The interaction of [3H]nitrendipine with receptors for calcium antagonists in the cerebral cortex and heart of rats.
The interaction of [3H]nitrendipine with receptors for calcium antagonists in the cerebral cortex and heart of rats.
复制标题
[3H]尼群地平与大鼠大脑皮层和心脏中钙拮抗剂受体的相互作用。
DOI：
10.1016/0006-291x(82)91339-0
复制
发表时间：
1982
影响因子：
3.1
通讯作者：
H. Yamamura
中科院分区：
文献类型：
--
作者：
F. Ehlert;E. Itoga;W. Roeske;H. Yamamura
研究了钙拮抗剂[~ 3 H]尼群地平在大鼠大脑皮层和心肌匀浆中的结合特性。[3 H]尼群地平结合的特定组分与质量作用行为一致，并由0.1 - 0.3 nM范围内的高亲和力解离常数描述。[3 H]尼群地平结合对其他钙拮抗剂和阳离子Ca+2和La+3的抑制敏感。维拉帕米对[~ 3 H]尼群地平结合的抑制作用不是简单的竞争型，而是类似于变构抑制，这表明钙拮抗剂至少有两个结合位点。
The binding properties of the calcium antagonist, [3H]nitrendipine, were investigated in homogenates of the rat cerebral cortex and myocardium. The specific component of [3H]nitrendipine binding was consistent with mass action behavior and was described by a high affinity dissociation constant in the range of 0.1 – 0.3 nM. [3H]nitrendipine binding was sensitive to inhibition by other calcium antagonists and by the cations Ca+2and La+3. The inhibition of [3H]nitrendipine binding by verapamil was not of the simple competitive type but resembled allosteric inhibition, suggesting that there are at least two binding sites for calcium antagonists.