J. Ong et al., ACTIONS OF THIENYL ANALOGS OF BACLOFEN AT GABA(B) RECEPTORS IN RAT NEOCORTICAL SLICES, European journal of pharmacology, 329(2-3), 1997, pp. 133-136
In rat neocortical slices maintained 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)-butano
ic acid (5j) dose-dependently suppressed the spontaneous discharges, a
ntagonised by the GABAB receptor antagonist 2-hydrosaclofen (200 eta M
). Their relative potencies were baclofen > 5h > 5d > 5f > 5j. These h
eterocyclic analogs may prove useful as GABA(B) receptor agonist in fu
nctional studies. (C) 1997 Elsevier Science B.V.