Ligands of the melanocortin receptors, 2002 – 2003 update

Abstract

α-Melanocyte-stimulating hormone (α-MSH), an endogenous ligand for the melanocortin receptors, has been long recognised as a mediator of numerous physiological processes including, among others, energy homeostasis, immunity, inflammation, sexual function, pigmentation and neurite outgrowth. Compounds mimicking or suppressing actions of α-MSH could therefore be useful in the treatment of many clinically important conditions. Since the cloning of the five melanocortin receptors, medicinal chemistry efforts have centred on the development of melanocortin-4 receptor-specific agonists for the treatment of obesity and erectile dysfunction. Yet, the growing research interest in the other α-MSH functions, reflected in part by the constantly increasing repertoire of ligands specific for the other melanocortin receptors, suggests that some medicinal chemistry efforts might soon be directed towards identification of compounds suitable for treating other diseases. In previous reviews in this journal, the pharmacology of the melanocortin receptors and melanocortin receptor ligands has been discussed in detail. This article will only report the newest ligands, those disclosed in patents published at the end of 2002 and in 2003.

• α-melanocyte-stimulating hormone (MSH)
• cachexia
• depression
• inflammation
• melanocortin receptor
• melanocortin receptor (MCR) ligand
• obesity
• sexual dysfunction