Binding of phencyclidine to the detergent solubilized acetylcholine receptor from Torpedomarmorata

作者: Robert E. Oswald

DOI: 10.1016/0024-3205(83)90120-0

关键词: TorpedoSodium CholateReceptorPhencyclidineAcetylcholine receptorBiochemistryChemistryCholinergicBinding siteAgonist

摘要: Abstract The binding of phencyclidine to the acetylcholine receptor from Torpedo marmorata electroplague was measured following solubilization in sodium cholate followed by exchange for Tween 80. In both membrane-bound and solubilized AChR, addition cholinergic agonists simultaneously with PCP results a 100 1000 fold increase association rate 5 10 dissociation as compared unliganded AChR or equilibrated agonist prior addition. addition, number sites pharmacological properties are not markedly changed soluble receptor. These suggest that can undergo similar conformational transitions 80 form monitor these cases.

参考文章(26)
A Maelicke, B W Fulpius, R P Klett, E Reich, Acetylcholine receptor. Responses to drug binding. Journal of Biological Chemistry. ,vol. 252, pp. 4811- 4830 ,(1977) , 10.1016/S0021-9258(17)40128-1
R. Anholt, J. Lindstrom, M. Montal, Stabilization of acetylcholine receptor channels by lipids in cholate solution and during reconstitution in vesicles. Journal of Biological Chemistry. ,vol. 256, pp. 4377- 4387 ,(1981) , 10.1016/S0021-9258(19)69445-7
Andre SOBEL, Thierry HEIDMANN, Jean CARTAUD, Jean-Pierre CHANGEUX, Reconstitution of a Functional Acetylcholine Receptor FEBS Journal. ,vol. 110, pp. 13- 33 ,(1980) , 10.1111/J.1432-1033.1980.TB04838.X
Jeffery W. Walker, Mark G. McNamee, Elena Pasquale, Derek J. Cash, George P. Hess, Acetylcholine receptor inactivation in torpedo californica electroplax membrane vesicles. Detection of two processes in the millisecond and second time regions Biochemical and Biophysical Research Communications. ,vol. 100, pp. 86- 90 ,(1981) , 10.1016/S0006-291X(81)80066-6
Bianca M. Conti-Tronconi, Susan M. J. Dunn, Michael A. Raftery, Functional stability of Torpedo acetylcholine receptor. Effects of protease treatment. Biochemistry. ,vol. 21, pp. 893- 899 ,(1982) , 10.1021/BI00534A013
George Scatchard, The Attractions of Proteins for Small Molecules and Ions Annals of the New York Academy of Sciences. ,vol. 51, pp. 660- 672 ,(1949) , 10.1111/J.1749-6632.1949.TB27297.X
Mark G. McNamee, Cheryl L. Weill, Arthur Karlin, PURIFICATION OF ACETYLCHOLINE RECEPTOR FROMTORPEDO CALIFORNICAAND ITS INCORPORATION INTO PHOSPHOLIPID VESICLESfn1 Annals of the New York Academy of Sciences. ,vol. 264, pp. 175- 182 ,(1975) , 10.1111/J.1749-6632.1975.TB31482.X