Identification of putative calcium channels in skeletal muscle microsomes

FEBS Letters

Ferry, David R.¹  Glossmann, Hartmut¹ 

[1] Rudolf Buchheim-Institut für Pharmakologie, Justus-Liebig-Universität, Frankfurter Straße 107, D-63 Gießen, FRG

关键词: Skeletal muscle;    Calcium channel;    Antagonist;    Receptor;    Allosterism;    Nimodipine;   

DOI  :  10.1016/0014-5793(82)80835-1

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

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.

【 授权许可】

Unknown