In:
Canadian Journal of Physiology and Pharmacology, Canadian Science Publishing, Vol. 76, No. 7-8 ( 1998-07-01), p. 798-801
Abstract:
(R,S)-4-Amino-3-(7-methylbenzo[b]furan-2-yl)-butanoic acid (7-MBFG), a new benzofuran analogue of the GABA B receptor agonist baclofen, has been evaluated for pharmacological activity on GABA B receptors in the guinea-pig isolated ileum and rat neocortical slices. 7-MBFG (300 and 500 µM) reversibly antagonized the (R,S)-baclofen induced depression of cholinergic twitch contractions in the guinea-pig ileum and shifted the concentration-response curve for baclofen to the right, in a parallel manner, giving an apparent pA 2 value of 3.7 ± 0.3. Likewise, 7-MBFG (300 and 500 µM) reversibly blocked the baclofen-induced suppression of spontaneous discharges, in rat neocortical slices maintained in Mg 2+ -free Krebs medium, and caused a rightward, parallel shift of the baclofen concentration-response curve, giving an apparent pA 2 value of 4.1 ± 0.1. The compound 7-MBFG belongs to a novel, new class of antagonist at central and peripheral GABA B receptors, in which the antagonist properties reside in the pseudo-aromatic character of their 3-benzo[b]furan-2-yl substituents, and might provide useful leads for further development of GABA B receptor ligands.Key words: (R,S)-baclofen, 4-amino-3-(7-methylbenzo[b]furan-2-yl)-butanoic acid, GABA B receptor antagonist, rat neocortex, guinea-pig ileum.
Type of Medium:
Online Resource
ISSN:
0008-4212
,
1205-7541
Language:
English
Publisher:
Canadian Science Publishing
Publication Date:
1998
detail.hit.zdb_id:
2004356-9
Permalink
