Benzofuran analogues of baclofen: a new class of central and peripheral GABAB-receptor antagonists.
Two novel beta-(benzo[b]furan) analogues of baclofen (4-amino-3-benzo[b]furan-2-ylbutanoic acid, 9G, and 4-amino-3-(5-methoxybenzo[b]furan-2-yl)butanoic acid, 9H) antagonised the baclofen-induced depression of twitch contractions in the guinea-pig isolated ileum (estimated apparent pA2 3.9 and 4.1 respectively); both 9G and 9H also antagonised in a dose-dependent manner the baclofen-induced reduction of repetitive paroxysmal discharges in rat neo-cortical slice preparations maintained in Mg2+-free Krebs solution. These benzofurans evidently represents a new class of GABAB-receptor antagonist.
Kerr
D I
DI
Department of Pharmacology, University of Sydney, New South Wales, Australia.
Ong
J
J
Johnston
G A
GA
Berthelot
P
P
Debaert
M
M
Vaccher
C
C
D000818:Animals; D001418:Baclofen / Q000031:analogs & derivatives* / Q000494:pharmacology; D001572:Benzofurans / Q000494:pharmacology*; D002540:Cerebral Cortex / Q000187:drug effects; D058787:GABA-A Receptor Antagonists; D006168:Guinea Pigs; D007082:Ileum / Q000187:drug effects; D066298:In Vitro Techniques; D008274:Magnesium / Q000494:pharmacology; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects / Q000378:metabolism; D051381:Rats; D011919:Rats, Inbred Strains
D001572:Benzofurans; D058787:GABA-A Receptor Antagonists; D001418:Baclofen; D008274:Magnesium