marrubenol and 4-desmethoxyverapamil

marrubenol has been researched along with 4-desmethoxyverapamil* in 1 studies

Other Studies

1 other study(ies) available for marrubenol and 4-desmethoxyverapamil

Article	Year
Marrubenol interacts with the phenylalkylamine binding site of the L-type calcium channel. European journal of pharmacology, 2004, May-25, Volume: 492, Issue:2-3 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. Topics: Animals; Binding Sites; Binding, Competitive; Calcium Channel Blockers; Calcium Channels, L-Type; Dihydropyridines; Diterpenes; Furans; Ileum; In Vitro Techniques; Isradipine; Male; Membranes; Muscle Contraction; Muscle, Smooth; Potassium Chloride; Radioligand Assay; Rats; Rats, Wistar; Vasodilator Agents; Verapamil	2004

Article

Year

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

European journal of pharmacology, 2004, May-25, Volume: 492, Issue:2-3

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.

Topics: Animals; Binding Sites; Binding, Competitive; Calcium Channel Blockers; Calcium Channels, L-Type; Dihydropyridines; Diterpenes; Furans; Ileum; In Vitro Techniques; Isradipine; Male; Membranes; Muscle Contraction; Muscle, Smooth; Potassium Chloride; Radioligand Assay; Rats; Rats, Wistar; Vasodilator Agents; Verapamil

2004