• T Ohta, S Ito, and A Ohga.
• Department of Pharmacology, Faculty of Veterinary Medicine, Hokkaido University, Sapporo, Japan.
• Eur. J. Pharmacol. 1990 Mar 13; 178 (1): 11-9.

AbstractThe effects of dantrolene on the sarcoplasmic reticulum and contractile machinery were examined in skinned skeletal muscles of guinea pigs. Dantrolene inhibited Ca-induced Ca2+ release at 38 degrees C. The inhibitory effect of dantrolene on Ca2+ release was greater in the presence of caffeine or adenine nucleotide than in their absence at low Ca2+ concentrations. Dantrolene suppressed the maximum rate of Ca-induced Ca2+ release but did not affect the sensitivity to Ca2+. At 20 degrees C, however, dantrolene did not inhibit Ca2+ release induced by any Ca2+ concentration, regardless of the presence and absence of caffeine, adenine nucleotide or Mg2+. Ca2+ uptake into the sarcoplasmic reticulum and the Ca2+ sensitivity of the contractile machinery were not affected by dantrolene at 38 degrees C and 20 degrees C. These results suggest that dantrolene is a selective inhibitor of the Ca-induced Ca2+ release mechanism at physiological temperatures without having an effect on the Ca2+ pump of the sarcoplasmic reticulum or on the contractile machinery of skeletal muscle.

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