PM 226 是一种选择性大麻素 CB2R 激动剂 (Ki (CB2R)\u003d13 nM; EC50 (CB2R)\u003d39 nM; Ki (CB1R) \u003e40 μM;)，在体外和体内具有神经保护特性。
Potent and selective CB2 receptor agonist (Ki = 12.8 nM; EC50 = 38.67 nM). Exhibits negligible affinity for the CB1 receptor (Ki > 40,000 nM) and no activity at the GPR55. Suppresses neuroinflammation by reducing microglial activation in a multiple sclerosis mouse model. BBB permeable; anti-inflammatory and neuroprotective.
Navarro et al (2016) Targeting cannabinoid CB2 receptors in the central nervous system. Medicinal chemistry approaches with focus on neurodegenerative disorders. Front. Neurosci. 10 406 PMID:27679556 |Morales et al (2016) Chromenopyrazole, a versatile cannabinoid scaffold with in vivo activity in a model of multiple sclerosis. J.Med.Chem. 59 6753 PMID:27309150 |Gómez-Ca?as et al (2016) Biological characterization of PM226, a chromenoisoxazole, as a selective CB2 receptor agonist with neuroprotective profile. Pharmacol.Res. 110 205 PMID:27013280
动态评分
0.0