Ziprasidone mesylate trihydrate (Synonyms: CP-88059 mesylate trihydrate)

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Ziprasidone (CP-88059) mesylate trihydrate is an orally active combined 5-HT and dopamine receptor antagonist. Ziprasidone mesylate trihydrate has affinities for Rat D₂ (K_i=4.8 nM), 5-HT_2A (K_i=0.42 nM) and 5-HT_1A (K_i=3.4 nM).

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Ziprasidone mesylate trihydrate Chemical Structure

CAS No. : 199191-69-0

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Other In-stock Forms of Ziprasidone mesylate trihydrate:

Ziprasidone Ziprasidone hydrochloride monohydrate

Other Forms of Ziprasidone mesylate trihydrate:

Ziprasidone In-stock
Ziprasidone hydrochloride monohydrate In-stock
Ziprasidone-d₈ Get quote
Ziprasidone hydrochloride Get quote
Ziprasidone mesylate Get quote

1 Publications Citing Use of MCE Ziprasidone mesylate trihydrate

•Research Square Preprint. 2021 Jul.

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Dopamine Receptor D₁ Receptor D₂ Receptor D₃ Receptor D₄ Receptor D₅ Receptor

Biological Activity
Purity & Documentation
References
Customer Review

Description

Ziprasidone (CP-88059) mesylate trihydrate is an orally active combined 5-HT and dopamine receptor antagonist^[1]. Ziprasidone mesylate trihydrate has affinities for Rat D₂ (K_i=4.8 nM), 5-HT_2A (K_i=0.42 nM) and 5-HT_1A (K_i=3.4 nM)^[1].

IC₅₀ & Target

Rat 5-HT₂ Receptor

0.42 nM (Ki)

Rat 5-HT_1A Receptor

3.4 nM (Ki)

Rat D₂ Receptor

4.8 nM (Ki)

In Vitro

Ziprasidone mesylate trihydrate (0-500 nM, 150 seconds) blocks wild-type hERG current^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

Cell Line:	HEK-293 cells^[2]
Concentration:	0-500 nM
Incubation Time:	150 seconds
Result:	Blocked wild-type hERG current in a voltage- and concentration-dependent manner (IC₅₀ = 120 nm).

In Vivo

Ziprasidone mesylate trihydrate (oral gavage; 20 mg/kg; once daily; 7 weeks) results in weight loss, low level physical activity, high resting energy expenditure and greater capacity for thermogenesis when subjected to cold^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Eight-week-old female Sprague-Dawley rats weighing 200 to 250 g^[3]
Dosage:	20 mg/kg
Administration:	Oral gavage; 20 mg/kg; once daily; 7 weeks
Result:	Gained significantly less weight (P = 0.031), had a lower level of physical activity (P = 0.016), showed a higher resting energy expenditure (P < 0.001), and displayed a greater capacity for thermogenesis when subjected to cold (P < 0.001).

Clinical Trial

Molecular Weight

563.09

Formula

C₂₂H₃₁ClN₄O₇S₂

CAS No.

199191-69-0

SMILES

O=S(C)(O)=O.ClC1=CC2=C(CC(N2)=O)C=C1CCN(CC3)CCN3C4=NSC5=C4C=CC=C5.O.O.O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. H Rollema, et al. 5-HT(1A) receptor activation contributes to ziprasidone-induced dopamine release in the rat prefrontal cortex. Biol Psychiatry. 2000 Aug 1;48(3):229-37. [Content Brief]

[2]. Zhi Su, et al. Block of hERG channel by ziprasidone: biophysical properties and molecular determinants. Biochem Pharmacol. 2006 Jan 12;71(3):278-86. [Content Brief]

[3]. Subin Park, et al. The effect of ziprasidone on body weight and energy expenditure in female rats. Metabolism. 2012 Jun;61(6):787-93. [Content Brief]

Ziprasidone mesylate trihydrate Related Classifications

Neurological Disease

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Ziprasidone mesylate199191-69-0CP-88059 mesylate5-HT ReceptorDopamine ReceptorSerotonin Receptor5-hydroxytryptamine Receptorantipsychotic agent5-HT receptorserotonindopamine receptorHEK-293Inhibitorinhibitorinhibit

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