A-836339 is a cannabinoid CB2 receptor-selective agonist; exhibits high potencies at CB(2) and selectivity over CB(1) receptors.IC50 value: 1.6 nM(EC50) Target: CB2 agonist in vitro: In radioligand binding assays, A-836339 displays high affinities at CB(2) receptors and selectivity over CB(1) receptors in both human and rat.In addition A-836339 exhibits a profile devoid of significant affinity at other G-protein-coupled receptors and ion channels.in vivo: In the complete Freund's adjuvant model of inflammatory pain, A-836339 exhibits a potent CB(2) receptor-mediated antihyperalgesic effect that is independent of CB(1) or mu-opioid receptors. A-836339 has also demonstrated efficacies in the chronic constrain injury (CCI) model of neuropathic pain, skin incision, and capsaicin-induced secondary mechanical hyperalgesia models.Similar to systemic delivery, intra-spinal injection of A-836339 (0.3 and 1 nmol) also attenuated both von Frey-evoked and spontaneous firing of WDR neurons in neuropathic rats. Intra-spinal injections of A-836339 were ineffective in sham rats.Systemic A-836339 and AM1241 produced dose-dependent efficacy in both inflammatory and neuropathic pain models. Local administration of CB? agonists also produced significant analgesic effects in SNL (intra-DRG and i.t.) and CFA (intra-DRG) pain models. Form:Solid
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A-836339
CAS number：959746-77-1 molecular formula：C16H26N2O2S
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| Chinese alias | - | ||
| English alias | CyclopropanecarboxaMide, N-[3-(2-Methoxyethyl)-4,5-diMethyl-2(3H)-thiazolylidene]-2,2,3,3-tetraMethy | SCHEMBL14783506 | UNII-Z6Y1J258EG | MK2206 2HCl | Cyclopropanecarboxamide, N-(3-(2-methoxyethyl)-4,5-dimethyl-2(3H)-thiazolylidene)-2,2,3,3-tetramethyl- | ||
| CAS number | 959746-77-1 | molecular formula | C16H26N2O2S |
| molecular weight | 310.5 g/mol | Exact mass | ≥99% |
| PSA | 67.200 Ų | logp | 3.200 |
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