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Submit ReviewSB 205384
Description: GABAA modulator; slows current decay
Chemical Name: 4-Amino-5,6,7,8-tetrahydro-7-hydroxy-2-methyl-[1H]benzothieno[2,3-b]pyridine-3-carboxylic acid 2-butynyl ester
Purity: ≥98% (HPLC)
Biological Activity
GABAA receptor modulator; slows current decay. Potentiates α6, α3 and α5-subunit-containing receptors (EC50 values are 280, 695 and 730 nM respectively). Displays little effect on receptors containing α1 or α2 subunits.
Technical Data
| M. Wt | 330.4 |
| Formula | C17H18N2O3S |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 160296-13-9 |
| PubChem ID | 197690 |
| InChI Key | JDTZAGLGBRRCJT-UHFFFAOYSA-N |
| Smiles | CC#CCOC(=O)C1=C(C)N=C2SC3=C(CCC(O)C3)C2=C1N |
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 | |||
| DMSO | 16.52 | 50 | |
| 1eq. HCl | 33.04 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 330.4. 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 | 3.03 mL | 15.13 mL | 30.27 mL |
| 5 mM | 0.61 mL | 3.03 mL | 6.05 mL |
| 10 mM | 0.3 mL | 1.51 mL | 3.03 mL |
| 50 mM | 0.06 mL | 0.3 mL | 0.61 mL |
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References
References are publications that support the biological activity of the product.
Meadows et al (1997) Effect of SB-205384 on the decay of GABA-activated chloride currents in granule cells cultured from rat cerebellum. Br.J.Pharmacol. 121 1334 PMID: 9257911
Meadows et al (1998) SB-205384: a GABAA receptor modulator with novel mechanism of action that shows subunit selectivity. Br.J.Pharmacol. 123 1253 PMID: 9559912
Hutcheon et al (2000) Developmental change in GABAA receptor desensitization kinetics and its role in synapse function in rat cortical neurons. J.Physiol. 522 3 PMID: 10618148
Heidelberg
et al
(2013)
SB-205384 is a positive allosteric modulator of recombinant GABAA receptors containing rat α3, α5, or α6 subunit subtypes coexpressed with
J.Pharmacol.Exp.Ther. 347
235 PMID: 23902941
If you know of a relevant reference for SB 205384, please let us know.
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Keywords: SB 205384, SB 205384 supplier, GABAA, receptor, modulators, slows, current, decay, Receptors, SB205384, 1512, Tocris Bioscience
2 Citations for SB 205384
Citations are publications that use Tocris products. Selected citations for SB 205384 include:
Miller et al (2010) Quantitative trait locus analysis identifies Gabra3 as a regulator of behavioral despair in mice. Sci Rep 21 247 PMID: 20512339
Heidelberg et al (2013) SB-205384 is a positive allosteric modulator of recombinant GABAA receptors containing rat α3, α5, or α6 subunit subtypes coexpressed with β3 and γ2 subunits. J Pharmacol Exp Ther 347 235 PMID: 23902941
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