Description: GABAA receptor 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
Technical Data
Solubility
Calculators
Datasheets
References
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.
Compound Libraries
SB 205384 is also offered as part of the
Tocriscreen Plus. Find out more about compound libraries available from Tocris.
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.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent
Max Conc. mg/mL
Max Conc. mM
Solubility
1eq. HCl
33.04
100
DMSO
16.52
50
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 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
3.03 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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Product Datasheets
Certificate of Analysis / Product Datasheet
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References
References are publications that support the products' biological activity.
Meadowset 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
Meadowset al (1998) SB-205384: a GABAA receptor modulator with novel mechanism of action that shows subunit selectivity. Br.J.Pharmacol. 123 1253 PMID: 9559912
Hutcheonet 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
Heidelberget al (2013) SB-205384 is a positive allosteric modulator of recombinant GABAA receptors containing rat α3, α5, or α6 subunit subtypes coexpressed with 347 235 PMID: 23902941
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