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Antagonism by beta-eudesmol of neostigmine-induced neuromuscular failure in mouse diaphragms.

Abstract
beta-Eudesmol, a sesquiterpenol extracted from a Chinese herb, Atractylodes lancea, at 10-80 microM, did not affect muscle action potentials, miniature and evoked endplate potentials and acetylcholine-induced depolarization in the presence or absence of neostigmine in mouse phrenic nerve-diaphragms. However, the tetanic fade, muscle fasciculation and twitch potentiation induced by neostigmine were effectively antagonized by 20 microM beta-eudesmol. When trains of pulses were applied to the nerve in the presence of neostigmine, beta-eudesmol reduced the incidence of explosive depolarization of the endplate from 95% to 35-67% of junctions, and shortened the duration when it occurred. Moreover, both the maximal and steady-state depolarizations during repetitive stimulation were reduced while the amplitudes of steady-state endplate potentials were increased. The results suggest that beta-eudesmol antagonized neostigmine-induced neuromuscular failure mainly by a presynaptic action to depress the regenerative release of acetylcholine during repetitive stimulation. The mechanism of antagonism is obviously not tubocurarine-like and it is unrelated to desensitization of acetylcholine channels.
AuthorsL C Chiou, C C Chang
JournalEuropean journal of pharmacology (Eur J Pharmacol) Vol. 216 Issue 2 Pg. 199-206 (Jun 05 1992) ISSN: 0014-2999 [Print] Netherlands
PMID1397007 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Drugs, Chinese Herbal
  • Neuromuscular Blocking Agents
  • Sesquiterpenes, Eudesmane
  • Terpenes
  • Neostigmine
  • beta-eudesmol
  • Acetylcholine
Topics
  • Acetylcholine (pharmacology)
  • Action Potentials (drug effects)
  • Animals
  • Diaphragm (drug effects, innervation)
  • Drug Interactions
  • Drugs, Chinese Herbal (pharmacology)
  • Electric Stimulation
  • Female
  • Male
  • Mice
  • Mice, Inbred ICR
  • Muscle Contraction (drug effects)
  • Neostigmine (pharmacology)
  • Neuromuscular Blocking Agents (pharmacology)
  • Sesquiterpenes, Eudesmane
  • Terpenes (pharmacology)

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