Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 45, Issue 21, Pages 4589-4593Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm025539h
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Synthetic and natural peptides that act as nonselective melanocortin receptor agonists have been found to be anorexigenic and to stimulate erectile activity. We report the design and development-of 1, a potent, selective (1184-fold vs MC3R, 350-fold vs MC5R), small-molecule agonist of the MC4 receptor. Pharmacological testing confirms the food intake lowering effects of MC4R agonism and suggests another role for the receptor in the stimulation of erectile activity.
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