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 well-characterized heterocyclic compound belonging to the class of benzisothiazolyl piperazine derivatives, frequently utilized in biochemical and pharmacological research. As a water-soluble salt form, it is particularly valued for its stability and ease of handling in laboratory settings. Researchers are drawn to its unique molecular structure, which enables interactions with multiple neurotransmitter systems. The compound's physicochemical properties make it an excellent candidate for diverse in vitro and in vivo experimental models, facilitating the exploration of receptor binding, cellular signaling, and metabolic pathways. Its versatility and established research background have positioned it as a staple in neuropharmacological investigations and beyond.
Receptor Binding Studies: Ziprasidone Hydrochloride Monohydrate is extensively employed in receptor binding assays to elucidate the affinity and selectivity of ligands for various neurotransmitter receptors, particularly dopamine and serotonin subtypes. By incorporating this compound into radioligand binding experiments, scientists can dissect its interaction profile, providing critical data for understanding receptor modulation. Such studies are fundamental for mapping neurotransmitter pathways and for the development of novel molecules with targeted central nervous system activity. The compound's high specificity aids in distinguishing between receptor subtypes, thereby enhancing the precision of pharmacological profiling.
Neurotransmitter Pathway Analysis: In neurochemical research, Ziprasidone HCl Monohydrate serves as a valuable tool for dissecting the effects of neurotransmitter modulation on neuronal signaling. Its ability to influence dopaminergic and serotonergic transmission makes it suitable for use in cellular models and brain slice preparations, where researchers can monitor downstream effects such as changes in second messenger systems, gene expression, and synaptic plasticity. By leveraging its pharmacological action, scientists gain insight into the complex regulation of mood, cognition, and behavior at the molecular level.
Behavioral Pharmacology: The compound is widely used in animal behavioral studies designed to investigate the effects of neuroactive agents on mood, anxiety, and cognitive functions. By administering Ziprasidone Hydrochloride Monohydrate to animal models, researchers can assess alterations in locomotor activity, social interaction, and learning paradigms. These experiments are instrumental in identifying the behavioral correlates of neurotransmitter modulation and in evaluating the efficacy of potential neuropsychiatric therapies. The reproducibility and reliability of results obtained with this compound make it a preferred choice for preclinical behavioral research.
Metabolic and Pharmacokinetic Investigations: Scientists utilize Ziprasidone Hydrochloride Monohydrate in metabolic stability and pharmacokinetic studies to characterize its absorption, distribution, metabolism, and excretion profiles in biological systems. By tracing its biotransformation and quantifying its metabolites, researchers can delineate the enzymatic pathways involved and predict potential drug-drug interactions. These investigations are crucial for optimizing dosing regimens in experimental models and for understanding the compound's systemic behavior under various physiological conditions.
Drug Discovery and Screening Platforms: In early-stage drug discovery, Ziprasidone Hydrochloride Monohydrate is incorporated into high-throughput screening assays aimed at identifying novel modulators of neurotransmitter receptors. Its well-defined pharmacological profile provides a benchmark for comparative analysis, enabling the selection of promising lead compounds. Furthermore, its use in structure-activity relationship studies informs the rational design of next-generation molecules with improved efficacy and safety profiles. By serving as a reference compound, it accelerates the iterative optimization of candidate drugs and supports the advancement of neuropharmacological research pipelines.
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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