Abstract
This chapter discusses the chemistry and potential therapeutic utilities of melanocortin-4 receptor agonists and antagonists. The melanocortin receptors are a family of five G protein-coupled receptor subtypes–namely, MC1R, MC2R, MC3R, MC4R, and MC5R. Of these five subtypes, the melanocortin-4 receptor (MC4R) is linked to the regulation of energy homeostasis. These melanocortin receptors are activated by α-MSH, β-MSH, γ-MSH, or ACTH, all of which are derived from a single precursor peptide, pro-opiomelancortin. Based upon in situ hybridization studies, MC4R appears to be widely distributed throughout the brain with highest expression in the hypothalamus and dorsal motor nucleus of the vagus in the caudal brainstem. This localization correlates quite well with the brain sites where melanocortin-regulated feeding responses to exogenously applied ligands are shown. The melanocortin agonist precursor, POMC, and an endogenous MC3R/4R antagonist, agouti related protein (AGRP), are also produced in the brain. The chapter discusses MC4R agonists, small molecule MC4R agonists, and MC4R antagonists.
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