ACTIONS OF THIENYL ANALOGS OF BACLOFEN AT GABA(B) RECEPTORS IN RAT NEOCORTICAL SLICES

Citation
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
Citations number
11
Categorie Soggetti
Pharmacology & Pharmacy
ISSN journal
00142999
Volume
329
Issue
2-3
Year of publication
1997
Pages
133 - 136
Database
ISI
SICI code
0014-2999(1997)329:2-3<133:AOTAOB>2.0.ZU;2-E
Abstract
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.