AM1241是一种选择性的cannabinoid CB2 receptor激动剂，K_i为3.4 nM，比作用于CB1受体选择性高82倍。在免疫细胞化学研究中，AM1241作用于炎症卡拉胶模型，抑制脊髓Fos蛋白表达，Fos蛋白是神经元活动标记。 AM1241是蛋白兴奋剂，根据多种实验观察不同结果(钙内流, 细胞外信号调节蛋白激酶(ERK)磷酸化和cAMP测量)，在cAMP实验中，当forskolin浓度降低时，拮抗作用变为兴奋作用。在[³H]CP 55,940 竞争性结合实验中，AM1241与人CB2受体高亲和力结合，K_i为7 nM,而与人CB1受体结合亲和力弱80多倍，使用从表达重组人CB2和CB1受体的稳定HEK和CHO细胞系中制备的膜。

>98%

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

(R,S)-AM1241

yellow solid

DMSO ：101 mg/mL (200.66 mM)

CB2,CB1

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 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.

AM-1241 dose-dependently reverses tactile and thermal hypersensitivity produced by ligation of the L5 and L6 spinal nerves in rats. AM-1241 is also active in blocking spinal nerve ligation-induced tactile and thermal hypersensitivity in mice lacking CB1 receptors (CB1-/- mice), confirming that AM-1241 reverses sensory hypersensitivity independent of actions at CB1 receptors. AM-1241 (100, 330 μg/kg i.p.) suppresses the development of carrageenan-evoked thermal and mechanical hyperalgesia and allodynia. And this suppression is blocked by CB2 antagonist SR144528 but not by CB1 antagonist SR141716A. AM1241 produces dose-dependent antinociception to a thermal stimulus applied to the hindpaw, when administered into the hindpaw on the side of testing (ipsilateral i. paw), while much less active into the contralateral to the side. A50 (analgesic dose yielding a 50% effect) of AM1241 is 847 μg/kg with the maximum possible effect (100% MPE) being achieved at 3.3 mg/kg. AM1241 also produces dose-dependent antinociception when administered intraperitoneally (i.p.), with an A50 of 103μg/kg. The antinociceptive actions of AM1241 are blocked by the CB2 receptor-selective antagonist AM630, but not by the CB1 receptor-selective antagonist AM251. AM1241 dosn’t produce the CNS cannabinoid effects of hypothermia, catalepsy, inhibition of activity or impaired ambulation, while this tetrad of effects is produced by the mixed CB1/CB2 receptor agonist WIN55,212-2. Daily injections of AM-1241 through a i.p. route, initiated at symptom onset, increases the survival interval after amyotrophic lateral sclerosis (ALS) onset by 56% in a transgenic mouse model of ALS.