Structural Components of β-Eudesmol Essential for Its Potentiating Effect on Succinylcholine-Induced Neuromuscular Blockade in Mice

Abstract

Eudesmol, a sesquiterpenoid alcohol isolated from Atractylodes lancea rhizoma, potentiates the neuromuscular blocking effect of succinylcholine (SuCh). The potentiating effect is greater in diabetic muscles than in normal ones. To identify the structural components ofβ-eudesmol contributing to this action, we examined the potentiating effect of newly synthesized tertiary alcohols related to β-eudesmol in phrenic nerve-diaphragm muscle preparations of normal and alloxan-diabetic mice. Potentiating effects were exhibited by cyclohexylidene derivatives but not by cyclohexanone or cyclohexanol derivatives. The compound 2-(3-hydroxy-3-methylbutyl)cyclohexylidene exhibited a potentiating effect, but 3-(3-hydroxy-3-methylbutyl)cyclohexylidene did not. These results indicate that both the presence of an exo-methylene attached to a cyclohexane ring and the distance between the exo-methylene and the hydroxy group in β-eudesmol are involved in the potentiating effect on SuCh-induced neuromuscular blockade. © 1994, The Pharmaceutical Society of Japan. All rights reserved.