RO5166017 is an orally active, potent and selective trace amine-associated receptor 1 (TAAR1) agonist for the study of conditioned taste aversion frontal nerve disorders.

RO5166017 exhibits high affinity and potent functional activity against mouse/rat/cynomolgus/human TAAR1 stably expressed in HEK293 cells and demonstrates high selectivity relative to other targets[2].

RO5166017 prevents stress-induced hyperthermia and blocks dopamine-dependent hyperlocomotion in cocaine-treated and dopamine transporter knockout mice, as well as NMDA antagonist-induced hyperactivity[2].Administered orally at doses of 0.01-1 mg/kg, RO5166017 dose-dependently prevents stress-induced hyperthermia in NMRI mice. At doses of 0.1-0.3 mg/kg, RO5166017 exhibits TAAR1-mediated anxiolytic-like properties[2].RO5166017 prevents cocaine-induced hyperlocomotion and inhibits cocaine-induced stereotypies in WT mice, similar to olanzapine, an effect that disappears in Taar1 mice[1].Activation of TAAR1 by RO5166017 increases glucose-dependent insulin secretion in INS1E cells and human islets, and elevates plasma levels of peptide YY (PYY) and glucagon-like peptide 1 (GLP-1) in mice[1]. Chronic treatment of diet-induced obese (DIO) mice with RO5166017 reduces food intake and body weight[1].