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|Title:||GABAB receptor antagonism by 7-MBFG, a benzo[b]furan analogue of baclofen, in central and peripheral tissues|
|Citation:||Canadian Journal of Physiology and Pharmacology, 1998; 76(7-8):798-801|
|Ong, Jennifer ; Kerr, David I. ; Ansar, M'hammed ; Vaccher, Claude ; Berthelot, Pascal|
|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 microM) 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 pA2 value of 3.7+/-0.3. Likewise, 7-MBFG (300 and 500 microM) reversibly blocked the baclofen-induced suppression of spontaneous discharges, in rat neocortical slices maintained in Mg2+ -free Krebs medium, and caused a rightward, parallel shift of the baclofen concentration-response curve, giving an apparent pA2 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.|
|Keywords:||Muscle, Smooth; Ileum; Neocortex; Animals; Guinea Pigs; Rats; Rats, Sprague-Dawley; Butyric Acids; Baclofen; Benzofurans; GABA Antagonists; Muscle Contraction; Dose-Response Relationship, Drug; Male; GABA-B Receptor Antagonists|
|Appears in Collections:||Anaesthesia and Intensive Care publications|
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