Binding of [3H]isradipine (PN 200-110) on smooth muscle cell membranes from different bovine arteries.
The binding of [3H]isradipine [( 3H]PN 200-110), a new dihydropyridine (DHP) calcium blocker on smooth muscle cell (SMC) membranes from different bovine arteries was saturable with comparable high affinities but different binding site densities (Bmax). The data were fitted to a model that provided a common estimation for the dissociation constant (Kd = 0.46 nM, SD = 0.03) but different Bmax values. Two groups of arteries could be distinguished, large-sized with high Bmax (aorta, 149 fmol/mg, SD = 4; intrapulmonary, 134 fmol/mg, SD = 4) and medium-sized with lower Bmax (mesenteric, 67 fmol/mg, SD = 2; internal carotid, 50 fmol/mg, SD = 2; renal artery, 29 fmol/mg, SD = 2). The Kd values were similar to those previously reported, but the Bmax value on aorta SMC was higher than usually reported with other DHPs, showing that isradipine was a high full antagonist of calcium channel. Our results also suggest that the increase in arterial compliance induced by DHPs will probably be more important on large-sized arteries than on medium-sized arteries because of higher DHP binding.
D000818:Animals; D000959:Antihypertensive Agents / Q000378:metabolism*; D001158:Arteries / Q000378:metabolism; D002121:Calcium Channel Blockers / Q000378:metabolism*; D002417:Cattle; D002462:Cell Membrane / Q000378:metabolism; D066298:In Vitro Techniques; D017275:Isradipine; D009131:Muscle, Smooth, Vascular / Q000378:metabolism*; D011725:Pyridines / Q000378:metabolism*; D014316:Tritium
D000959:Antihypertensive Agents; D002121:Calcium Channel Blockers; D011725:Pyridines; D014316:Tritium; D017275:Isradipine