大鼠心肌中鸟嘌呤核苷酸敏感的毒蕈碱激动剂结合位点的增溶与特性研究
Solubilization and characterization of guanine nucleotide-sensitive muscarinic agonist binding sites from rat myocardium.
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. 1984 Aug;82(4):853-61. doi: 10.1111/j.1476-5381.1984.tb16482.x.
Abstract
Muscarinic receptors from rat myocardial membranes may be solubilized by digitonin in good yield at low temperatures in the presence of Mg2+. Under these conditions, up to 60% of the soluble receptors show high affinity binding for the potent agonist [3H]-oxotremorine-M (KA = 10(9)M-1), which is inhibited by 5'-guanylylimidodiphosphate. The muscarinic binding site labelled with [3H]-oxotremorine-M has a higher sedimentation coefficient (13.4 s) than sites labelled with a 3H antagonist in the presence of guanylylimidodiphosphate (11.6 s) and probably represents a complex between the ligand binding subunit of the receptor and a guanine nucleotide binding protein.
摘要
在Mg2+存在的情况下，用洋地黄皂苷在低温下可高产率地溶解大鼠心肌膜中的毒蕈碱受体。在这些条件下，高达60%的可溶性受体对强效激动剂[3H]-氧震颤素-M（KA = 10(9)M-1）表现出高亲和力结合，该结合被5'-鸟苷酰亚胺二磷酸抑制。与[3H]-氧震颤素-M标记的毒蕈碱结合位点的沉降系数（13.4 s）高于在鸟苷酰亚胺二磷酸存在下用3H拮抗剂标记的位点（11.6 s），并且可能代表受体的配体结合亚基与鸟嘌呤核苷酸结合蛋白之间的复合物。
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