Abstract
Saturable binding sites for the labelled calcium antagonist (±)[ 3H]nimodipine were found in guinea-pig hind limb skeletal muscle homogenates. Binding sites were enriched in a microsomal pellet by differential centrifugation of the homogenate. [ 3H]Nimodipine binding ( K d = 1.5±0.03 nM, B max = 2.1 ± 0.25 pmol/protein, at 37°C) copurified (6-fold) in this fraction with [ 3H]ouabain binding (6.6-fold) and 125I-α-bungarotoxin binding (5-fold). d- cis-Diltiazem (but not 1- cis-diltiazem) stimulated (±) [ 3H]nimodipine binding ( ED 50 1 μM) by increasing the B max. Binding sites discriminated between the optical enantiomers of 1,4-dihydropyridine calcium antagonists and the optically pure enantiomers of D-600. The data confirm, with biochemical techniques, the presence of 1,4-dihydropyridine and (±)D-600 inhibitable calcium channels in skeletal muscle, previously found with electrophysiological techniques.
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