PT-141 is a cyclic peptide agonist of melanocortin receptor 4 (MC4R) and an analog of α-melanocyte stimulating hormone .1 It binds to MC3R and MC4R and increases intracellular cAMP levels in HEK293 cells expressing MC4R. It increases dopamine release in the medial preoptic area (mPOA) of the hypothalamus in female rats.2 PT-141 (100 and 200 ?g/kg) increases the number of solicitations, an appetitive sexual behavior, by ovariectomized estrogen- and progesterone-primed female rats. Intranasal administration of PT-141 (50 ?g/kg) induces penile erections in male rats.1 Formulations containing PT-141 have been used in the treatment of hypoactive sexual desire disorder (HSDD) in premenopausal women.
References:
1.Molinoff, P.B., Shadiack, A.M., Earle, D., et al.PT-141: A melanocortin agonist for the treatment of sexual dysfunctionAnn. N. Y. Acad. Sci.994(1)96-102(2003) 2.Pfaus, J., Giuliano, F., and Gelez, H.Bremelanotide: An overview of preclinical CNS effects on female sexual functionJ. Sex Med.4(Suppl 4)269-279(2007)