Marrubenol interacts with the phenylalkylamine binding site of the L-type calcium channel

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• 作者：El Bardai ; Sanae ; Hamaide ; Marie-Christine ; Lyoussi ; Badiaa ; Quetin-Leclercq ; Joë ; lle ; et. al.
• 关键词：Marrubenol ; Calcium antagonist ; L-type Ca²⁺ channel ; 1 ; 4-Dihydropyridine ; Phenylalkylamine
• 刊名：European Journal of Pharmacology
• 出版年：2004
• 出版时间：May 25, 2004
• 年：2004
• 卷：492
• 期：2-3
• 页码：269-272
• 全文大小：157 K

文摘

Marrubenol inhibits contraction of rat arteries by blocking L-type calcium (Ca²⁺) channels in smooth muscle cells, but its interaction with binding sites for calcium antagonists had never been investigated. Competition binding studies indicated that marrubenol was a weak inhibitor of 1,4-dihydropyridine binding in membranes isolated from rat intestinal smooth muscle but completely displaced specifically bound (−)-[³H]desmethoxyverapamil ([³H]D888) with an apparent K_i value of 16 μM (95 % confidence interval: 6.5–39.5 μM). As marrubenol inhibited the contraction evoked by KCl depolarization of intestinal smooth muscle half-maximally at a concentration of 12 μM, interaction with the phenylalkylamine binding site seems to account for the inhibition of L-type Ca²⁺ channels by marrubenol.