AM251

AM251 is a potent and selective small molecule antagonist and inverse agonist of the cannabinoid receptor 1 (CB1), with high affinity for CB1 (Ki ≈ 7.5 nM) and significant selectivity over the cannabinoid receptor 2. It is structurally related to rimonabant and has been widely used as a research tool to study endocannabinoid signaling. AM251 acts by blocking or inversely modulating CB1 receptor activity, thereby affecting neurotransmitter release, synaptic plasticity, memory formation, feeding behavior, energy expenditure, and drug-seeking behaviors. In preclinical studies, it has shown effects such as inhibition of cocaine-induced reinstatement of drug-seeking behavior via modulation of glutamate in the nucleus accumbens, reduction in food intake and body weight in obese animal models, impairment of long-term potentiation (LTP), and induction of retrograde amnesia in rats. Additionally, AM251 can act as an agonist at G protein-coupled receptor 55 and may have off-target effects including modulation of tumor cell growth through interactions with estrogen-related receptor alpha (ERRα).

Other names

AM-251AM251AM 251