Marrubenol interacts with the phenylalkylamine binding site of the L-type calcium channel.
(2004) European Journal of Pharmacology — Vol. 492, n° 2-3, p. 269-272 (2004)
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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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El Bardai, S., Hamaide, M.-C., Lyoussi, B., Quetin-Leclercq, J., Morel, N., & Wibo, M. (2004). Marrubenol interacts with the phenylalkylamine binding site of the L-type calcium channel. European Journal of Pharmacology, 492(2-3), 269-272. https://doi.org/10.1016/j.ejphar.2004.04.007 (Original work published 2004)