Eldefrawi M E, O'Brien R D
Proc Natl Acad Sci U S A. 1971 Sep;68(9):2006-7. doi: 10.1073/pnas.68.9.2006.
Binding of [(3)H]acetylcholine (measured by equilibrium dialysis) to a particulate preparation of Torpedo electroplax exhibits autoinhibition at concentrations higher than 1 muM. It is suggested that autoinhibition results from acetylcholine binding to regulatory sites on its receptor macromolecules. This binding causes the change to a new and inactive conformation and rejection of acetylcholine bound to the larger number of active sites. The relationship to the physiological phenomenon of desensitization is discussed.
[(3)H]乙酰胆碱(通过平衡透析测定)与电鳐电板颗粒制剂的结合在浓度高于1μM时表现出自身抑制作用。有人认为自身抑制是由于乙酰胆碱与受体大分子上的调节位点结合所致。这种结合导致转变为新的无活性构象,并排斥与大量活性位点结合的乙酰胆碱。文中讨论了其与脱敏生理现象的关系。