Melanocortin 4 receptors play important roles in the regulation of energy homeostasis, eating behavior and sexual functions (1). (3R)-N-[(1R)-1-[(4-Chlorophenyl)methyl]-2-[4-cyclohexyl-4-(1H-1,2,4-triazol-1-ylmethyl)-1-piperidinyl]-2-oxoethyl]-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide is a potent and selective melanocortin 4 receptor agonist (2,3). It inhibits parasympathetic preganglionic neurons in the brainstem and regulates sympathetic and parasympathetic preganglionic neurons.
Potent and selective melanocortin 4 (MC 4 ) receptor agonist (IC 50 values are 1.2, 761 and 2067 nM for human MC 4 , MC 3 and MC 1 receptors respectively). Enhances intracavernosal pressure and stimulates erectile activity in rats ex copula following systemic administration.
