Marrubenol interacts with the phenylalkylamine binding site of the L-type calcium channel |
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Authors: | El Bardai Sanae Hamaide Marie-Christine Lyoussi Badiaa Quetin-Leclercq Joëlle Morel Nicole Wibo Maurice |
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Institution: | Laboratoire de Pharmacologie, Université Catholique de Louvain, UCL 5410, Avenue Hippocrate, 54, B-1200 Brussels, Belgium. |
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Abstract: | Marrubenol inhibits contraction of rat arteries by blocking L-type calcium (Ca(2+)) 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 (-)-(3)H]desmethoxyverapamil ((3)H]D888) with an apparent K(i) value of 16 microM (95% confidence interval: 6.5-39.5 microM). As marrubenol inhibited the contraction evoked by KCl depolarization of intestinal smooth muscle half-maximally at a concentration of approximately 12 microM, interaction with the phenylalkylamine binding site seems to account for the inhibition of L-type Ca(2+) channels by marrubenol. |
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