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|Title:||Antagonism of GABAB receptors by morpholino-2-acetic acid derivatives Sch 54679 and Sch 51324 in rat brain|
|Citation:||European Journal of Pharmacology, 1999; 369(1):33-37|
|Publisher:||ELSEVIER SCIENCE BV|
|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.|
|Appears in Collections:||Dentistry publications|
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