Behavioral and functional studies indicate a role for GABAAergic transmission in the actions of ethanol.
Ethanol interacts allosterically with the picrotoxin binding sites on the oligomeric GABA receptor complex in vitro. Chronic ethanol treatment does not alter the binding properties of [35S]t-butyl-bicyclophosphorothioate or [3H]flunitrazepam to brain membranes. In behavioral studies, ethanol prevents convulsions induced by bicuculline, picrotoxin and maximal electroshock seizures. Further, subprotective dose of ethanol in combination with other facilitators of GABAergic transmission, provide protection against these convulsions. Finally, ethanol potentiates the effect of GABA on 36Cl-influx in cultured spinal cord neurons. These studies indicate a role for GABAAergic transmission in the actions of ethanol.
Ticku
M K
MK
University of Texas Health Science Center, Department of Pharmacology, San Antonio 78284-7764.
D000818:Animals; D001921:Brain / Q000187:drug effects; D001643:Bridged Bicyclo Compounds / Q000494:pharmacology; D019086:Bridged Bicyclo Compounds, Heterocyclic; D002462:Cell Membrane / Q000187:drug effects; D002712:Chlorides / Q000378:metabolism; D000431:Ethanol / Q000494:pharmacology*; D005445:Flunitrazepam / Q000494:pharmacology; D008297:Male; D051379:Mice; D008810:Mice, Inbred C57BL; D010852:Picrotoxin / Q000494:pharmacology; D051381:Rats; D011963:Receptors, GABA-A / Q000187:drug effects*; D012640:Seizures / Q000139:chemically induced; D013116:Spinal Cord / Q000166:cytology / Q000187:drug effects
D001643:Bridged Bicyclo Compounds; D019086:Bridged Bicyclo Compounds, Heterocyclic; D002712:Chlorides; D000431:Ethanol; D005445:Flunitrazepam; D010852:Picrotoxin; D011963:Receptors, GABA-A; C037476:tert-butylbicyclophosphorothionate