RO5203648

RO5203648 is a partial agonist of trace amine-associated receptor 1 (TAAR1).¹ It increases cAMP production in HEK293 cells expressing TAAR1 (EC₅₀s = 4, 6.8, 30, and 31 nM for the mouse, rat, human, and monkey receptors, respectively). RO5203648 (500 nM) increases the firing frequency of dopaminergic and serotonergic neurons in the ventral tegmental area (VTA) and dorsal raphe nucleus (DRN) in brain slices from wild-type but not Taar1^-/- mice. It reduces cocaine-induced hyperlocomotion in mice when administered at doses of 1 and 3, but not 10, mg/kg. It also reduces catalepsy induced by haloperidol (Item No. 12014) and reduces immobility time in the forced swim test in rats. RO5203648 (10 mg/kg) increases the percentage of correct responses in an object retrieval task in cynomolgus monkeys and reduces cocaine administration in a self-administration paradigm in rats.

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1. Revel, F.G., Moreau, J.L., Gainetdinov, R.R., et al. Trace amine-associated receptor 1 partial agonism reveals novel paradigm for neuropsychiatric therapeutics. Biol. Psychiatry 72(11), 934-942 (2012).