| 应用 |
(R,S)-AM1241, a selective CB2 cannabinoid receptor agonist, has been used to study neuropathic pain in animal models |
| 产品介绍 |
AM-1241 is a selective cannabinoid CB2 receptor agonist with Ki of 3.4 nM, exhibits 82-fold selectivity over CB1 receptor. |
| 备注 |
AM-1241 is a selective cannabinoid CB2 receptor agonist with Ki of 3.4 nM, exhibits 82-fold selectivity over CB1 receptor. |
| 生化机理 |
AM-1241 is a protean agonist of CB2 based on the different effect observed in various assays (calcium influx, extracellular signal-regulated kinase (ERK) phosphorylatin and cAMP measurement)) and on the switch from neutral antagonism to agonism in the cAMP assay when forskolin concentration is lowered. In [3H]CP 55,940 competition binding assays, AM-1241 displays high affinity at the human CB2 receptor with a Ki value of about 7 nM, whereas its affinity at the human CB1 receptor is more than 80-fold weaker, using membrane preparations from stable HEK and CHO cell lines expressing the recombinant human CB2 and CB1 receptors, respectively. |
| 别名 |
((R,S)-AM 1241; (R,S)-3-(2-碘-5-硝基苯甲酰)-1-(1-甲基-2-哌啶甲基)-1H-吲哚;(R,S)-AM1241; (R,S)-3-(2-Iodo-5-nitrobenzoyl)-1-(1-methyl-2-piperidinylmethyl)-1H-indole |
