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Cicloprolol hydrochloride

Cat. No. M22109
Cicloprolol hydrochloride Structure
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Biological Activity

Cicloprolol hydrochloride

Chemical Information
Molecular Weight 359.89
Formula C18H30ClNO4
CAS Number 63686-79-3
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] P M McCaffrey, et al. Eur J Clin Pharmacol. Studies of the agonist and antagonist activity of cicloprolol in man

[2] P E Hicks, et al. J Pharmacol Exp Ther. Comparative analysis of beta-1 adrenoceptor agonist and antagonist potency and selectivity of cicloprolol, xamoterol and pindolol

[3] S Weber, et al. Br J Clin Pharmacol. Pharmacodynamic without pharmacokinetic interaction between cicloprolol, a partial beta 1-adrenoceptor agonist, and digoxin in healthy subjects

[4] L Bonandi, et al. Cardiovasc Drugs Ther. Combined invasive and noninvasive study of left ventricular systolic and diastolic function following acute administration of cicloprolol to subjects with normal cardiac function

[5] G Cocco, et al. Clin Cardiol. An evaluation of the safety of the beta-modulator cicloprolol in chronic heart failure

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