AM251 (C09-0734-821)

InformationAM251 block the inhibitory effects of endocannabinoids and synthetic cannabinoid agonists on transmitter release through an action at presynaptic cannabinoid 1 receptors in brain.In vitroAM251 reduces veratridine-dependent (tetrodotoxin suppressible) release of L-glutamic acid and GABA from synaptosomes with IC50 of 8.5 μM and 9.2 μM, respectively. AM251 increases (by 2.3 times) the Kd of radioligand without altering Bmax. AM251 inhibits equilibrium binding by allosterically accelerating the dissociation of the [3H]-batrachotoxinin A 20-alpha-benzoate:sodium channel complex. AM251 reduces cholesteryl ester synthesis in unstimulated and acetylated LDL-stimulated Raw 264.7 macrophages, CB2+/+ and CB2 −/− peritoneal macrophages.In vivoAM251 causes a sustained reduction of daily food intake in the rat. AM251 produces food avoidance and behaviors associated with nausea but does not impair feeding efficiency in rats. AM251 disrupts memory consolidation of the inhibitory avoidance task. AM251 has caused a significative decrease in the test step-down latency when compared to the control group, but no differences are detected in the open field habituation task, including the number of crossings, i.e. there are no motor effects. AM251 (4.0 mg/kg) reduces freezing during a conditioned tone cue played within a novel context.Cell Datacell lines：3T3-SA cellsConcentrations：Incubation Time：Powder Purity:≥99%. Specifications and Purity: 10mM in DMSO. Molecular Formula: C22H21Cl2IN4O. Molecular Weight: 555.24.