RTI-7470-44 is a potent and selective antagonist of the human trace amine-associated receptor 1 (TAAR1) which is used in scientific research.

[3][4][5] The affinity (Ki) of RTI-7470-44 for the human TAAR1 is 0.3 nM and its inhibitory potency (IC50Tooltip half-maximal inhibitory concentration) at the receptor is 8.4 nM in vitro.

[4] The compound has favorable in vivo drug-like properties, including good blood–brain barrier permeability, moderate metabolic stability, and a favorable preliminary profile of off-target activity (≥1–10 μM at 42 other targets).

[1][3][4] It is far more potent (893-fold) as an antagonist of the human TAAR1 than the earlier TAAR1 inverse agonist EPPTB in vitro, which has dramatically lower potency (165–272-fold) at the human TAAR1 and rat TAAR1 compared to the mouse TAAR1.

[4] RTI-7470-44 has been found to increase the spontaneous firing rate of dopaminergic neurons in mouse ventral tegmental area (VTA) slices ex vivo and to block the effects of the high-efficacy TAAR1 partial agonist RO5166017 in this system.