Discovery of a selective small-molecule melanocortin-4 receptor agonist with efficacy in a pilot study of sexual dysfunction in humans

MI Lansdell, D Hepworth, A Calabrese…

Index: Lansdell, Mark I.; Hepworth, David; Calabrese, Andrew; Brown, Alan D.; Blagg, Julian; Burring, Denise J.; Wilson, Peter; Fradet, David; Brown, T. Bruce; Quinton, Faye; Mistry, Neela; Tang, Kim; Mount, Natalie; Stacey, Peter; Edmunds, Nick; Adams, Cathryn; Gaboardi, Samantha; Neal-Morgan, Stevie; Wayman, Chris; Cole, Susan; Phipps, Joanne; Lewis, Mark; Verrier, Hugh; Gillon, Val; Feeder, Neil; Heatherington, Anne; Sultana, Stefan; Haughie, Scott; Martin, Steven W.; Sudworth, Maria; Tweedy, Sarah Journal of Medicinal Chemistry, 2010 , vol. 53, # 8 p. 3183 - 3197

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Citation Number: 16

Abstract

The relevance of the melanocortin system to sexual activity is well established, and nonselective peptide agonists of the melanocortin receptors have shown evidence of efficacy in human sexual dysfunction. The role of the MC4 receptor subtype has received particular scrutiny, but the sufficiency of its selective activation in potentiating sexual response has remained uncertain owing to conflicting data from studies in preclinical ...