RO5166017

RO5166017 is an agonist of trace amine-associated receptor 1 (TAAR1). It binds to TAAR1 (Kis = 31, 24, 1.9, and 2.7 nM in HEK293 cells expressing the recombinant human, cynomolgus monkey, mouse, or rat receptor, respectively) and is greater than 15-fold selective for TAAR1 over a panel of 123 receptors, ion channels, and transporters at 10 µM. RO5166017 induces cAMP production in HEK293 cells expressing the recombinant human, cynomolgus monkey, mouse, or rat TAAR1 (EC50s = 55, 97, 3.3, and 14 nM, respectively). It reduces the frequency of neuronal firing in mouse ventral tegmental area (VTA) and dorsal raphe nucleus (DRN) slices (IC50s = 1.73 and 2.99 nM, respectively), which endogenously express high levels of dopaminergic and serotonergic neurons, respectively. RO5166017 (0.3 mg/kg) inhibits stress-induced hyperthermia, indicating anxiolytic-like activity, as well as reduces cocaine-induced hyperlocomotion, in mice. It also impairs expression, but not reconsolidation, of cocaine-induced place preference in rats.Formal Name: (4S)-2-amino-N-ethyl-4,5-dihydro-N-phenyl-4-oxazolemethanamine. CAS Number: 1048346-74-2. Molecular Formula: C12H17N3O. Formula Weight: 219.3. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMF:PBS (pH 7.2) (1:2): 0.3 mg/ml, DMSO: 10 mg/ml, Ethanol: 10 mg/ml. lambdamax: 253 nm. SMILES: CCN(C1=CC=CC=C1)C[C@H]2COC(N)=N2. InChi Code: InChI=1S/C12H17N3O/c1-2-15(11-6-4-3-5-7-11)8-10-9-16-12(13)14-10/h3-7,10H,2,8-9H2,1H3,(H2,13,14)/t10-/m0/s1. InChi Key: PPONHQQJLWPUPH-JTQLQIEISA-N.