Biological Activity
GABAA receptor antagonist that binds the picrotoxin site and stabilizes the inactive form of the channel via allosteric interaction. Accelerates the decay of GABA-induced Cl- currents with little effect on peak amplitude. Also inhibits 5-HT3A receptors via a similar mechanism.
Technical Data
| M. Wt | 299.37 |
| Formula | C17H21N3O2 |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 152273-12-6 |
| PubChem ID | 197626 |
| InChI Key | NXBSEJKZKXIYMD-UHFFFAOYSA-N |
| Smiles | CC(C)(C)OC(=O)C1=C2N(C=N1)C1=CC=CC=C1NC2(C)C |
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 | |||
| DMSO | 29.94 | 100 | |
| ethanol | 29.94 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 299.37. 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.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.34 mL | 16.7 mL | 33.4 mL |
| 5 mM | 0.67 mL | 3.34 mL | 6.68 mL |
| 10 mM | 0.33 mL | 1.67 mL | 3.34 mL |
| 50 mM | 0.07 mL | 0.33 mL | 0.67 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Dillon et al (1993) U-93631 causes rapid decay of γ-aminobutyric acid-induced chloride currents in recombinant rat γ-aminobutyric acid type A receptors. Mol.Pharmacol. 44 860 PMID: 8232235
Dillon et al (1995) [4-Dimethyl-3-t-butylcarboxyl-4,5-dihydro (1,5-a) quinoxaline] is a novel ligand to the picrotoxin site on GABAA receptors, and decreases single-channel open probability. J.Pharmacol.Exp.Ther. 272 597 PMID: 7531762
Das et al (2003) The GABAA receptor antagonist picrotoxin inhibits 5-hydroxytryptamine type 3A receptors. Neuropharmacology 44 431 PMID: 12646280
Keywords: U 93631, supplier, GABAA, receptor, antagonists, Receptors, U93631, GABAA, Receptors, GABAA, Receptors, Tocris Bioscience
