GABAB receptor antagonism by 7-MBFG, a benzo[b]furan analogue of baclofen, in central and peripheral tissues

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dc.contributor.authorOng, J.
dc.contributor.authorKerr, D.
dc.contributor.authorAnsar, M.
dc.contributor.authorVaccher, C.
dc.contributor.authorBerthelot, P.
dc.date.issued1998
dc.description.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.
dc.description.statementofresponsibilityOng, Jennifer ; Kerr, David I. ; Ansar, M'hammed ; Vaccher, Claude ; Berthelot, Pascal
dc.identifier.citationCanadian Journal of Physiology and Pharmacology, 1998; 76(7-8):798-801
dc.identifier.doi10.1139/cjpp-76-7-8-798
dc.identifier.issn0008-4212
dc.identifier.issn1205-7541
dc.identifier.orcidOng, J. [0000-0002-0958-460X]
dc.identifier.urihttp://hdl.handle.net/2440/5958
dc.language.isoen
dc.publisherCanadian Science Publishing
dc.source.urihttps://doi.org/10.1139/cjpp-76-7-8-798
dc.subjectMuscle, Smooth
dc.subjectIleum
dc.subjectNeocortex
dc.subjectAnimals
dc.subjectGuinea Pigs
dc.subjectRats
dc.subjectRats, Sprague-Dawley
dc.subjectBaclofen
dc.subjectButyrates
dc.subjectBenzofurans
dc.subjectGABA Antagonists
dc.subjectMuscle Contraction
dc.subjectDose-Response Relationship, Drug
dc.subjectMale
dc.subjectGABA-B Receptor Antagonists
dc.subjectIn Vitro Techniques
dc.titleGABAB receptor antagonism by 7-MBFG, a benzo[b]furan analogue of baclofen, in central and peripheral tissues
dc.typeJournal article
pubs.publication-statusPublished

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