Effects of oxodipine and elgodipine on (+)-[3H]-isradipine binding to cardiac and vascular membranes: cardiovascular selectivity.

L. Rakotoarisoa, N. Leprêtre, J. Mironneau, A. Galiano, C. Mironneau
Fundamental & Clinical Pharmacology. 1994-11-12; 8(6): 546-552
DOI: 10.1111/j.1472-8206.1994.tb00836.x

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1. Fundam Clin Pharmacol. 1994;8(6):546-52.

Effects of oxodipine and elgodipine on (+)-[3H]-isradipine binding to cardiac and
vascular membranes: cardiovascular selectivity.

Rakotoarisoa L(1), Leprêtre N, Mironneau J, Galiano A, Mironneau C.

Author information:
(1)Laboratoire de Physiologie Cellulaire et Pharmacologie Moléculaire, URA CNRS
1489, Université de Bordeaux II, France.

We studied the effects of six dihydropyridines on the specific binding of
(+)-[3H]-isradipine to vascular (portal vein) and cardiac isolated membranes to
achieve the relative cardiovascular selectivity of these compounds. Elgodipine,
(+)-oxodipine and nifedipine had a significantly higher affinity for the vascular
L-type calcium channel than for the cardiac calcium channel while nicardipine
showed opposite properties. The other dihydropyridines (nitrendipine and
(+)-isradipine) had similar affinities for the cardiac and vascular calcium
channels. As the membrane potential of isolated membranes is about 0 mV, these
results suggest that the differences in binding of these dihydropyridines to
L-type calcium channels in vascular and cardiac cells may be attributed to
differences in the molecular structure of these calcium channels.

DOI: 10.1111/j.1472-8206.1994.tb00836.x
PMID: 7721232 [Indexed for MEDLINE]

Auteurs Bordeaux Neurocampus