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Submit ReviewSR 95531 hydrobromide
说明： Competitive and selective GABAA antagonist
别名： Gabazine
化学名： 6-Imino-3-(4-methoxyphenyl)-1(6H)-pyridazinebutanoic acid hydrobromide
纯度： ≥98% (HPLC)
生物活性 for SR 95531 hydrobromide
SR 95531 hydrobromide is a selective, competitive GABAA receptor antagonist and allosteric inhibitor (IC50 = 200 nM). SR 95531 displaces [3H]-GABA from rat brain membranes with a Ki of 150 nM. Unlike Bicuculline (Cat. No. 0130), SR 95531 selectively antagonizes GABA-induced Cl- currents with little action on Pentobarbitone-induced currents (Cat. No. 4579). SR 95531 can act as an agonist at high concentrations (>100 μM) and is a weak agonist at GABAA receptors with α1β2(Y157S)γ2L subunits. SR 95531 also acts as a competitive antagonist of recombinant glycine receptors and exhibits greater potency at glycine receptors containing β subunits.
化合物库 for SR 95531 hydrobromide
SR 95531 hydrobromide is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for SR 95531 hydrobromide
| 分子量 | 368.23 |
| 公式 | C15H17N3O3.HBr |
| 储存 | Store at RT |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 104104-50-9 |
| PubChem ID | 107895 |
| InChI Key | GFZHNFOGCMEYTA-UHFFFAOYSA-N |
| Smiles | Br.COC1=CC=C(C=C1)C1=NN(CCCC(O)=O)C(=N)C=C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for SR 95531 hydrobromide
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| water | 9.21 | 25 | |
| DMSO | 36.82 | 100 |
制备储备液 for SR 95531 hydrobromide
以下数据基于产品分子量 368.23。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.72 mL | 13.58 mL | 27.16 mL |
| 5 mM | 0.54 mL | 2.72 mL | 5.43 mL |
| 10 mM | 0.27 mL | 1.36 mL | 2.72 mL |
| 50 mM | 0.05 mL | 0.27 mL | 0.54 mL |
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产品说明书 for SR 95531 hydrobromide
参考文献 for SR 95531 hydrobromide
参考文献是支持产品生物活性的出版物。
Beato et al (2007) The kinetics of inhibition of rat recombinant heterotrimeric α1β glycine receptors by the low affinity antagonist SR-95531. J.Physiol. 580 171 PMID: 17218350
Heaulme et al (1986) Biochemical characterization of the interaction of three pyridazinyl-GABA derivatives with the GABAA receptor site. Brain Res. 384 224 PMID: 3022866
Uchida et al (1996) The differential antagonism by bicuculline and SR95531 of pentobarbitone-induced currents in cultured hippocampal neurons. Eur.J.Pharmacol. 307 89 PMID: 8831109
Wang and Slaughter (2005) Effects of GABA receptor antagonists on retinal glycine receptors and on homomeric glycine receptor alpha subunits. J.Neurophysiol. 93 3120 PMID: 15728760
Ueno et al (1997) Bicuculline and gabazine are allosteric inhibitors of channel opening of the GABAA receptor. J.Neurosci. 17 625 PMID: 8987785
Bright and Smart (2013) Methods for recording and measuring tonic GABAA receptor-mediated inhibition. Front.Neural Circuits 7 193 PMID: 24367296
If you know of a relevant reference for SR 95531 hydrobromide, please let us know.
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关键词: SR 95531 hydrobromide, SR 95531 hydrobromide supplier, Selective, competitive, GABAA, antagonists, receptors, SR95531, hydrobromide, gabazine, recombinant, glycine, allosteric, inhibitors, Gabazine, Receptors, Glycine, 1262, Tocris Bioscience
171 篇 SR 95531 hydrobromide 的引用文献
引用文献是使用了 Tocris 产品的出版物。 SR 95531 hydrobromide 的部分引用包括：
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SR95531 for slice electrophysiology.
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Anonymous on 01/08/2018
分析类型： Ex Vivo
种属： Mouse
I use SR95531 to block GABAA channels when performing slice electrophysiology.
I use this at a concentration of 10 uM in my aCSF bath.
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