GW 405833

Discontinued Product

This product has been withdrawn from sale and is superseded by LEI 101 hydrochloride (Cat. No. 5826)
说明: Selective, high affinity CB2 receptor partial agonist
别名: L-768,242
化学名: 1-(2,3-Dichlorobenzoyl)-5-methoxy-2-methyl-3-[2-(4-morpholinyl)ethyl]-1H-indole
纯度: ≥98% (HPLC)
说明书
引用文献 (4)
评论
文献 (1)

生物活性 for GW 405833

Potent and selective CB2 receptor partial agonist (EC50 = 0.65 nM; maximum inhibition = 44.6%). Binds with high affinity to both human and rat CB2 receptors and displays ~ 1200-fold selectivity over CB1 (Ki values are 3.92 and 4772 nM for human recombinant CB2 and CB1 receptors respectively). Produces potent antihyperalgesic effects in several rodent models of pain.

技术数据 for GW 405833

分子量 447.36
公式 C23H24Cl2N2O3
储存 Store at RT
纯度 ≥98% (HPLC)
CAS Number 180002-83-9
PubChem ID 9911463
InChI Key FSFZRNZSZYDVLI-UHFFFAOYSA-N
Smiles COC1=CC=C2N(C(=O)C3=C(Cl)C(Cl)=CC=C3)C(C)=C(CCN3CCOCC3)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.

产品说明书 for GW 405833

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参考文献 for GW 405833

参考文献是支持产品生物活性的出版物。

Clayton et al (2002) CB1 and CB2 cannabinoid receptors are implicated in inflammatory pain. Pain 96 253 PMID: 11972997

Valenzano et al (2005) Pharmacological and pharmacokinetic characterization of the cannabinoid receptor 2 agonist, GW405833, utilizing rodent models of acute and chronic pain, anxiety, ataxia and catalepsy. Neuropharmacology 48 658 PMID: 15814101

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关键词: GW 405833, GW 405833 supplier, Selective, high, affinity, CB2, receptor, partial, agonists, cannabinoids, Receptors, GW405833, L768242, cb2r, L-768,242, 2374, Tocris Bioscience

4 篇 GW 405833 的引用文献

引用文献是使用了 Tocris 产品的出版物。 GW 405833 的部分引用包括:

Li et al (2017) Cannabinoid CB2 Agonist GW405833 Suppresses Inflammatory and Neuropathic Pain through a CB1 Mechanism that is Independent of CB2 Receptors in Mice. J Pharmacol Exp Ther 362 296 PMID: 28592614

McGuinness et al (2009) Characterizing cannabinoid CB2 receptor ligands using DiscoveRx PathHunter β-arrestin assay. Cardiovasc Res 14 49 PMID: 19171920

Marini et al (2013) Characterization of cannabinoid receptor ligands in tissues natively expressing cannabinoid CB2 receptors. Br J Pharmacol 169 887 PMID: 23711022

Schuelert et al (2010) Paradoxical effects of the cannabinoid CB2 receptor agonist GW405833 on rat osteoarthritic knee joint pain. Osteoarthritis Cartilage 18 1536 PMID: 20863899


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该领域的文献

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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Cannabinoid Receptor Ligands Scientific Review

Cannabinoid Receptor Ligands Scientific Review

Written by Roger Pertwee, this review discusses compounds which affect the activity of the endocannabinoid system, focusing particularly on ligands that are most widely used as experimental tools and denotes compounds available from Tocris.