S7936
SB 205384
solid
别名:
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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选择尺寸
关于此项目
经验公式（希尔记法）:
C17H18N2O3S
化学文摘社编号:
分子量:
330.40
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
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)
SMILES string
CC#CCOC(=O)c1c(C)nc2sc3CC(O)CCc3c2c1N
InChI key
JDTZAGLGBRRCJT-UHFFFAOYSA-N
form
solid
color
off-white
solubility
DMSO: 18 mg/mL, H2O: insoluble
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
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)
法规信息
新产品
此项目有
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
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
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
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
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
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