Oswald R E
Life Sci. 1983 Mar 7;32(10):1143-9. doi: 10.1016/0024-3205(83)90120-0.
The binding of phencyclidine to the acetylcholine receptor from Torpedo marmorata electroplaque was measured following solubilization of the receptor in sodium cholate followed by the exchange of cholate for Tween 80. In both the membrane-bound and solubilized AChR, the addition of cholinergic agonists simultaneously with the addition of PCP results in a 100 to 1000 fold increase in the PCP association rate and a 5 to 10 fold increase in the dissociation rate as compared to the unliganded AChR or AChR equilibrated with agonist prior to PCP addition. In addition, the number of binding sites and the pharmacological properties of the binding are not markedly changed in the soluble receptor. These results suggest that the acetylcholine receptor can undergo similar conformational transitions in the membrane-bound and the Tween 80 solubilized form and that phencyclidine can monitor these transitions in both cases.
在将受体溶解于胆酸钠中，随后用吐温80替换胆酸盐后，测定了苯环利定与电鳐电板乙酰胆碱受体的结合情况。在膜结合型和溶解型乙酰胆碱受体中，与未结合配体的乙酰胆碱受体或在添加苯环利定之前用激动剂平衡的乙酰胆碱受体相比，同时添加胆碱能激动剂和苯环利定会导致苯环利定结合速率增加100至1000倍，解离速率增加5至10倍。此外，可溶性受体中结合位点的数量和结合的药理学特性没有明显变化。这些结果表明，乙酰胆碱受体在膜结合型和吐温80溶解型中可以经历类似的构象转变，并且苯环利定在这两种情况下都可以监测这些转变。
