Biological Activity
AM281 is a selective CB1 receptor antagonist with an IC50 of 9.91 nM. AM281 inhibits CB2 receptor with an IC50 of 13000 nM[1].
In Vitro
AM281 (0.01-10 μM) promotes a concentration dependent increase in 10 μM Aβ 25-35 induced neurotoxicity in SH-SY5Y cells in the presence of 10 μM KSO 1-6[2].
In Vivo
Acute administration (2.5, 5 and 10 mg/kg) of AM281 shortens exploration time and improves memory performance, as does chronic administration (0.62, 1.25 and 2.5 mg/kg) of AM281[3]. Chronic administration of AM281 at 2.5 mg/kg improves recognition index to the 22.1±4.8 and single dose of AM281 at 5 mg/kg improves the memory impairment to the 8.5±4, as compared with vehicle-treated which is 4.8±2.5. Administration of AM281 at a dose of 2.5 mg/kg in chronic form and 5 mg/kg in acute dose improve memory[3]. Animal Model: Male NMRI mice with the weight of 25-30 g[3] Dosage: 0.62, 1.25 and 2.5 mg/kg (chronic administration); 2.5, 5 and 10 mg/kg (acute administration) Administration: Administrated i.p. every day concurrently with morphine except the day of experiment (chronic administration); Singly injected 40 min before second trial (acute administration) Result: The simultaneous daily administration of AM281 with morphine significantly shortened the exploration time, as compared with morphine-dependent mice receiving vehicle. Acute administration at a dose of 5 mg/kg, significantly augmented recognition index.
References & source
Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.