Description
A TAAR1 agonist; binds to TAAR1 (Kis = 31, 24, 1.9, and 2.7 nM in HEK293 cells expressing the recombinant human, cynomolgus monkey, mouse, or rat enzyme, respectively) and is >15-fold selective for TAAR1 over a panel of 123 receptors, ion channels, and transporters at 10 µM; induces cAMP production in HEK293 cells expressing human, cynomolgus monkey, mouse, or rat TAAR1 (EC50s = 55, 97, 3.3, and 14 nM, respectively); reduces the frequency of neuronal firing in mouse VTA and DRN slices (IC50s = 1.73 and 2.99 nM, respectively); inhibits stress-induced hyperthermia, as well as reduces cocaine-induced hyperlocomotion, in mice; impairs expression of cocaine-induced place preference in rats