Referenced in: none

Automatically associated channels: Kv2.1

Title: Unusual effects of benzodiazepines and cyclodiene insecticides on an expressed invertebrate GABAA receptor.

Authors: S H Zaman, R J Harvey, E A Barnard, M G Darlison

Journal, date & volume: FEBS Lett., 1992 Aug 3 , 307, 351-4

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/1379544

Abstract
We have previously reported [(1991) EMBO J. 10, 3239-3245] the sequence of an invertebrate gamma-aminobutyric acid (GABA) type A (GABAA) receptor polypeptide which forms homo-oligomeric GABA-gated, bicuculline-sensitive, chloride-ion channels upon heterologous expression. We now demonstrate that the benzodiazepines Ro5-4864 (4'-chlorodiazepam) and diazepam, that are active at mammalian peripheral benzodiazepine sites, and not those benzodiazepines specific for central sites, directly active the homo-oligomeric receptor and evoke larger maximal responses than those elicited by GABA. In addition, members of the cyclodiene class of insecticides block the channel of the receptor in a manner indistinguishable from that of picrotoxin.