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GABA-induced /sup 36/Cl/sup -/ influx: a biochemical correlate of the physiological event regulated by GABA receptors

Conference · · Fed. Proc., Fed. Am. Soc. Exp. Biol.; (United States)
OSTI ID:6898893
Microsacs from whole rat brain were prepared in HEPES-buffered saline, as described by Harris and Allan. GABA-induced /sup 36/Cl/sup -/ influx into brain microsacs at 30/sup 0/C was dose dependent, saturable, and had an ED/sub 50/ of 25 ..mu..M. The Hill coefficient of the dose-response curve of the GABA response was >1. Other GABA agonists induced /sup 36/Cl/sup -/ influx similarly and with a rank order that paralleled their physiological potencies. Preincubation with GABA produced receptor desensitization and reduced the influx. Bicuculline inhibited the GABA-induced influx competitively, and the inhibition was stereospecific ((+)bicuculline was >10-fold more effective than (-)bicuculline). The convulsants picrotoxinin and t-butyl-bicyclophosphorothionate also inhibited to GABA-induced /sup 36/Cl/sup -/ influx, but noncompetitively. The same effect was observed with cyclodiene insecticides, and their action was stereospecific. Pentobarbital, on the other hand, potentiated the GABA-induced /sup 36/Cl/sup -/ influx.
Research Organization:
Univ. of Maryland School of Medicine, Baltimore
OSTI ID:
6898893
Report Number(s):
CONF-8604222-
Conference Information:
Journal Name: Fed. Proc., Fed. Am. Soc. Exp. Biol.; (United States) Journal Volume: 45:4
Country of Publication:
United States
Language:
English