Sieber M, Nastainczyk W, Röhrkasten A, Hofmann F
Institut für Physiologische Chemie, Universität des Saarlandes, Homburg/Saar.
Biomed Biochim Acta. 1987;46(8-9):S357-62.
The purified receptor for calcium channel blockers from rabbit skeletal muscle was reconstituted into phospholipid vesicles. The reconstitution did not alter the stoichiometry of the peptide chains. [3H]PN 200-110 bound to one site with apparent KD and Bmax values of 9.8 nM and 980 pmol/mg protein, respectively. The binding was stereospecific. D-cis-diltiazem and (-) desmethoxyverapamil affected allosterically the binding of dihydropyridines. This demonstrates the coinsertion of specific binding sites for the three calcium channel blocker into phospholipid vesicles.
