Ferry D R, Glossmann H
Naunyn Schmiedebergs Arch Pharmacol. 1982 Oct;321(1):80-3. doi: 10.1007/BF00586355.
[3H]-Nimodipine a potent calcium channel blocker, binds to an apparently homogenous population of receptors in guinea-pig brain membranes (KD=0.62 nM, Hill coefficient or approximately 1.0). Diltiazem (10(-5) M) lowers the KD for [3H]-nimodipine by a factor of 3 without changing the maximum number of binding sites. Diltiazem decreased the dissociation rate constant of the nimodipine-receptor complex from 0.18 min-1 to 0.049 min-1 and altered the pharmacological profile as revealed by displacement studies with (-) and (+) verapamil, (-) and (+) prenylamine and 1,4 dihydropyridines. In conclusion [3H]-nimodipine binding can be utilized as a tool to evaluate complex molecular interactions between calcium channel blockers.
[3H] - 尼莫地平是一种强效钙通道阻滞剂，它与豚鼠脑膜中明显同质的受体群体结合（解离常数KD = 0.62 nM，希尔系数约为1.0）。地尔硫卓（10^(-5) M）可使[3H] - 尼莫地平的KD降低3倍，而不改变结合位点的最大数量。地尔硫卓将尼莫地平 - 受体复合物的解离速率常数从0.18 min^(-1)降至0.049 min^(-1)，并改变了药理学特征，这在使用（-）和（+）维拉帕米、（-）和（+）普尼拉明以及1,4 - 二氢吡啶进行的置换研究中得到了揭示。总之，[3H] - 尼莫地平结合可作为评估钙通道阻滞剂之间复杂分子相互作用的一种工具。
