大鼠大脑皮层中高亲和力和低亲和力哌仑西平结合位点的增溶及特性研究
Solubilization and characterization of high and low affinity pirenzepine binding sites from rat cerebral cortex.
作者信息
Berrie C P, Birdsall N J, Hulme E C, Keen M, Stockton J M
出版信息
Br J Pharmacol. 1985 Jul;85(3):697-703. doi: 10.1111/j.1476-5381.1985.tb10566.x.
Abstract
An apparently monomeric form of the digitonin-solubilized muscarinic acetylcholine receptor from the rat cerebral cortex retains a high affinity of 7 X 10(7) M-1 for pirenzepine. Muscarinic receptor binding sites in the rat cerebral cortex with a low affinity for pirenzepine are solubilized with relatively little change in affinity. The ability of pirenzepine to distinguish between subtypes of muscarinic binding site in the cerebral cortex is manifest in both the membrane-bound and soluble state.
摘要
从大鼠大脑皮层中提取的经洋地黄皂苷增溶的毒蕈碱型乙酰胆碱受体的一种明显的单体形式，对哌仑西平仍保持7×10⁷ M⁻¹的高亲和力。大鼠大脑皮层中对哌仑西平低亲和力的毒蕈碱受体结合位点在增溶时亲和力变化相对较小。哌仑西平区分大脑皮层中毒蕈碱结合位点亚型的能力在膜结合状态和可溶状态下均有体现。
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2
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Nature. 1980 Jan 3;283(5742):90-2. doi: 10.1038/283090a0.
3
Two populations of binding sites for muscarinic antagonists in the rat heart.大鼠心脏中毒蕈碱拮抗剂的两类结合位点
Eur J Pharmacol. 1981 Jul 17;73(2-3):137-42. doi: 10.1016/0014-2999(81)90085-6.
4
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