Compound 22 is a low-potency and non-selective trace amine-associated receptor 1 (TAAR1) antagonist that was identified in 2015 and was further studied in animals in 2018.
[2] Compound 22 increases the firing rate of dopaminergic neurons in mouse ventral tegmental area (VTA) slices ex vivo similarly to the TAAR1 antagonist EPPTB.
[2] Compound 22 decreased basal locomotor activity in mice in vivo significantly by 58% at 5 mg/kg and non-significantly by 26% at 30 mg/kg.
[2] On the basis of the preceding findings, it was concluded that compound 22 augments psychostimulant-induced hyperlocomotion in a manner that is partially or fully independent of TAAR1 antagonism.
[2] Compound 22 was predicted to have good physicochemical and pharmacokinetic properties and to be able to cross the blood–brain barrier.
[2][4] In accordance with predictions, compound showed clear centrally mediated effects in rodents, indicating that it indeed crosses the blood–brain barrier.