title: Effects of oxodipine and elgodipine on (+)-[3H]-isradipine binding to cardiac and vascular membranes: cardiovascular selectivity.
abstract: 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.
authors.affiliation: Laboratoire de Physiologie Cellulaire et Pharmacologie Moléculaire, URA CNRS 1489, Université de Bordeaux II, France.
authors.forename: L
authors.initials: L
authors.lastname: Rakotoarisoa
authors.forename: N
authors.initials: N
authors.lastname: Leprêtre
authors.forename: J
authors.initials: J
authors.lastname: Mironneau
authors.forename: A
authors.initials: A
authors.lastname: Galiano
authors.forename: C
authors.initials: C
authors.lastname: Mironneau
mesh_terms: D000818:Animals; D001665:Binding Sites; D002121:Calcium Channel Blockers / Q000494:pharmacology*; D004095:Dihydropyridines / Q000494:pharmacology*; D006736:Horses; D066298:In Vitro Techniques; D017275:Isradipine / Q000378:metabolism*; D009206:Myocardium / Q000378:metabolism*; D011169:Portal Vein / Q000378:metabolism*; D051381:Rats
chemical_list: D002121:Calcium Channel Blockers; D004095:Dihydropyridines; C063839:elgodipine; C053783:oxodipine; D017275:Isradipine