Effects of oxodipine and elgodipine on (+)-[3H]-isradipine binding to cardiac and vascular membranes: cardiovascular selectivity.
Fundamental & Clinical Pharmacology. 1994-11-12; 8(6): 546-552
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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.
(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.
PMID: 7721232 [Indexed for MEDLINE]