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Submit ReviewPotent 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.
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.
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
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
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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