CB1 antagonist 2

CB1 antagonist 2 (AM4113) is an orally active cannabinoid receptor type 1 (CB1R) antagonist. CB1 antagonist 2 suppresses appetite, reduces body weight, and blocks addictive behaviors such as heroin addiction, without causing adverse effects like nausea and depression that are associated with traditional CB1 inverse agonists. CB1 antagonist 2 can be used in studies related to obesity and opioid addiction^[1][2][3]. In Vitro:CB1 antagonist 2 does not alter Forskolin (HY-15371)-stimulated cAMP formation in in vitro, indicating a lack of inverse agonist profile at CB₁ receptors^[2]. In Vivo:AM4113 (0.3-5.6 mg/kg; i.p.; single administration) causes a dose-dependent reduction in locomotion and rearing behaviors in untreated adult male Sprague-Dawley rats at higher doses; at doses ≥1 mg/kg, it induces a dose-dependent increase in scratching and grooming behaviors in these rats^[1].
AM4113 (0.3-3 mg/kg; i.p.; single administration) dose-dependently antagonizes WIN55,212-2-induced inhibition of spontaneous activity and rearing behavior, prolongation of latency, and circling behavior^[1].
AM4113 (3-10 mg/kg; i.p.; single administration) dose-dependently inhibits heroin self-administration behavior in male Long-Evans rats. At i.p. doses of 3 mg/kg and 10 mg/kg, both the number of heroin infusions and active lever presses decrease with statistical significance^[2].
AM4113 (2-10 mg/kg; i.p.; 14 days) causes a transient, dose-dependent reduction in food intake in rats, which in turn results in sustained, dose-dependent inhibition of body weight gain^[3].
AM4113 (50 mg/kg; p.o.; 7 days) causes a sustained reduction in food intake in rats over 7 days, thereby significantly inhibiting body weight gain^[3].