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Submit ReviewSCH 50911
Description: Selective and competitive GABAB antagonist; orally bioavailable
Chemical Name: (2S)-(+)-5,5-Dimethyl-2-morpholineacetic acid
Purity: ≥98%
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% |
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
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 the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 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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References
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for SCH 50911, please let us know.
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Keywords: SCH 50911, SCH 50911 supplier, Selective, competitive, orally, active, GABAB, antagonist, Receptors, SCH50911, 0984, Tocris Bioscience
10 Citations for SCH 50911
Citations are publications that use Tocris products. Selected citations for SCH 50911 include:
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
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
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
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
Yu et al (2016) Dentate cannabinoid-sensitive interneurons undergo unique and selective strengthening of mutual synaptic inhibition in experimental epilepsy. Neurobiol Dis 89 23 PMID: 26804027
Kreye et al (2016) Human cerebrospinal fluid monoclonal N-MthD.-aspartate receptor autoantibodies are sufficient for encephalitis pathogenesis. Brain 139 2641 PMID: 27543972
Do you know of a great paper that uses SCH 50911 from Tocris? Please let us know.
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