PT-141 (Bremelanotide) is a cyclic 7 amino acid peptide, a metabolite of Melanotan II. A selective agonist of melanocortin receptors MC3R and MC4R in the central nervous system, it is studied for its effects on central neurological signaling.
OVERVIEW
PT-141 binding to hypothalamic MC3R and MC4R receptors leads to activation of surrounding neurons, increased immunoreactivity, and potentially to nitric oxide (NO) production in target tissues via the NO-cyclic GMP pathway. This pathway is associated with documented increases in cavernosal pressure in murine models.
A randomized double-blind study suggested that MC4R agonism may elevate desire for up to 24 hours and amplify activity in cerebellar and supplementary motor areas during erotic stimulation.
RESEARCH AREAS
Central MC4R agonism — activation of hypothalamic and limbic neurons; interaction with the medial preoptic area (mPOA) involved in appetitive behaviors.
NO / cGMP pathway — potential increase in cavernosal pressure via neuronal NO release; inhibited by pudendal nerve transection or L-NAME pretreatment.
Selective behavior — increase in solicitation behavior in female rats without impact on lordosis or copulatory pace.
Brain connectivity — amplification of amygdala-insula functional connectivity during erotic stimulation vs. placebo (functional neuroimaging).
CHEMICAL DATA
| Molecular formula | C₅₀H₆₈N₁₄O₁₀ |
| Molecular weight | 1,025.18 g/mol |
| Other names | Bremelanotide, MT-II metabolite |
| Form | Lyophilized powder |
| Purity | >99% HPLC |
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