黑皮素类似物在治疗性功能障碍中的研究进展

Potentials of melanocortin analogues for the treatment of erectile dysfunction

黑皮素类似物是目前研究较多的一类治疗性功能障碍的新型药物。现从作用受体亚型、作用位点、作用机制、临床研究结果以及合成方法几方面介绍α-黑素细胞刺激激素(α-MSH)及其类似物黑皮素-Ⅱ(MT-Ⅱ), PT-141等在性功能障碍治疗中的研究进展。目前研究表明,此类化合物可能同时通过MC3R和MC4R对性功能进行调节,而且从脑、脊髓以及外周同时起作用。其中,可通过鼻腔给药的肽类药物PT-141有望弥补西地那非等现有药物的一些不足,成为一种安全、有效的新型性功能障碍治疗药物。

Melanocortin（MC） analogues with diversified bioactivities are becoming one of intensive targets in the development of new agents used to treat erectile dysfunction. Pharmacological researches have defined the role of these analogues in the regulation of MC3R and MC4R, which improve the penile erection by integrating functions of peripheral, supraspinal and spinal origin. One of potential candidates, PT-141 （a nasal spray peptide） , has shown the potential to offer significant safety and efficacy benefits over currently available products in the management of male and female sexual dysfunction. This paper presents the receptor subtypes, acting sites, mechanism of melanocortin and their analogues, e. g, α-MSH, MT- Ⅱ and PT-141, as well as the ongoing clinical trials and synthetic aspects.