The binding of agonists to brain muscarinic receptors.
The binding of agonists to brain muscarinic receptors.
复制标题
激动剂与脑毒蕈碱受体的结合。
作者：
N. Birdsall;A. Burgen;E. Hulme
通过测量[3H]毒蕈碱激动剂与来自大鼠皮质的膜制剂的结合以及通过[3H]激动剂/激动剂和[3H]拮抗剂/激动剂竞争实验，研究了激动剂与毒蕈碱受体的相互作用。结合数据可以通过激动剂结合位点的两个主要群体的存在来解释，这两个主要群体在结合实验期间不相互转换并且对于拮抗剂具有相同的亲和力常数。激动剂对这两个位点的亲和常数的比率可以从1变化到约275。这两个位点的激动剂亲和常数与衍生自毒蕈碱激动剂对平滑肌的作用的参数之间存在定量一致性。已经检测到“超高”亲和力激动剂结合位点的第三(次要)群体。
The interaction of agonists with muscarinic receptors has been investigated by measuring the binding of [3H]muscarinic agonists to membrane preparations from the rat cortex and by means of [3H]agonist/agonist and [3H]antagonist/agonist competition experiments. The binding data can be explained by the presence of two major populations of agonist binding sites which do not interconvert during the binding experiments and have the same affinity constants for antagonists. The ratio of the affinity constants of an agonist for the two sites can vary from 1 to about 275. There is quantitative agreement between the agonist affinity constants for the two sites and parameters derived from the action of muscarinic agonists on smooth muscle, A third (minor) population of "super-high" affinity agonist binding sites has been detected.