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S7936

Sigma-Aldrich

SB 205384

solid

Sinonimo/i:

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

Formula empirica (notazione di Hill):
C17H18N2O3S
Numero CAS:
160296-13-9
Peso molecolare:
330.40
Numero MDL:
MFCD00918851
Codice UNSPSC:
12352200
ID PubChem:
24278711
NACRES:
NA.77

Forma fisica

solid

Livello qualitativo

100

Colore

off-white

Solubilità

DMSO: 18 mg/mL
H2O: insoluble

Stringa SMILE

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)
JDTZAGLGBRRCJT-UHFFFAOYSA-N

Applicazioni

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

Azioni biochim/fisiol

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
GABAA receptor modulator selective for the α3β2γ2 subunit combination.

Note legali

Manufactured and sold under license from GlaxoSmithKline Pharmaceuticals

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable

Dispositivi di protezione individuale

Eyeshields, Gloves, type N95 (US)

Certificati d'analisi (COA)

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Sung Kun Chun et al.
Journal of neurophysiology, 104(5), 2321-2328 (2010-09-17)
Adaptive changes in hypothalamic neural circuitry occur in response to alterations in nutritional status. This plasticity at hypothalamic synapses contributes to the control of food intake and body weight. Here we show that genetic ablation of leptin receptor gene expression
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
H J Meadows et al.
British journal of pharmacology, 121(7), 1334-1338 (1997-08-01)
1. 4-Amino-7-hydroxy-2-methyl-5,6,7,8,-tetrahydrobenzo[b]thieno[2,3-b]pyrid ine-3-carboxylic acid, but-2-ynyl ester (SB-205384) and other gamma-aminobutyric acid(A) (GABA(A)) receptor modulators were tested for their effects on GABA-activated chloride currents in rat cerebellar granule cells by use of the whole-cell patch clamp technique. 2. The major effect
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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