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Cloperastine hydrochloride

Cat. No. M20495
Cloperastine hydrochloride Structure
Synonym:

HT-11 hydrochloride

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Quality Control & Documentation
Biological Activity

Cloperastine is a drug with a central antitussive effect, and is also endowed with an antihistaminic activity.

Chemical Information
Molecular Weight 366.32
Formula C20H25Cl2NO
CAS Number 14984-68-0
Solubility (25°C) DMSO 73 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Hong-Yu Luo, et al. Drugs R D. Pharmacokinetics, Bioequivalence and Safety of Cloperastine in Chinese Healthy Subjects Under Fasting and Postprandial Conditions

[2] He-Ying Liu, et al. J Pharm Biomed Anal. Identification and quantification of five impurities in cloperastine hydrochloride

[3] Carlo Civardi, et al. Neurol Sci. Induced hemichorea by cloperastine overuse

[4] Akira Takahara, et al. J Pharmacol Sci. Effects of the antitussive drug cloperastine on ventricular repolarization in halothane-anesthetized guinea pigs

[5] Fumio Soeda, et al. Environ Toxicol. Cloperastine rescues impairment of passive avoidance response in mice prenatally exposed to diethylstilbestrol

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