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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
Issue Date: 1999
ISSN: 0014-2999
Statement of
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.
RMID: 0030002966
DOI: 10.1016/S0014-2999(99)00047-3
Appears in Collections:Dentistry publications

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