S7936
SB 205384
solid
Sinónimos:
4-Amino-7-hydroxy-2-methyl-5,6,7,8-tetrahydrobenzo[b]thieno[2,3-b]pyridine-3-carboxylic acid but-2-ynyl ester
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Acerca de este artículo
Fórmula empírica (notación de Hill):
C17H18N2O3S
Número CAS:
Peso molecular:
330.40
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
Form:
solid
Servicio técnico
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solid
color
off-white
solubility
DMSO: 18 mg/mL, H2O: insoluble
SMILES string
CC#CCOC(=O)c1c(C)nc2sc3CC(O)CCc3c2c1N
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)
InChI key
JDTZAGLGBRRCJT-UHFFFAOYSA-N
Application
SB 205384 was used to study GABA-gated currents in rat locus coeruleus neurons.6
Biochem/physiol Actions
GABAA receptor modulator selective for the α3β2γ2 subunit combination.
SB 205384 is a selective and positive allosteric modulator of non-benzodiazepine site of the GABAA receptor.3 It affects the extrasynaptic GABAA receptors in rat cortical neurons4 and enhances the GABAergic transmission onto pro-opiomelanocortin neurons in mice.5
Legal Information
Manufactured and sold under license from GlaxoSmithKline Pharmaceuticals
Clase de almacenamiento
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)
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Product Information Sheet
José Francisco Navarro et al.
Psicothema, 20(1), 144-147 (2008-01-22)
GABA-A receptors are involved in the control of aggressive behaviour. Various studies suggest a role for a1-containing GABA-A receptors in modulating aggression. However, the possible involvement of a3 subunit of GABA-A receptors has not been examined. In this study, we
H J Meadows et al.
British journal of pharmacology, 123(6), 1253-1259 (1998-04-29)
1. SB-205384, and its (+) enantiomer (+)-SB-205384 were tested for their modulatory effects on human GABA(A) receptor subunit combinations expressed in Xenopus oocytes by electrophysiological methods. 2. The slowing of the decay rate induced by SB-205384 on native GABA-activated currents
B Hutcheon et al.
The Journal of physiology, 522 Pt 1, 3-17 (2000-01-05)
We examined the maturation of GABAA receptor synapses in cortical pyramidal neurons cultured from embryonic rats. The decay kinetics of GABAA receptor-mediated miniature postsynaptic currents (mPSCs) were compared with those of responses evoked by GABA in excised membrane patches. Fast