RO5073012 is a selective low-efficacy partial agonist of the trace amine-associated receptor 1 (TAAR1) which has been used in scientific research.

[1][2][3][4] TAAR1 partial agonists like RO5073012 can have agonist- or antagonist-like effects at the TAAR1 depending on the context and level of TAAR1 signaling.

[4] RO5073012 has high affinity for the mouse, rat, cynomolgus monkey, and human TAAR1 (Ki = 0.5–6 nM), is highly potent and selective as an agonist of the TAAR1 of these species (EC50Tooltip half-maximal effective concentration = 8.8–25 nM), and has relatively low intrinsic activity at the TAAR1 of these species (EmaxTooltip maximal efficacy = 24–43% relative to β-phenethylamine).

[6] Conversely however, and in contrast to other TAAR1 partial agonists, RO5073012 non-significantly reduced the locomotor activity induced by amphetamine in normal mice.

[3][1] Amphetamine produces only weak locomotor stimulation in mice with TAAR1 overexpression, and RO5073012, by antagonizing the TAAR1, has been found to restore dextroamphetamine-induced hyperlocomotion in this context.