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SCH 50911

Catalog #: 0984
10 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
0984/10
0984/50
SCH 50911 | CAS No. 733717-87-8 | GABA-B Receptor Antagonists
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Description: Selective and competitive GABAB antagonist; orally bioavailable

Chemical Name: (2S)-(+)-5,5-Dimethyl-2-morpholineacetic acid

Purity: ≥98%

Product Details
Citations (10)
Supplemental Products
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Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

SCH 50911 is 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.

Technical Data

M.Wt:
173.21
Formula:
C8H15NO3
Solubility:
Soluble to 100 mM in water and to 100 mM in phosphate buffered saline
Purity:
≥98%
Storage:
Desiccate at -20°C
CAS No:
733717-87-8

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:
Sold with the permission of Schering Plough Corporation

Background References

  1. Regulator of G-protein signaling 6 (RGS6) promotes anxiety and depression by attenuating serotonin-mediated activation of the 5-HT(1A) receptor-adenylyl cyclase axis.
    Stewart A, Maity B, Wunsch A, Meng F, Wu Q, Wemmie J, Fisher R
    FASEB J, 2014;28(4):1735-44.
  2. The pharmacology of SCH 50911: a novel, orally active GABA-B receptor antagonist.
    Bolser et al.
    J.Pharmacol.Exp.Ther., 1995;274:1393
  3. Characterization of the antiabsence effects of SCH 50911, a GABAB receptor antagonist, in the lethargic mouse, γ-hydroxybutyrate, and pentylenetetrazole models.
    Hosford et al.
    J.Pharmacol. Exp.Ther., 1995;274:1399
  4. The morpholino-acetic acid analogue Sch 50911 is a selective GABAB receptor antagonist in rat neocortical slices.
    Ong et al.
    Eur.J.Pharmacol., 1998;362:35
  5. Substituted morpholine-2S-acetic acid derivatives: SCH 50911 and related compounds as novel GABAB antagonists.
    Blythin et al.
    Bioorg.Med.Chem.Lett., 1996;6:1529

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Citations for SCH 50911

The citations listed below are publications that use Tocris products. Selected citations for SCH 50911 include:

10 Citations: Showing 1 - 10

  1. Dentate cannabinoid-sensitive interneurons undergo unique and selective strengthening of mutual synaptic inhibition in experimental epilepsy.
    Authors: Yu Et al.
    Neurobiol Dis  2016;89:23
  2. Human cerebrospinal fluid monoclonal N-MthD.-aspartate receptor autoantibodies are sufficient for encephalitis pathogenesis.
    Authors: Kreye Et al.
    Brain  2016;139:2641
  3. Reduction in focal ictal activity following transplantation of MGE interneurons requires expression of the GABAA receptor α4 subunit.
    Authors: Jaiswal Et al.
    J Psychopharmacol  2015;9:127
  4. The reinforcing effects of ethanol within the nucleus accumbens shell involve activation of local GABA and serotonin receptors.
    Authors: Ding Et al.
    Br J Pharmacol  2015;29:725
  5. Prediction and validation of a mechanism to control the threshold for inhibitory synaptic plasticity.
    Authors: Kitagawa Et al.
    Mol Syst Biol  2009;5:280
  6. Pathological alterations in GABAergic interneurons and reduced tonic inhibition in the basolateral amygdala during epileptogenesis.
    Authors: Fritsch Et al.
    Neuroscience  2009;163:415
  7. Evidence for low GluR2 AMPA receptor subunit expression at synapses in the rat basolateral amygdala.
    Authors: Gryder Et al.
    Toxins (Basel)  2005;94:1728
  8. Ligand-induced signal transduction within heterodimeric GABA(B) receptor.
    Authors: Margeta-Mitrovic Et al.
    Front Cell Neurosci  2001;98:14643
  9. The human GABA(B1b) and GABA(B2) heterodimeric recombinant receptor shows low sensitivity to phaclofen and saclofen.
    Authors: Wood Et al.
    J Neurochem  2000;131:1050
  10. Glutamate and gamma-aminobutyric acid mediate a heterosynaptic depression at mossy fiber synapses in the hippocampus.
    Authors: Vogt and Nicoll
    Proc Natl Acad Sci U S A  1999;96:1118

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