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Ziprasidone

Catalog No. T0031L2 CAS 146939-27-7

Synonyms: Geodon, Zeldox, CP-88059

Ziprasidone (Geodon) is a united 5-HT (serotonin) and dopamine receptor antagonist which shows potent effects of antipsychotic activity.

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Ziprasidone, CAS 146939-27-7

Pack Size	Availability	Price/USD
10 mg	In stock	$ 65.00
25 mg	In stock	$ 102.00
50 mg	In stock	$ 164.00
100 mg	In stock	$ 213.00
1 mL * 10 mM (in DMSO)	In stock	$ 71.00

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Purity: 100%

Purity: 99.53%

Biological Description

Chemical Properties

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Description	Ziprasidone (Geodon) is a united 5-HT (serotonin) and dopamine receptor antagonist which shows potent effects of antipsychotic activity.
Targets&IC50	5-HT2A:0.42 nM (Ki), 5-HT1A receptor (human):2.5 nM (Ki), D2 receptor (rat):4.8 nM (Ki), 5-HT1A receptor (rat):3.4 nM (Ki)
In vitro	Ziprasidone demonstrates the ability to inhibit the significant increase in food intake induced by olanzapine in rats, indicating an intrinsic protective mechanism against drug-induced hyperphagia. Furthermore, Ziprasidone significantly enhances the immunoreactivity of NGF and ChAT in the dentate gyrus, CA1, and CA3 regions of the rat hippocampus. In anesthetized rats, Ziprasidone exhibits a dose-dependent reduction in the activity of midline thalamic neurons, similar to atypical antipsychotic drugs such as clozapine (ED50 = 250 mg/kg i.v.) and olanzapine (ED50 = 1000 mg/kg i.v.), with an ED50 value of 300 mg/kg i.v. Additionally, Ziprasidone has a relatively low blocking effect on the wild-type hERG current in Xenopus oocytes, with an IC50 of 2.8 mM.
In vivo	Ziprasidone selectively blocks wild-type hERG currents in stably transfected HEK-293 cells in a voltage and concentration-dependent manner with an IC(50) of 120nM. It demonstrates minimal torsadogenic risk as evidenced by minimal hERG current blockade during depolarized voltages (-20 or +30mV) or assessed via envelope of tails experiments at +30mV. Ziprasidone significantly prolongs the deactivation time constant of hERG currents at -50mV. It acts as a 5-HT(1A) receptor agonist and antagonizes 5-HT(2A), 5-HT(2C), and 5-HT(1B/1D) receptors. The compound's potency in inhibiting neuronal uptake of 5-HT and norepinephrine is similar to that of the antidepressant imipramine. Ziprasidone also exhibits high affinity for human 5-HT receptors and human dopamine D(2) receptors.

Synonyms	Geodon, Zeldox, CP-88059
Molecular Weight	412.94
Formula	C21H21ClN4OS
CAS No.	146939-27-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 13.5 mg/mL (32.69 mM), Sonication is recommended.

References and Literature

1. Seeger TF, et al. J Pharmacol Exp Ther. 1995 Oct;275(1):101-13.

Citations

1. Xu Z, Guo L, Yu J, et al.Ligand recognition and G protein coupling of trace amine receptor TAAR1.Nature.2023: 1-3.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Anti-Cancer Drug Library Inhibitor Library Membrane Protein-targeted Compound Library Anti-Cancer Approved Drug Library GPCR Compound Library Anti-Neurodegenerative Disease Compound Library FDA-Approved Drug Library Preclinical Compound Library

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Related compounds with same targets

PF2562 Acetophenazine dimaleate lumateperone Tosylate Dasotraline hydrochloride L-741626 Tiaspirone hydrochloride Brexpiprazole L-745870

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Keywords

Ziprasidone 146939-27-7 GPCR/G Protein Immunology/Inflammation Neuroscience 5-HT Receptor Dopamine Receptor Adrenergic Receptor Histamine Receptor Norepinephrine 5-hydroxytryptamine Receptor antipsychotic agent CP88059 Serotonin Receptor serotonin Geodon HEK-293 Zeldox inhibit CP 88059 CP-88059 Inhibitor inhibitor

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