1357266-05-7

RO 5263397 is a trace amine-associated receptor 1 agonist (TAAR1).

RO5256390 is an orally available partial agonist th at targets trace amine-associated receptor 1 (TAAR1) with high affinity (Ki in nM = 0.9/mouse4.1/human9.1/rat24/monkey TARR1)potency (EC50 in nM/relative efficacy with respect to β-phenylethylamine = 1.3/0.59/mouse17/0.81/human47/0.76/rat251/0.85/monkey TARR1-dependent cellular cAMP production)and selectivity (by a 112-receptor/channel/transporter and a 42-enzyme panel)without agonistic activity toward mouse TAAR4-expressing cells even at a high concentration of 30 μM. When applied via oral administration (0.003-1 mg/kg)RO5256390 exhibits similar in vivo efficacy as the full agonist RO5256390 in blocking psychostimulants-induced hyperlocomotion in mice.