Kuno T, Shirakawa O, Tanaka C
Biochem Biophys Res Commun. 1983 May 16;112(3):948-53. doi: 10.1016/0006-291x(83)91709-6.
The muscarinic acetylcholine receptor was solubilized, in a sensitive form for GTP and Na+, from bovine cerebral cortex using a zwitterionic detergent 3-[(3-cholamidopropyl)-dimethylammonio]-1-propane sulfonate. The solubilized muscarinic receptor displayed characteristics as follows: (1) high affinity to nanomolar concentration of Z-[3H]quinuclidinyl benzilate; (2) muscarinic agonists and antagonists had similar inhibitory potencies as on the membrane-bound receptor; (3) without Na+, GTP did not significantly alter the binding affinity of muscarinic agonists and antagonists; (4) GTP in the presence of Na+, selectively decreased the affinity of muscarinic agonists, carbamylcholine and oxotremoline, but not the antagonist binding affinity; (5) Na+ in the absence or presence of GTP, reduced both muscarinic agonist and antagonist affinities.
使用两性离子去污剂3-[(3-胆酰胺丙基)-二甲基铵]-1-丙烷磺酸盐，从牛大脑皮层中以对GTP和Na⁺敏感的形式溶解毒蕈碱型乙酰胆碱受体。溶解的毒蕈碱受体表现出以下特征：(1) 对纳摩尔浓度的Z-[³H]喹核醇基苯甲酸酯具有高亲和力；(2) 毒蕈碱激动剂和拮抗剂对膜结合受体的抑制效力相似；(3) 无Na⁺时，GTP不会显著改变毒蕈碱激动剂和拮抗剂的结合亲和力；(4) 在有Na⁺存在时，GTP选择性降低毒蕈碱激动剂氨甲酰胆碱和氧化震颤素的亲和力，但不影响拮抗剂的结合亲和力；(5) 在无或有GTP存在时，Na⁺都会降低毒蕈碱激动剂和拮抗剂的亲和力。
