RO5256390

RO5256390 is an orally effective trace amine associated receptor 1 (TAAR1) agonist. RO5256390 exhibits pro-cognitive and antidepressant-like properties in rodent and primate models, showing similar brain activation patterns to Olanzapine (HY-14541). RO5256390 blocks compulsive overeating behavior in rats. RO5256390 can inhibit ATP (HY-B2176)-induced TNF secretion in mouse bone marrow-derived macrophages^[1][2][3]. In Vitro:RO5256390 (0-100 nM; 0-6 h) inhibits ATP (HY-B2176) -induced TNF secretion in mouse bone marrow-derived macrophages in a concentration-dependent manner (IC₅₀ : 19.8 nM), but has no effect on IL-6 secretion^[1].
RO5256390 (0-100 nM; 0-6 h) has no effect on TNF and IL-6 secretion in ADP (HY-W010918) -induced mouse microglia^[1]. In Vivo:RO5256390 (0-15 μg Intracranial administration for 10 minutes; 0-10 mg/kg Intraperitoneal injection for 30 minutes; Single dose) can block compulsive overeating behavior in rats^[2].
RO5256390 (0.03-30 mg/kg; Oral administration; 15-60 minutes) exhibits pro-cognitive and antidepressant-like properties in rodent and primate models. RO5256390 produces a brain activation pattern reminiscent of Olanzapine (HY-14541) in rodents^[3].