European Journal of Pharmacology - Molecular Pharmacology Section p. 285 - 294 (1995)
Update date:2022-08-11
Topics:
Takahashi, Yukiko
Furukawa, Ken-Ichi
Ishibashi, Masami
Kozutsumi, Daisuke
Ishiyama, Haruaki
Kobayashi, Jun'ichi
Ohizumi, Yasushi
Bromoeudistomin D and 9-methyl-7-bromoeudistomin D which have a β-carboline skeleton are powerful Ca2+ releasers from skeletal muscle sarcoplasmic reticulum exhibiting caffeine-like properties. We examined the effects of bromoeudistomin D analogues on Ca2+-induced Ca2+ release from skeletal muscle sarcoplasmic reticulum. Among bromoeudistomin D analogues, the Ca2+-releasing activities of carboline derivatives were higher than those of carbazole derivatives, suggesting that a carboline skeleton is significantly important for the manifestation of Ca2+-releasing activity and Ca2+ sensitivity of Ca2+-induced Ca2+ release. On the contrary, the analogues which have a carbazole skeleton and bromine at C-6 inhibit both Ca2+- and caffeine-induced Ca2+ release. 9-Methyl-substitution of the analogue elevated its Ca2+-releasing activity. Moreover, there is a close correlation between the enhancement of [3H]ryanodine binding to sarcoplasmic reticulum by the analogues and the activation of Ca2+ release by them. Bromoeudistomin D analogues may provide valuable information about the structure-function relationship of the ryanodine receptor/Ca2+ release channels in skeletal muscle sarcoplasmic reticulum.
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