Please use this identifier to cite or link to this item: https://hdl.handle.net/2440/5958
Citations
Scopus Web of ScienceĀ® Altmetric
?
?
Full metadata record
DC FieldValueLanguage
dc.contributor.authorOng, J.-
dc.contributor.authorKerr, D.-
dc.contributor.authorAnsar, M.-
dc.contributor.authorVaccher, C.-
dc.contributor.authorBerthelot, P.-
dc.date.issued1998-
dc.identifier.citationCanadian Journal of Physiology and Pharmacology, 1998; 76(7-8):798-801-
dc.identifier.issn0008-4212-
dc.identifier.issn1205-7541-
dc.identifier.urihttp://hdl.handle.net/2440/5958-
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.language.isoen-
dc.publisherCanadian Science Publishing-
dc.source.urihttp://dx.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-
dc.identifier.doi10.1139/cjpp-76-7-8-798-
pubs.publication-statusPublished-
dc.identifier.orcidOng, J. [0000-0002-0958-460X]-
Appears in Collections:Anaesthesia and Intensive Care publications
Aurora harvest 5

Files in This Item:
There are no files associated with this item.


Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.