SCH 50911

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Cat.No. 0984 - SCH 50911 | C8H15NO3 | CAS No. 733717-87-8
Description: Selective, competitive, orally active GABAB antagonist
Chemical Name: (2S)-(+)-5,5-Dimethyl-2-morpholineacetic acid
Purity: ≥98% (HPLC)
Datasheet
Citations (9)
Literature

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.

Licensing Information

Sold with the permission of Schering Plough Corporation

Technical Data

M. Wt 173.21
Formula C8H15NO3
Storage Desiccate at -20°C
Purity ≥98% (HPLC)
CAS Number 733717-87-8
PubChem ID 5311429
InChI Key SEYCKMQSPUVYEF-LURJTMIESA-N
Smiles [H][C@]1(CC(O)=O)CNC(C)(C)CO1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 17.32 100
phosphate buffered saline 17.32 100

Preparing Stock Solutions

The following data is based on the product molecular weight 173.21. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 5.77 mL 28.87 mL 57.73 mL
5 mM 1.15 mL 5.77 mL 11.55 mL
10 mM 0.58 mL 2.89 mL 5.77 mL
50 mM 0.12 mL 0.58 mL 1.15 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

Bolser et al (1995) The pharmacology of SCH 50911: a novel, orally active GABA-B receptor antagonist. J.Pharmacol.Exp.Ther. 274 1393 PMID: 7562513

Hosford et 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 PMID: 7562514

Ong et al (1998) The morpholino-acetic acid analogue Sch 50911 is a selective GABAB receptor antagonist in rat neocortical slices. Eur.J.Pharmacol. 362 35 PMID: 9865527

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 PMID:


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Keywords: Selective competitive orally active GABAB antagonist Receptors SCH50911 GABAB Receptors

9 Citations for SCH 50911

Citations are publications that use Tocris products. Selected citations for SCH 50911 include:

Kreye et al (2016) Human cerebrospinal fluid monoclonal N-methyl-D-aspartate receptor autoantibodies are sufficient for encephalitis pathogenesis. Brain 139 2641 PMID: 27543972

Jaiswal et al (2015) Reduction in focal ictal activity following transplantation of MGE interneurons requires expression of the GABAA receptor α4 subunit. J Psychopharmacol 9 127 PMID: 25914623

Ding et al (2015) The reinforcing effects of ethanol within the nucleus accumbens shell involve activation of local GABA and serotonin receptors. Br J Pharmacol 29 725 PMID: 25922425

Kitagawa et al (2009) Prediction and validation of a mechanism to control the threshold for inhibitory synaptic plasticity. Mol Syst Biol 5 280 PMID: 19536203

Fritsch et al (2009) Pathological alterations in GABAergic interneurons and reduced tonic inhibition in the basolateral amygdala during epileptogenesis. Neuroscience 163 415 PMID: 19540312

Gryder et al (2005) Evidence for low GluR2 AMPA receptor subunit expression at synapses in the rat basolateral amygdala. Toxins (Basel) 94 1728 PMID: 16045445

Margeta-Mitrovic et al (2001) Ligand-induced signal transduction within heterodimeric GABA(B) receptor. Front Cell Neurosci 98 14643 PMID: 11724957

Wood et al (2000) The human GABA(B1b) and GABA(B2) heterodimeric recombinant receptor shows low sensitivity to phaclofen and saclofen. J Neurochem 131 1050 PMID: 11082110

Vogt and Nicoll (1999) Glutamate and gamma-aminobutyric acid mediate a heterosynaptic depression at mossy fiber synapses in the hippocampus. Proc Natl Acad Sci U S A 96 1118 PMID: 9927703


Do you know of a great paper that uses SCH 50911 from Tocris? If so please let us know.

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