AM4113 is a novel cannabinoid CB1 receptor neutral antagonist and reverses the effects of the CB1 agonist AM411. CB1 antagonists like AM4113 are used in the development of treatment for diseases associated with neuronal dendritic abnormalities
am4113, a pyrazole analog structurally related to sr141716 and am251, is a novel cannabinoid cb1 neutral antagonist. am4113 suppressed food intake and food-reinforced behavior in rats.
am4113 was able to bind with high affinity to cb1 receptors, exhibiting 100-fold selectivity for cb1 against cb2 receptors. the ki value for cb1 was 0.897 ± 0.44 nm, while the ki value for hcb2 was 92 ± 6.9 nm [1].
in rats, treatment with am4113 (2.0 and 4.0 mg/kg) attenuated the am411-induced locomotor suppression and analgesia. in addition, 4.0 mg/kg am4113 alone significantly suppressed locomotor activity when compared with vehicle. am4113 dose-dependently decreased lever pressing on an fr1 schedule. am4113 produced conditioned taste avoidance and suppression of ingestive (hedonic) taste reactivity scores in a dose-dependent manner [1]. am4113 didn’t induce signs of nausea [1].
[1] sink k s, mclaughlin p j, wood j a t, et al. the novel cannabinoid cb1 receptor neutral antagonist am4113 suppresses food intake and food-reinforced behavior but does not induce signs of nausea in rats[j]. neuropsychopharmacology, 2008, 33(4): 946-955.
