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https://hdl.handle.net/2440/5958
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DC Field | Value | Language |
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dc.contributor.author | Ong, J. | - |
dc.contributor.author | Kerr, D. | - |
dc.contributor.author | Ansar, M. | - |
dc.contributor.author | Vaccher, C. | - |
dc.contributor.author | Berthelot, P. | - |
dc.date.issued | 1998 | - |
dc.identifier.citation | Canadian Journal of Physiology and Pharmacology, 1998; 76(7-8):798-801 | - |
dc.identifier.issn | 0008-4212 | - |
dc.identifier.issn | 1205-7541 | - |
dc.identifier.uri | http://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.statementofresponsibility | Ong, Jennifer ; Kerr, David I. ; Ansar, M'hammed ; Vaccher, Claude ; Berthelot, Pascal | - |
dc.language.iso | en | - |
dc.publisher | Canadian Science Publishing | - |
dc.source.uri | http://dx.doi.org/10.1139/cjpp-76-7-8-798 | - |
dc.subject | Muscle, Smooth | - |
dc.subject | Ileum | - |
dc.subject | Neocortex | - |
dc.subject | Animals | - |
dc.subject | Guinea Pigs | - |
dc.subject | Rats | - |
dc.subject | Rats, Sprague-Dawley | - |
dc.subject | Baclofen | - |
dc.subject | Butyrates | - |
dc.subject | Benzofurans | - |
dc.subject | GABA Antagonists | - |
dc.subject | Muscle Contraction | - |
dc.subject | Dose-Response Relationship, Drug | - |
dc.subject | Male | - |
dc.subject | GABA-B Receptor Antagonists | - |
dc.subject | In Vitro Techniques | - |
dc.title | GABAB receptor antagonism by 7-MBFG, a benzo[b]furan analogue of baclofen, in central and peripheral tissues | - |
dc.type | Journal article | - |
dc.identifier.doi | 10.1139/cjpp-76-7-8-798 | - |
pubs.publication-status | Published | - |
dc.identifier.orcid | Ong, J. [0000-0002-0958-460X] | - |
Appears in Collections: | Anaesthesia and Intensive Care publications Aurora harvest 5 |
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