Detail of "66778-36-7"

Reference

Influence of genetic polymorphism on the metabolism and disposition of encainide in man

Influence of genetic polymorphism on the metabolism and disposition of encainide in man. Wang, T.; Roden, D. M.; Wolfenden, H. T.; Woosley, R. L.; Wood, A. J. J.; Wilkinson, G. R.There are some reagents with their cas registry numbers 81329-70-6 and 87085-10-7 are used in this study. (Dep. Med., Vanderbilt Univ., Nashville, TN, USA). J. Pharmacol. Exp. Ther., 228(3), 605-11 (English) 1984. CODEN: JPETAB. ISSN: 0022-3565. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Encainide (I) [66778-36-7] metab. was studied in human volunteers. Approx. 10% of the subjects were found to be deficient metabolizers of I, producing different metabolites than did proficient metabolizers. Correlations with phenotypic variation in the metab. of other drugs are discussed, as is the clin. significance of defective I metab. .

Effect of encainide and its two major metabolites on cardiac conduction

Effect of encainide and its two major metabolites on cardiac conduction. Dresel, Peter E. (Dep. Pharmacol., Dalhousie Univ., Halifax, NS B3H 4H7, Can.). J. Pharmacol. Exp. Ther., 228(1), 180-6 (English) 1984. CODEN: JPETAB. ISSN: 0022-3565. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) The effect of encainide [66778-36-7] and its 2 major metabolites, MJ 9444 [81329-70-6] and MJ 14030 [81329-71-7] on cardiac conduction was studied by recording His bundle potentials in isolated perfused rabbit hearts and Purkinje and muscle conduction in vivo in dog hearts after destruction of the atrioventricular node. Both metabolites were 4 to 15 times more potent than encainide in slowing conduction through the atria, the AV-node and the His-Purkinje system of the rabbit heart. They did not differ from each other in potency but MJ 9444 increased the duration and decreased the height of the ventricular potential whereas MJ 14030 had no effect at doses which caused conduction block. In the dog, encainide (0.8-3.2 mg/kg, i.v.) slowed conduction of extrasystoles in both Purkinje and muscle at all coupling intervals, increased the effective refractory period and the functional refractory period of the Purkinje pathway. MJ 9444 (0.05-0.4 mg/kg) speeded Purkinje conduction of early (<300 ms) without affecting or while slowing conduction of late (>350 ms) extrasystoles. Higher doses (0.4-1.6 mg/kg) slowed conduction at all intervals. The effective refractory period and the functional refractory period were decreased but in some cases returned to control values at the higher doses. Muscle conduction was slowed at ￡0.4 mg/kg. MJ 14030 (0.05-3.2 mg/kg) had variable effects, behaving like MJ 9444 in 3 expts. but like the parent compd. in two others. Only slowing of conduction was seen with the 3 drugs when heart rate was changed. Thus, the 2 metabolites are more potent in both species, that low doses of MJ 9444 have properties like those reported previously for lidocaine whereas the effects of encainide resemble more closely those of quinidine. No reason for the variability of the effects of MJ 14030 is apparent.