Diltiazem enhancement of [3H]nitrendipine binding to calcium channel associated drug receptor sites in rat brain synaptosomes.
Diltiazem enhancement of [3H]nitrendipine binding to calcium channel associated drug receptor sites in rat brain synaptosomes.
复制标题
地尔硫卓增强[3H]尼群地平与大鼠脑突触体中钙通道相关药物受体位点的结合。
DOI：
10.1016/0006-291x(82)90877-4
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发表时间：
1982
影响因子：
3.1
通讯作者：
Roeske,WR
中科院分区：
文献类型：
--
作者：
Yamamura,HI;Schoemaker,H;Boles,RG;Roeske,WR
研究了二氢吡啶钙通道拮抗剂[3H]尼群地平与全大鼠脑突触体的结合。结合具有特异性、可饱和性和高亲和力 (Kd= 170 pM)。钙通道拮抗剂地尔硫卓在 1 和 10 μM 浓度下增强[3H]尼群地平在突触体中的结合。平衡饱和分析表明，这种效应是通过解离常数的降低介导的，这是由于配体-受体复合物解离速率降低了 3 倍。结论是地尔硫卓变构调节该制剂中[3H]尼群地平标记的钙通道药物受体。
The binding of the dihydropyridine calcium channel antagonist [3H]nitrendipine to whole rat brain synaptosomes was studied. Binding was specific, saturable, and of high affinity (Kd= 170 pM). The calcium channel antagonist diltiazem enhanced [3H]nitrendipine binding in synaptosomes in concentrations of 1 and 10 μM. Equilibrium saturation analysis demonstrated that this effect was mediated by a decrease in the dissociation constant, due to a 3-fold reduction in the rate of ligand-receptor complex dissociation. It is concluded that diltiazem allosterically modulates the calcium channel drug receptor labeled by [3H]nitrendipine in this preparation.