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Eur J Pharmacol. 2002 Aug 2;449(1-2):55-60.

Drotaverine interacts with the L-type Ca(2+) channel in pregnant rat uterine membranes.

Author information

1
Internal Medicine Department, Sanofi-Synthelabo CHINOIN, Tó utca 1-5, Budapest, H-1045 Hungary. zsuzsanna.tomoskozi@sanofi-synthelabo.com

Abstract

The effect of the isoquinoline derivative, drotaverine on the specific binding of [(3)H]nitrendipine and [(3)H]diltiazem to pregnant rat uterine membranes was examined. Drotaverine inhibited the specific [(3)H]nitrendipine and [(3)H]diltiazem bindings with IC(50) values of 5.6 and 2.6 microM, respectively. Saturation studies showed that diltiazem caused a significant increase in the maximum binding density without changing the K(D) of [(3)H]nitrendipine while drotaverine increased both the K(D) and the B(max) of [3H]nitrendipine. The dissociation kinetics of both [3H]nitrendipine and [(3)H]diltiazem were accelerated by drotaverine. These results suggest that drotaverine has a negative allosteric interaction with the binding sites for 1,4-dihydropyridines and 1,5-benzothiazepines on the L-type Ca(2+) channel in pregnant rat uterine membranes, which may have implications as to the potential usefulness of this drug in aiding child delivery.

PMID:
12163106
DOI:
10.1016/s0014-2999(02)01993-3
[Indexed for MEDLINE]

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