[3H]diltiazem binding to calcium channel antagonists recognition sites in rat cerebral cortex.
[3H]diltiazem binding to calcium channel antagonists recognition sites in rat cerebral cortex.
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[3H]地尔硫卓与大鼠大脑皮层钙通道拮抗剂识别位点结合。
DOI：
10.1016/0014-2999(85)90768-x
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发表时间：
1985
影响因子：
5
通讯作者：
S. Z. Langer
中科院分区：
文献类型：
--
作者：
H. Schoemaker;S. Z. Langer
基于与[3 H]二氢吡啶类钙通道拮抗剂的结合研究，假设脑中钙通道的大分子复合物内存在地尔硫卓识别位点。因此，在本研究中，我们表征了大鼠大脑皮质中[3 H]地尔硫卓结合位点的特征。饱和的高亲和力（Kd= 50 - 170 nM）[3 H]地尔硫卓与大鼠大脑皮层的结合被地尔硫卓的对映体立体特异性抑制，这取决于它们作为钙通道拮抗剂和[3 H]二氢吡啶结合调节剂的活性。化学异质性钙通道拮抗剂对[3 H]地尔硫卓结合的影响进一步证实了[3 H]地尔硫卓结合位点与钙通道之间的关联。根据其药理学作用，二氢吡啶类似乎会变构影响[3 H]地尔硫卓的结合;例如，在37°C下，尼群地平增强，而钙激动剂Bay K 8644在完全抑制[3 H]尼群地平结合的浓度下不能影响[3 H]地尔硫卓的结合。尼群地平的作用可能，至少部分地，是由[3 H]地尔硫卓的亲和力增加来解释的。
The presence of a diltiazem recognition site within the macromolecular complex of the calcium channel in the brain had been hypothesized on the basis of binding studies with [3H]dihydropyridine calcium channel antagonists. In the present study, we therefore characterized [3H]diltiazem binding sites in the rat cerebral cortex. Saturable high affinity (Kd= 50−170 nM) [3H]diltiazem binding to the rat cerebral cortex was stereospecifically inhibited by the enantiomers of diltiazem according to their activity as calcium channel antagonists and modulators of [3H]dihydropyridine binding. An association between the [3H]diltiazem binding site and the calcium channel was further corroborated by the effects of chemically heterogenous calcium channel antagonists on [3H]diltiazem binding. Dihydropyridines appeared to allosterically affect [3H]diltiazem binding according to their pharmacological effects; e.g. at 37°C nitrendipine enhanced whereas the calcium agonist Bay K 8644 failed to affect [3H]diltiazem binding at concentrations fully inhibiting [3H]nitrendipine binding. The effect of nitrendipine may, at least in part, be explained by an increase in the affinity of [3H]diltiazem.
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
发表时间：
1982
影响因子：
3.1
作者：
Yamamura,HI;Schoemaker,H;Boles,RG;Roeske,WR
通讯作者：
Roeske,WR
[3H]尼群地平与冠状动脉和心脏膜的特异性结合与药理作用的关系。
DOI：
10.1016/0006-291x(82)91838-1
发表时间：
1982
影响因子：
3.1
作者：
DePover,A;Matlib,MA;Lee,SW;Dubé,GP;Grupp,IL;Grupp,G;Schwartz,A
通讯作者：
Schwartz,A
尼群地平和 Bay k 8644 与离体犬心脏肌膜结合与其对犬心脏药理作用的相关性。
影响因子：
5
作者：
Vaghy,PL;Grupp,IL;Grupp,G;Balwierczak,JL;Williams,JS;Schwartz,A
通讯作者：
Schwartz,A