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

Article Details

Citation

Copy to clipboard

Tomoskozi Z, Finance O, Aranyi P

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

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

PubMed ID

12163106 [ View in PubMed

]

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.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Drotaverine	Voltage-dependent L-type calcium channel (Protein Group)	Protein group	Humans	Unknown	Inhibitor	Details