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Merck

S7936

Sigma-Aldrich

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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About This Item

Fórmula empírica (notación de Hill):
C17H18N2O3S
Número de CAS:
Peso molecular:
330.40
Número MDL:
Código UNSPSC:
12352200
ID de la sustancia en PubChem:
NACRES:
NA.77

Formulario

solid

Nivel de calidad

color

off-white

solubilidad

DMSO: 18 mg/mL
H2O: insoluble

cadena SMILES

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)

Clave InChI

JDTZAGLGBRRCJT-UHFFFAOYSA-N

Aplicación

SB 205384 was used to study GABA-gated currents in rat locus coeruleus neurons.6

Acciones bioquímicas o fisiológicas

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

Información legal

Manufactured and sold under license from GlaxoSmithKline Pharmaceuticals

Código de clase de almacenamiento

11 - Combustible Solids

Clase de riesgo para el agua (WGK)

WGK 3

Punto de inflamabilidad (°F)

Not applicable

Punto de inflamabilidad (°C)

Not applicable

Equipo de protección personal

Eyeshields, Gloves, type N95 (US)


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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
Timothy Ing et al.
The European journal of neuroscience, 25(3), 723-734 (2007-02-23)
Miniature GABA(A) receptor-mediated inhibitory postsynaptic currents (mIPSCs) in cortical pyramidal neurons have previously been categorized into two types: small amplitude mIPSCs with a mono-exponential deactivation (mono-mIPSCs) and relatively larger mIPSCs with bi-exponential deactivation (bi-mIPSCs). The aim of this study was
Laura S Heidelberg et al.
The Journal of pharmacology and experimental therapeutics, 347(1), 235-241 (2013-08-02)
Many drugs used to treat anxiety are positive modulators of GABAA receptors, which mediate fast inhibitory neurotransmission. The GABAA receptors can be assembled from a combination of at least 16 different subunits. The receptor's subunit composition determines its pharmacologic and

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