Description
SB-205384 is a selective and positive GABAA receptor modulator with EC50 values of 280, 695 and 730 nM on α6, α3 and α5-subunit-containing receptors, respectively . g-Aminobutyric acid (GABA) acting on the GABAA receptor can inhibit synaptic transmission in the mammalian central nervous system . Ligands that modulate the function of g-aminobutyric acid A (GABAA) receptor gated chloride channels have hypnotic, anaesthetic, anxiolytic, anticonvulsant and sedative actions . SB-205384 can slow the decay rate on GABAA currents in oocytes expressing human GABAA subunits, which is also seen on native GABA-activated currents in rat neurons . The isoforms containing the a3, a5, and a6 subunits show significantly greater enhancement of the current by SB-205384 and the receptors with the a6-subunit had the greatest sensitivity to SB-205384 . In rat cerebellum granule cells, SB-205384 dramatically pro-longed the half-life for decay of the GABA response in a concentration-dependent manner. The half-life of decay was increased about 10 fold compared with control responses at the highest concentration of SB-205384 used. Also, SB-205384 did not increase the maximum current evoked by 100 mM GABA but the half-life decay was dramatically increased, as saw at the lower dose of 1 mM GABA .
Product information
CAS Number: 160296-13-9
Molecular Weight: 330.40
Formula: C17H18N2O3S
Chemical Name: but-2-yn-1-yl (11S)-3-amino-11-hydroxy-5-methyl-8-thia-6-azatricyclo[7.4.0.0²,⁷]trideca-1(9),2,4,6-tetraene-4-carboxylate
Smiles: CC1N=C2SC3C[C@@H](O)CCC=3C2=C(N)C=1C(=O)OCC#CC
InChiKey: JDTZAGLGBRRCJT-JTQLQIEISA-N
InChi: InChI=1S/C17H18N2O3S/c1-3-4-7-22-17(21)13-9(2)19-16-14(15(13)18)11-6-5-10(20)8-12(11)23-16/h10,20H,5-8H2,1-2H3,(H2,18,19)/t10-/m0/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
Products are for research use only. Not for human use.
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