Characterization of the binding of [3H]muscimol, a potent gamma-aminobutyric acid agonist, to rat brain synaptosomal membranes using a filtration assay.

作者: Michael Williams , Edwin A. Risley

DOI: 10.1111/J.1471-4159.1979.TB04553.X

关键词: gamma-Aminobutyric acidLigand (biochemistry)Binding siteMuscimolKineticsAgonistCerebellumGABA receptorChemistryBiochemistry

摘要: — The binding of [3H]muscimol, a potent GABA agonist, to crude synaptic membranes prepared from rat brain was studied using filtration method isolate membrane-bound ligand. Specific found be saturable and occurred two sites Kd5 5 30 nm. Binding Na+-independent enhanced by both freezing Triton treatment. Regional subcellular distribution studies pharmacological characterization specific [3H]muscimol are consistent with the receptor.

参考文章(14)
A. Lewis Farr, Oliver H. Lowry, Rose J. Randall, Nira J. Rosebrough, Protein Measurement with the Folin Phenol Reagent Journal of Biological Chemistry. ,vol. 193, pp. 265- 275 ,(1951)
Tsuyoshi Ohnishi, Edward J. Masoro, Helen A. Bertrand, Byung Pal Yu, Analysis of a calcium ion binding system composed of two different sites. Biophysical Journal. ,vol. 12, pp. 1251- 1265 ,(1972) , 10.1016/S0006-3495(72)86160-5
S. ROBERT SNODGRASS, Use of 3 H-muscimol for GABA receptor studies Nature. ,vol. 273, pp. 392- 394 ,(1978) , 10.1038/273392A0
K. Beaumont, W.S. Chilton, H.I. Yamamura, S.J. Enna, Muscimol binding in rat brain: Association with synaptic GABA receptors Brain Research. ,vol. 148, pp. 153- 162 ,(1978) , 10.1016/0006-8993(78)90385-2
Michael J. Leach, Julie A. Wilson, GABA receptor binding with 3H-muscimol in calf cerebellum. European Journal of Pharmacology. ,vol. 48, pp. 329- 330 ,(1978) , 10.1016/0014-2999(78)90092-4
S.J. Enna, James F. Collins, Solomon H. Snyder, Stereospecificity and structure-activity requirements of GABA receptor binding in rat brain Brain Research. ,vol. 124, pp. 185- 190 ,(1977) , 10.1016/0006-8993(77)90878-2
S. R. zukin, A. B. Young, S. H. Snyder, Gamma-aminobutyric acid binding to receptor sites in the rat central nervous system. Proceedings of the National Academy of Sciences of the United States of America. ,vol. 71, pp. 4802- 4807 ,(1974) , 10.1073/PNAS.71.12.4802
G. Toffano, A. Guidotti, E. Costa, Purification of an endogenous protein inhibitor of the high affinity binding of gamma-aminobutyric acid to synaptic membranes of rat brain Proceedings of the National Academy of Sciences of the United States of America. ,vol. 75, pp. 4024- 4028 ,(1978) , 10.1073/PNAS.75.8.4024
H. MÖHLER, T. OKADA, GABA receptor binding with 3 H (+) bicuculline–methiodide in rat CNS Nature. ,vol. 267, pp. 65- 67 ,(1977) , 10.1038/267065A0