Explore studies of melanotan.
Bremelanotide activates female sexual function through MC3R/MC4R in hypothalamic/limbic sexual circuits, enhancing desire and arousal through dopaminergic and oxytocinergic pathway modulation — the comprehensive CNS mechanism supporting its clinical development for female HSDD.
Pfaus, James; Giuliano, François; Gelez, Hélène · Review
Melanocortin agonists (bremelanotide, melanotan II) treat sexual dysfunction in both sexes through central MC3R/MC4R activation: ED in men and HSDD/FSAD in women — the only drug class targeting desire/arousal centrally for both genders.
Shadiack, Annette M; Sharma, Shubh D; Earle, Dennis C; Spana, Carl; Hallam, Trevor J · Review
Novel macrocyclic melanocortin peptides synthesized by microwave-assisted methods showed potent MC1R/MC4R activity, with the macrocyclic constraint improving receptor selectivity and metabolic stability — advancing circular peptide drugs for melanocortin receptor-mediated therapies.
Grieco, Paolo; Cai, Minying; Liu, Lu; Mayorov, Alexander; Chandler, Kevin; Trivedi, Dev; Lin, Guangxin; Campiglia, Pietro; Novellino, Ettore; Hruby, Victor J · In Vitro
A modified version of the melanotropin peptide Melanotan II (MTII) — called F Peptide — showed superpotent and ultra-prolonged pigmentation activity in frogs. The modification involved replacing arginine at position 8 with lysine and adding a glycine at position 10, expanding the cyclic ring. In vivo testing showed the F Peptide matched MTII's melanotropic potency but lasted significantly longer, making it one of the most sustained-action melanocortin agonists reported.
Gao, Liqian; Yu, Zhiqiang; Meng, Dan; Zheng, Fang; Ong, Yong S; Miao, Peng; Lee, Su S; Wen, Longping · Animal Study
A case of renal infarction (blood flow blockage to the kidney) was reported in a patient using Melanotan II, a non-selective melanocortin receptor agonist used illicitly for skin tanning and sexual enhancement. The renal infarction was most likely attributed to the Melanotan II use. The authors propose two possible mechanisms for the kidney injury: a thrombotic (blood clot) effect from the drug's pharmacological action, and a possible direct toxic effect on kidney tissue. Previous reports had already linked Melanotan II to rhabdomyolysis (muscle breakdown) and kidney failure, and this case adds renal infarction to the list of serious adverse events.
Peters, Björn; Hadimeri, Henrik; Wahlberg, Rebecka; Afghahi, Henri · Case Report
α-MSH mutant zebrafish showed hyperphagic phenotypes and weight gain with upregulated orexigenic genes (NPY, AgRP2, pmch, hcrt) and altered anorexigenic genes. Melanotan II injection completely rescued the hyperphagia, confirming α-MSH as a key appetite regulator.
Hsieh, Yang-Wen; Tsai, Yi-Wen; Lai, Hsin-Hung; Lai, Chi-Yu; Lin, Chiu-Ya; Her, Guor Mour · Preclinical Animal Study (Zebrafish)
MCR agonist D-Tyr MTII: reduced Aβ accumulation, suppressed neuroinflammation, reduced neurotoxic A1 astrocytes, blunted microglial activation while enhancing plaque-associated microglia, and restored impaired hippocampal transcriptome in APP/PS1 mice.
Lau, Jackie K Y; Tian, Min; Shen, Yang; Lau, Shun-Fat; Fu, Wing-Yu; Fu, Amy K Y; Ip, Nancy Y · Animal