ZH8965 is an orally active TAAR1-Gs/Gq agonist (EC50: 6.1/14.8 nM). ZH8965 improves antipsychotic-like phenotypes and cognitive impairment in the MK-801-induced mouse psychosis model. ZH8965 can be used in schizophrenia research.

N-Methylphenethylamine (NMPEA) hydrochloride is a potent TAAR1 agonist. N-Methylphenethylamine hydrochloride also is a trace amine neuromodulator.

RTI-7470-44 is a highly potent and selective antagonist of the human trace amine-associated receptor 1 (hTAAR1), demonstrating an IC50 of 8.4 nM in an in vitro cAMP functional assay. In radioligand binding studies, it exhibits a Ki value of 0.3 nM, highlighting its strong affinity for hTAAR1. Notably, RTI-7470-44 shows significant species selectivity, with over 90-fold preference for hTAAR1 compared to its rat and mouse counterparts. This compound also possesses favorable pharmacokinetic properties, including good blood-brain barrier penetration, moderate metabolic stability, and a promising off-target safety profile. In electrophysiological studies, RTI-7470-44 enhanced the spontaneous firing rate of dopaminergic neurons in the mouse ventral tegmental area (VTA) and effectively counteracted the effects of the TAAR1 agonist RO5166017.

Ulotaront (SEP-363856, SEP-856) is a novel psychotropic agent with agonism at trace amine receptor 1 (TAAR1) and 5-HT1A receptors but no appreciable action at dopamine D2 receptors.Ulotaront significantly reduced the ketamine-induced increase in dopamine synthesis capacity.