BMS-819881 is a melaninconcentrating hormone receptor 1 (MCHR1) antagonist, which binds rat MCHR1 with a Ki of 7 nM and it also is selective and potent for CYP3A4 activity with an EC50 of 13 μM.
BMS-814580 is a potent and selective functional antagonist (Kb = 117 nM) of human MCHR1. BMS-814580 exhibits potent binding affinity (Ki = 17 nM) for human MCHR1. BMS-814580 also exhibits potent binding affinities for cynomolgus monkey and rat MCHR1 (Ki o
Ac-hMCH(6-16)-NH2 shows non-selective agonist activity towards both MCH-1R and MCH-2R, which are human MCH receptors in the brain. The compound effectively binds to and activates these receptors, with IC 50 values of 0.16 nM and 2.7 nM for MCH-1R and MCH-2R, respectively.