| Literature DB >> 6696758 |
J P Galizzi, M Fosset, M Lazdunski.
Abstract
[3H]verapamil binding to muscle tubule membrane has the following properties. KD = 27 +/- 5 nM and maximum binding capacity Bmax = 50 +/- 5 pmol/mg of protein. A 1 = 1 stoichiometry of binding was found for the ratio of [3H]verapamil versus [3H] nitrendipine binding sites. The dissociation constant found at equilibrium is near that determined from the ratio of the rate constants for association (k1) and dissociation (k-1). Antiarrhythmic drugs like D600, diltiazem and bepridil are competitive inhibitors of [3H] verapamil binding with KD values between 40 and 200 nM. Dihydropyridine analogs are apparent non competitive inhibitors of [3H]verapamil binding with half-maximum inhibition values (K0.5) between 1 and 5 nM.Entities:
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Year: 1984 PMID: 6696758 DOI: 10.1016/0006-291x(84)91092-1
Source DB: PubMed Journal: Biochem Biophys Res Commun ISSN: 0006-291X Impact factor: 3.575