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Submit ReviewSKF 89976A hydrochloride is a potent GABA uptake inhibitor, selective for GAT-1 (IC50 values are 0.13, 550, 944 and 7210 μM for hGAT-1, rGAT-2, hGAT-3 and hBGT-1 respectively). Inhibits transport current competitively (Ki = 7 μM) and transmitter-gated current non-competitively (Ki = 0.03 nM). Able to pass the blood-brain barrier after systemic administration and is active in vivo.
Sold with the permission of GlaxoSmithKline
SKF 89976A hydrochloride is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 371.91 |
公式 | C22H25NO2.HCl |
储存 | Desiccate at +4°C |
纯度 | ≥99% (HPLC) |
CAS Number | 85375-15-1 |
PubChem ID | 6917797 |
InChI Key | SNGGBKYQZVAQKA-UHFFFAOYSA-N |
Smiles | Cl[H].OC(=O)C1CCCN(CC\C=C(\C2=CC=CC=C2)C2=CC=CC=C2)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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
water | 100 温和加热 | ||
DMSO | 37.19 | 100 |
以下数据基于产品分子量 371.91。 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 | 2.69 mL | 13.44 mL | 26.89 mL |
5 mM | 0.54 mL | 2.69 mL | 5.38 mL |
10 mM | 0.27 mL | 1.34 mL | 2.69 mL |
50 mM | 0.05 mL | 0.27 mL | 0.54 mL |
参考文献是支持产品生物活性的出版物。
Ali et al (1985) Orally active and potent inhibitors of γ-aminobutyric acid. J.Med.Chem. 28 653 PMID: 2985785
Krause and Schwarz (2005) Identification and selective inhibition of the channel mode of the neuronal GABA transporter 1. Mol.Pharmacol. 68 1728 PMID: 16150932
Murali Dha (1996) On the bioactive conformation of the GABA uptake inhibitor SK&F 89976-A. Bioorg.Med.Chem.Lett. 6 1535
If you know of a relevant reference for SKF 89976A hydrochloride, please let us know.
关键词: SKF 89976A hydrochloride, SKF 89976A hydrochloride supplier, Potent, GABA, reuptake, inhibitors, inhibits, Penetrates, blood, brain, barrier, GAT-1, Transporters, Monoamine, Neurotransmitter, SKF89976A, hydrochloride, GlaxoSmithKline, GSK, 1081, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 SKF 89976A hydrochloride 的部分引用包括:
Sousa et al (2011) Regulation of hippocampal cannabinoid CB1 receptor actions by adenosine A1 receptors and chronic caffeine administration: implications for the effects of δ9-tetrahydrocannabinol on spatial memory. Neuropsychopharmacology 36 472 PMID: 20927050
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
Written by Ian Martin, Norman Bowery and Susan Dunn, this review provides a history of the GABA receptor, as well as discussing the structure and function of the various subtypes and the clinical potential of receptor modulators; compounds available from Tocris are listed.
The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.