential for ensuring the accuracy and reproducibility of quantitative assays in pharmaceutical and biochemical laboratories.
Neurotoxicity and Safety Assessment: Researchers utilize Ziprasidone Hydrochloride Monohydrate in experimental models to evaluate potential neurotoxic effects and off-target interactions of investigational compounds. By incorporating it into toxicity screening protocols, scientists can identify adverse cellular responses, assess receptor-mediated cytotoxicity, and characterize the safety profiles of candidate molecules. These studies facilitate risk assessment and guide the refinement of experimental compounds prior to further development.
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.
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