This paper reports the radioactive ligand binding technique for GABA receptor and the biochemical char acteristics of GABA receptor of ox cerebellum.The crude synaptic membrane fraction of ox cerebullum was prepared by high speed centrifugation. 3H-GABA binding to receptor on synaptic membrane is a saturate process, and with a dissociation constant of 96 nM, maximum number of binding site of 1.02 Pmol/mg protein and Hill number of 0.99. In binding with GABA receptor, compounds differ from each other in their pharmacological and stereo-scopic specificities. The kinetic constants of GABA receptor binding activity were determined by observed rate method. The rate con-stants for association and dissociation were 9.6×106 M-1 min-1 aud 0.115 min-1 respectively. The activty was increased to 114 fold by supersonic, freezing, thawing, washing and Triton X-100 treatment.
Key words
GABA Receptor /
ox Cerebellum /
Synaptic membrane /
3H-GABA /
radioactive ligand binding.
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References
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[3] David. B. Bylun(1980) in Receptor Binding Techniques, pp 70-99．
[4] Toffano, G. et al. (1978) Proc. Nat. Acad. Sci., USA, 75, 4024-4028．
[5] Olsen, R. W. et al. (1981) Mol. Pharmacol., 19, 217-227．
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Footnotes
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