COMPARISON OF LOCAL ANESTHETIC ACTIVITIES BETWEEN OPTICAL ISOMERS OF cis-1-BENZOYLOXY-2-DIMETHYLAMINO-1, 2, 3, 4-TETRAHYDRONAPHTHALENE

概要

論文の詳細を見る
The optical isomers of cis-1-benzoyloxy-2-dimethylamino-1, 2, 3, 4-tetrahydronaphthalene (YAU-17) were compared for their local anesthetic activity, acute toxicity, spasmolytic activity, and partition coefficient between chloroform and phosphate buffer. 1-YAU-17 was more active than d-YAU-17 in blocking the conduction of action potentials in isolated frog sciatic nerves. The difference in local anesthetic activities between the optical isomers was further substantiated by <I>in vivo</I> tests for corneal anesthesia, intracutaneous anesthesia and sciatic nerve block in guinea-pigs. Similarly, the i.v. injection to mice revealed a higher toxicity for 1-YAU-17 as compared to its d-isomer. In these tests, the potency ratios of the enantiomers ranged from 2 to 4, and the racemate had an intermediate potency. On the contrary, no difference among the compounds was found in their liposolubility, partition coefficient, and spasmolytic activity examined with isolated guinea-pig ileum. These results indicate that the steric factors play an important role in the production of different local anesthetic activities between the optical isomers of YAU-17, and their local anesthetic potency tends to be correlated to their intravenous acute toxicity but not to their spasmolytic activity.
社団法人日本薬理学会の論文