PMID: 44326Dec 1, 1979

Antiarrhythmic activity of dextro- and levo-isomers of 5-methyl-8-(2-hydroxy-3-t-butylamino-propoxy) coumarin hydrocholoride (bucumolol), a beta-adrenergic blocking agent, on aconitine-induced atrial and ouabain-induced ventricular arrhythmias in dogs

Japanese Journal of Pharmacology
K NakayamaH Koike

Abstract

The beta-blocking, antiarrhythmic, and local anesthetic effects of the racemic mixture and optical isomers of bucumolol, 5-methyl-8-(2-hydroxy-3-t-butylamino-propoxy) coumarin hydrochloride, were studied in dogs, guinea-pigs and frogs. In blocking the positive chrontropic response to isoproterenol, the levo-isomer of bucumolol was about 40 times more potent in dogs, and 270 times in guinea-pigs than its dextro-isomer and twice as effective in both species as the racemic mixture. In frog sciatic nerves bucumolol was 1/10-1/15 as potent in local anesthetic action as propranolol on a weight basis. Dextro- and levo-isomers and racemic bucumolol neither elevated electrical threshold for propagated impulses nor prolonged the effective refractory period of the dog right atrium. The levo-isomer and racemic bucumolol were capable of suppressing aconitine-induced atrial arrhythmia, while the dextro-isomer was less effective. Both isomers and racemic bucumolol were capable of reversing ventricular arrhythmia caused by ouabain, but the effective dose of the levo-isomer was significantly less than that of the dextro-isomer. The results suggest that both specific beta-blocking activity and non-specific membrane action of bucumolol suppressed...Continue Reading

References

Related Concepts

Molecular Stereochemistry
Quinidex
Structure of Sciatic Nerve
Aconite
Left Ventricular Structure
Structure-Activity Relationship
Bucumolol
Cavia
Salientia
Coumarin

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