英和和英

出典:『Wikipedia』 (2011/02/28 02:04 UTC 版)

英語による解説

引用

AM-1221 is a drug which acts as a potent and selective agonist for the cannabinoid receptor CB2, with a Ki of 0.28nM at CB₂ and 52.3nM at the CB1 receptor, giving it around 180x selectivity for CB₂. The 2-methyl and 6-nitro groups on the indole ring both tend to increase CB₂ affinity while generally reducing affinity at CB₁, explaining the high CB₂ selectivity of AM-1221. However despite this relatively high selectivity for CB₂, its CB₁ affinity is still too high to make it useful as a truly selective CB₂ agonist, so the related compound AM-1241 is generally preferred for research purposes.