Non-peptide, melanocortin MC4
receptor antagonist (IC50
values are 320, 810 and 2120 nM for MC4
receptors respectively). Decreases cAMP accumulation in HEK-293 cells expressing the MC4
receptor. Increases food intake and reduces loss of lean body mass in tumor bearing mice. Brain penetrant.
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Peripheral administration of a melanocortin 4-receptor inverse agonist prevents loss of lean body mass in tumor-bearing mice.
Nicholson et al.
Identification of 2-[2-[2-(5-bromo-2- methoxyphenyl)-ethyl]-3-fluorophenyl]-4,5-dihydro-1H-imidazole (ML00253764), a small molecule melanocortin 4 receptor antagonist that effectively reduces tumor-induced weight loss in a mouse model.
Vos et al.
Potent and orally active non-peptide antagonists of the human melanocortin-4 receptor based on a series of trans-2-disubstituted cyclohexylpiperazines.
Tucci et al.