These tools will no longer be maintained as of December 31, 2024. Archived website can be found here. PubMed4Hh GitHub repository can be found here. Contact NLM Customer Service if you have questions.


Pubmed for Handhelds

PUBMED FOR HANDHELDS

Search MEDLINE/PubMed

  • Title: Inhibition of 3H-nitrendipine binding in rat aortic and cerebral cortex membranes by the new dihydropyridine calcium antagonist benidipine hydrochloride.
    Author: Ishii A.
    Journal: Arzneimittelforschung; 1989 Dec; 39(12):1546-50. PubMed ID: 2624603.
    Abstract:
    Effects of a new calcium antagonist, benidipine hydrochloride (+/-)-(R*)-3-[(R*)-1-benzyl-3-piperidyl]methyl 1,4-dihydro-2,6-dimethyl-4-(m-nitrophenyl)-3,5-pyridinedi carboxylate hydrochloride, KW-3049), on the 3H-nitrendipine binding in the rat aortic microsomes and cerebral cortex membranes were examined. The equilibrium dissociation constant (Kd) and the binding capacity (Bmax) were 0.32 nmol/l and 59.0 fmol/mg protein, respectively, in the rat aorta and 0.17 nmol/l and 450 fmol/mg protein, respectively, in the rat cortex. In both types of membranes, the specific binding was inhibited completely and concentration-dependently by six calcium antagonists such as benidipine, nicardipine, nisoldipine, nitrendipine, nifedipine and flunarizine. Diltiazem enhanced concentration-dependently the 3H-nitrendipine binding in the aortic and cortex membranes. Benidipine had the highest affinity for specific 3H-nitrendipine binding sites in the aorta (Ki = 0.063 nmol/l) and in the cortex membranes (0.043 nmol/l). The decreasing order of binding affinity of the isomers of benidipine for 3H-nitrendipine binding sites was S-S, benidipine, S-R, R-R and R-S. Presumed metabolites had a weak affinity for 3H-nitrendipine binding sites.
    [Abstract] [Full Text] [Related] [New Search]