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https://hdl.handle.net/2440/14744
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dc.contributor.author | Ong, J. | - |
dc.contributor.author | Bexis, S. | - |
dc.contributor.author | Marino, V. | - |
dc.contributor.author | Parker, D. | - |
dc.contributor.author | Kerr, D. | - |
dc.contributor.author | Froestl, W. | - |
dc.date.issued | 2001 | - |
dc.identifier.citation | European Journal of Pharmacology, 2001; 415(2-3):191-195 | - |
dc.identifier.issn | 0014-2999 | - |
dc.identifier.issn | 1879-0712 | - |
dc.identifier.uri | http://hdl.handle.net/2440/14744 | - |
dc.description | Copyright © 2001 Elsevier Science B.V. All rights reserved. | - |
dc.description.abstract | In rat neocortical preparations maintained in Mg(2+)-free Krebs medium, baclofen depressed the frequency of spontaneous discharges in a concentration-dependent manner (EC(50) = 6 microM), sensitive to (3-aminopropyl)ethylphosphinic acid (CGP 36216) (100, 300 and 500 microM) (pA(2) = 3.9 +/- 0.1). By contrast, CGP 36216, up to 1 mM, was ineffective in antagonising baclofen-induced hyperpolarisations, mediated through gamma-aminobutyric acid(B) (GABA(B)) postsynaptic receptors. In electrically stimulated brain slices preloaded with [3H]GABA, CGP 36216 increased [3H]GABA release (IC(50) = 43 microM), which was reversed by baclofen (20 microM). While CGP 36216 is ineffective at GABA(B) postsynaptic receptors, it is appreciably more active at presynaptic receptors. | - |
dc.description.statementofresponsibility | Jennifer Ong, Sotiria Bexis, Victor Marino, David A. S. Parker, David I. B. Kerr and Wolfgang Froestl | - |
dc.description.uri | http://www.elsevier.com/wps/find/journaldescription.cws_home/506087/description#description | - |
dc.language.iso | en | - |
dc.publisher | Elsevier Science BV | - |
dc.source.uri | http://dx.doi.org/10.1016/s0014-2999(01)00842-1 | - |
dc.subject | Neocortex | - |
dc.subject | Animals | - |
dc.subject | Rats | - |
dc.subject | Rats, Sprague-Dawley | - |
dc.subject | Phosphinic Acids | - |
dc.subject | gamma-Aminobutyric Acid | - |
dc.subject | Baclofen | - |
dc.subject | Organophosphorus Compounds | - |
dc.subject | Autoreceptors | - |
dc.subject | Receptors, GABA-B | - |
dc.subject | GABA Agonists | - |
dc.subject | GABA Antagonists | - |
dc.subject | Dose-Response Relationship, Drug | - |
dc.subject | Male | - |
dc.title | CGP 36216 is a selective antagonist at GABAB presynaptic receptors in rat brain | - |
dc.type | Journal article | - |
dc.identifier.doi | 10.1016/S0014-2999(01)00842-1 | - |
pubs.publication-status | Published | - |
dc.identifier.orcid | Ong, J. [0000-0002-0958-460X] | - |
Appears in Collections: | Anaesthesia and Intensive Care publications Aurora harvest 2 |
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