Dube G P, Baik Y H, Vaghy P L, Schwartz A
Biochem Biophys Res Commun. 1985 May 16;128(3):1295-302. doi: 10.1016/0006-291x(85)91081-2.
Bay k 8644 and nitrendipine, dihydropyridines classified as calcium channel agonist and antagonist, respectively, produced concentration-dependent biphasic responses (contraction and relaxation) in porcine coronary artery rings. Nitrendipine relaxed rings (IC50 = 60 nM) that were contracted with 100 nM Bay k 8644. Pretreatment of rings with 60 nM nitrendipine caused paradoxical potentiation of Bay k 8644-induced contraction. The data are consistent with a model that consists of two functionally-distinct dihydropyridine "receptors" with which Bay k 8644 and nitrendipine interact as partial agonists. We propose that these excitatory and inhibitory dihydropyridine receptor subtypes mediate contraction and relaxation, respectively, by dihydropyridines.
分别归类为钙通道激动剂和拮抗剂的二氢吡啶类化合物Bay k 8644和尼群地平，在猪冠状动脉环中产生浓度依赖性双相反应（收缩和舒张）。尼群地平使由100 nM Bay k 8644引起收缩的环舒张（IC50 = 60 nM）。用60 nM尼群地平预处理环导致Bay k 8644诱导的收缩出现反常增强。这些数据与一个模型相符，该模型由两个功能不同的二氢吡啶“受体”组成，Bay k 8644和尼群地平作为部分激动剂与它们相互作用。我们提出，这些兴奋性和抑制性二氢吡啶受体亚型分别通过二氢吡啶介导收缩和舒张。
