Ziprasidone hydrochloride monohydrate

SKU: orb1226385

Description

A full antagonist of D2 and 5-HT2A receptors with Ki of 6.8 and 0.6 nM, respectively; also is a partial agonist of 5-HT1A, and a partial antagonist of 5-HT2C and 5-HT1D receptors; exhibits potent antipsychotic activity in vivo.Schizophrenia Approved(In Vitro):Ziprasidone hydrochloride monohydrate (0-500 nM, 150 seconds) blocks wild-type hERG current.(In Vivo):Ziprasidone hydrochloride monohydrate (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.

Key Properties

• CAS Number: 138982-67-9
• MW: 467.4119
• Purity: >98% (HPLC)
• Formula: C₂₁H₂₄Cl₂N₄O₂S
• SMILES: O=C1CC2=CC(CCN3CCN(C4=NSC5=C4C=CC=C5)CC3)=C(Cl)C=C2N1.Cl.O
• Target: 5-HT Receptor
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  Ziprasidone hydrochloride monohydrate (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. Animal model: Eight-week-old female Sprague-Dawleyrats weighing 200 to 250 g. 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).
• In Vitro:
  Ziprasidone hydrochloride monohydrate (0-500 nM, 150 seconds) blocks wild-type hERG current. Cell Viability Assay Cell line: HEK-293 cells. Concentration: 0-500 nM. Incubation time: 150 seconds. Result: Blocked wild-type hERG current in a voltage- and concentration-dependent manner (IC50 = 120 nm).

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CP-88059

Quick Database Links

Gene Symbol

5-HT Receptor