新型二氢吡啶CGP 28392对人血小板钙内流的增强作用。
Enhancement of calcium influx in human platelets by CGP 28392, a novel dihydropyridine.
作者信息
Erne P, Bürgisser E, Bühler F R, Dubach B, Kühnis H, Meier M, Rogg H
出版信息
Biochem Biophys Res Commun. 1984 Feb 14;118(3):842-7. doi: 10.1016/0006-291x(84)91471-2.
CGP 28392, a novel compound structurally related to the dihydropyridine Ca2+-entry blockers, causes a dose-dependent increase in intracellular free Ca2+ in human platelets, as measured with the Quin-2 Ca2+ indicator, with a semimaximal effective concentration of 2.2 X 10(-7) M. This effect occurs in a concentration range in which CGP 28392 competes for specific [3H]nitrendipine binding in guinea pig heart membranes. It can be inhibited by nitrendipine. The data presented furnish direct evidence of the Ca2+-entry-stimulating properties of CGP 28392 and indicate the presence of dihydropyridine-susceptible structures in human platelets.
CGP 28392是一种在结构上与二氢吡啶类钙内流阻滞剂相关的新型化合物，在用喹啉-2钙指示剂测定时，它会使人类血小板内的游离钙浓度呈剂量依赖性增加，其半数有效浓度为2.2×10⁻⁷M。这种效应发生在CGP 28392与豚鼠心脏膜片中特异性[³H]尼群地平结合发生竞争的浓度范围内。它可被尼群地平抑制。所呈现的数据为CGP 28392的钙内流刺激特性提供了直接证据，并表明人类血小板中存在对二氢吡啶敏感的结构。
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