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with the permission of Schering Plough Corporation
Chemical Name:(2S)-(+)-5,5-Dimethyl-2-morpholineacetic acid
Biological Activity:
A selective, competitive and orally
active GABAB antagonist. Displays an IC50 of 1.1 μM
at GABAB, approximately 60 times that of CGP 35348 (Cat. No. 1245)
and no binding affinity for GABAA at concentrations up to 100 μM.
Bolseret al (1995) The pharmacology of SCH 50911: a novel,
orally active GABA-B receptor antagonist. J.Pharmacol.Exp.Ther. 274
1393. Hosfordet al (1995) Characterization of the antiabsence
effects of SCH 50911, a GABAB receptor antagonist, in the lethargic
mouse, γ-hydroxybutyrate, and pentylenetetrazole models. J.Pharmacol.
Exp.Ther. 274 1399. Blythin et al (1996) Substituted
morpholine-2S-acetic acid derivatives: SCH 50911 and related compounds as novel
GABAB antagonists. Bioorg.Med.Chem.Lett. 6 1529. Onget al (1998) The morpholino-acetic acid analogue Sch 50911 is a
selective GABAB receptor antagonist in rat neocortical slices.
Eur.J.Pharmacol. 362 35.
Selective antagonist of neuro-steroid potentiation and direct gating of GABAA receptors. Selectively reduces the effects of 5α-reduced steroids compared to 5β-reduced steroids & displays no effect on potentiation evoked by barbiturates & benzodiazepines. Attenuates 3α,5α-THP-induced loss of righting reflex and total sleep time following i.c.v administration in rats.
