Actions of thienyl analogs of baclofen at GABA(B) receptors in rat neocortical slices.
In rat neocortical slices maintained in Mg2+-free Krebs medium, baclofen and its thienyl analogs, 4-amino-3-(5-chlorothien-2-yl)-butanoic acid (5h), 4-amino-3-(5-methylthien-2-yl)-butanoic acid (5d), 4-amino-3-(5-bromothien-2-yl)-butanoic acid (5f) and 4-amino-3-(thien-3-yl)-butanoic acid (5j) dose-dependently suppressed the spontaneous discharges, antagonised by the GABA(B) receptor antagonist 2-hydroxysaclofen (200 microM). Their relative potencies were baclofen > 5h > 5d > 5f > 5j. These heterocyclic analogs may prove useful as GABA(B) receptor agonists in functional studies.
Ong
J
J
Department of Anaesthesia and Intensive Care, The University of Adelaide, South Australia. jong@medicine.adelaide.edu.au
Kerr
D I
DI
Vaccher
C
C
Berthelot
P
P
D000818:Animals; D001418:Baclofen / Q000031:analogs & derivatives* / Q000494:pharmacology*; D002540:Cerebral Cortex / Q000187:drug effects* / Q000378:metabolism; D004594:Electrophysiology; D018755:GABA Agonists / Q000494:pharmacology*; D058786:GABA-B Receptor Agonists; D008297:Male; D051381:Rats; D017207:Rats, Sprague-Dawley; D013329:Structure-Activity Relationship
D018755:GABA Agonists; D058786:GABA-B Receptor Agonists; D001418:Baclofen