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Bunitrolol

Cat. No. M41780
Bunitrolol Structure
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Biological Activity

Bunitrolol is a beta-adrenergic antagonist.

Chemical Information
Molecular Weight 248.32
Formula C14H20N2O2
CAS Number 34915-68-9
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] S Narimatsu et al. J Pharm Pharmacol. In-vitro metabolic interaction of bunitrolol enantiomers in rabbit liver microsomes

[2] K Chiba et al. J Pharm Sci. Effects of bunitrolol on ischemic myocardial energy metabolism in dogs

[3] S Narimatsu et al. Biol Pharm Bull. Involvement of a cytochrome P4502D subfamily in human liver microsomal bunitrolol 4-hydroxylation

[4] H Tsuchihashi et al. Jpn J Pharmacol. Effects of bunitrolol on adrenergic and serotonergic receptors

[5] H Tsuchihashi et al. Jpn J Pharmacol. Selectivity of bunitrolol for beta 1- and beta 2-adrenergic receptors and 5HT1B-receptors: assessment by biphasic Scatchard plots and biphasic displacement curve analysis with 125I-iodocyanopindolol and 3H-CGP12177

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