Janis R A, Maurer S C, Sarmiento J G, Bolger G T, Triggle D J
Eur J Pharmacol. 1982 Aug 27;82(3-4):191-4. doi: 10.1016/0014-2999(82)90511-8.
Specific binding of [3H]nimodipine to membranes from rat ventricle and guinea pig ileal longitudinal smooth muscle was studied. Dissociation constants were 0.24 and 0.12 nM, and the maximal number of binding sites were 0.4 and 0.75 pmol/mg protein for cardiac and smooth muscle, respectively. The values obtained for both types of muscle were similar to those obtained for [3H]nitrendipine binding, as were the potencies of a series of dihydropyridines for competing with [3H]nimodipine. These results support the hypothesis that the binding site characterized is that mediating the pharmacological effects of these compounds.
研究了[3H]尼莫地平与大鼠心室和豚鼠回肠纵行平滑肌膜的特异性结合。解离常数分别为0.24和0.12 nM，心肌和平滑肌的最大结合位点数分别为0.4和0.75 pmol/mg蛋白质。两种肌肉获得的值与[3H]尼群地平结合获得的值相似，一系列二氢吡啶与[3H]尼莫地平竞争的效力也相似。这些结果支持了这样的假设，即所表征的结合位点是介导这些化合物药理作用的位点。
