ATC 0175

An MC1R antagonist (IC50 = 7.23 nM), selective for MC1R over MC2R (IC50 = >10,000 nM) but does antagonize 5-HT2B and 5-HT1A receptors (IC50s = 9.66 and 16.9 nM, respectively), inhibits MCH-induced [35S]GTPgammaS binding and calcium influx in HEK293 cells expressing human MC1R at 3 nM, reduces stress-induced decreases in the time spent in the open arms of the elevated plus maze in mice at 1, 3, and 10 mg/kg, decreases immobility time in the forced swim test in mice. Formulation: A solid. InChI: InChI=1S/C23H25F2N5O.ClH/c1-30(2)21-17-5-3-4-6-20(17)28-23(29-21)27-16-10-8-15(9-11-16)26-22(31)14-7-12-18(24)19(25)13-14,/h3-7,12-13,15-16H,8-11H2,1-2H3,(H,26,31)(H,27,28,29),1H/t15-,16+,. InChIKey: HUUPKFUYSQNNLO-FAESNJTISA-N. SMILES: O=C(C1=CC(F)=C(C=C1)F)N[C@@H](CC2)CC[C@@H]2NC(N=C3N(C)C)=NC4=C3C=CC=C4.Cl