AZD1940 是一种具有口服活性，高亲和力的大麻素 CB1/CB2 受体激动剂，对 CB1R 和 CB2R 的 pKi 值分别为 7.93 和 9.06，并具有强大的镇痛作用。
AZD1940 is an orally active, high affinity cannabinoid CB1/CB2 receptor agonist with pKi values of 7.93 and 9.06 for human CB1R and CB2R, respectively. AZD1940 shows a robust analgesia action[1][2].
AZD1940 binds with high affinity to human, rat and mouse CB1 and CB2 receptors and displays full agonism at both receptors in all three species[1][2].
When given orally to rats, AZD1940 produces a robust analgesia in different models of inflammatory and neuropathic pain[1][2].For AZD1940, low brain uptake at analgesic doses has been demonstrated in both rats and primates[1].
[1]. Jarkko Kalliom?ki, et al. Evaluation of the analgesic efficacy and psychoactive effects of AZD1940, a novel peripherally acting cannabinoid agonist, in human capsaicin-induced pain and hyperalgesia. Clin Exp Pharmacol Physiol. 2013 Mar;40(3):212-8.
[2]. Magnus Schou, et al. Radiolabeling of the cannabinoid receptor agonist AZD1940 with carbon-11 and PET microdosing in non-human primate. Nucl Med Biol. 2013 Apr;40(3):410-4.
动态评分
0.0