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https://hdl.handle.net/2440/3933
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Type: | Journal article |
Title: | Antagonism of GABAB receptors by morpholino-2-acetic acid derivatives Sch 54679 and Sch 51324 in rat brain |
Author: | Ong, J. Marino, V. Parker, D. Kerr, D. Blythin, D. |
Citation: | European Journal of Pharmacology, 1999; 369(1):33-37 |
Publisher: | ELSEVIER SCIENCE BV |
Issue Date: | 1999 |
ISSN: | 0014-2999 1879-0712 |
Statement of Responsibility: | Jennifer Ong, Victor Marino, David A.S Parker, David I.B Kerr, David J Blythin |
Abstract: | In rat neocortical slices maintained in Mg2+-free Krebs medium, baclofen depressed the rate of spontaneous discharges in a concentration-dependent manner (EC50 = 4.5 microM). This depression was reversibly antagonised by 5-(S,R)-hydroxymethyl-5-methylmorpholinyl-2-(R,S)-acetic acid (Sch 54679) and 2-(R,S)-5-[spirocyclopentyl]-morpholinyl-acetic acid (Sch 51324) (respective pA2 values of 5.8+/-0.15 and 5.4+/-0.2). In electrically-stimulated slices preloaded with [3H]gamma-aminobutyric acid (GABA), Sch 54679 (EC50 = 3 microM) was 2.3 times more potent than Sch 51324 (EC50 = 7 microM) in increasing [3H]GABA release through antagonism of GABA(B) autoreceptors. These structurally novel analogues may be pharmacologically useful for elucidating GABA(B) receptor functions. |
Keywords: | Baclofen GABAB receptor GABAB receptor antagonist Sch 54679 Sch 51324 Neocortical slice, rat |
Rights: | Copyright © 1999 Elsevier Science B.V. All rights reserved. |
DOI: | 10.1016/S0014-2999(99)00047-3 |
Published version: | http://dx.doi.org/10.1016/s0014-2999(99)00047-3 |
Appears in Collections: | Aurora harvest 2 Dentistry publications |
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