アラキドニル-2-クロロエチルアミド 化学特性,用途語,生産方法
説明
Arachidonoyl 2-chloroethylamide (ACEA) is a potent and selective cannabinoid (CB) receptor 1 agonist with K
i values of 1.4 and >2,000 nM for CB
1 and CB
2 receptors, respectively. In whole animal experiments, ACEA induces hypothermia in mice with the same efficacy as arachidonoyl ethanolamide (AEA; ), in spite of its higher affinity for the CB
1 receptor. These data have been interpreted to indicate that ACEA may be a substrate for fatty acid amide hydrolase (FAAH), and thus only transiently available in whole animal experiments.
使用
A synthetic agonist of the cannabinoid receptor 1 (CB1R). ACEA is considered to be a selective cannabinoid agonist as it binds primarily to the CB1R and has low affinity to the cannabinoid receptor 2
(CB2R).
生物活性
Potent and highly selective CB 1 receptor agonist (K i = 1.4 nM). Displays > 1400-fold selectivity over CB 2 receptors. Active in vivo . Also available as part of the Cannabinoid CB 1 Receptor Tocriset™ .
酵素阻害剤
This synthetic CB1 receptor agonist and anandamide (N- arachidonylethanolamide) analogue (FW = 365.99 g/mol; CAS 220556-69-4; Symbol: ACEA) is a selective agonist of cannabinoid receptor-1 (Ki = 1.4 nM) but has low affinity to the cannabinoid receptor 2 (Ki = 3.1 μM). ACEA inhibits forskolin-induced cAMP accumulation in Chinese hamster ovary cells expressing the human CB1 receptor. It also increases the binding of [ 35 S]GTPgS to cerebellar membranes and inhibits electrically evoked contractions of the mouse vas deferens. ACEA produces hypothermia in mice, an effect that is inhibited by co-administration of the CB1 receptor antagonist SR141716A.
アラキドニル-2-クロロエチルアミド 上流と下流の製品情報
原材料
準備製品