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Description
PT-141 (Bremelanotide) is a highly potent synthetic peptide analogue of α-MSH that may elicit aphrodisiac effects through stimulation of melanocortin receptors. PT-141 (Bremelanotide) consists of seven amino acids and is a cyclic, shortened lactam variant of alpha-Melanocyte-stimulating hormone (α-MSH), a multifunctional peptide that regulates a broad array of physiological functions. In studies, bremelanotide was shown to induce lordosis in an animal model and was also effective in treating sexual dysfunction in both men (erectile dysfunction or impotence) and women (sexual arousal disorder).
Specification
Name: PT-141
Synonyms: Bremelanotide, PT-141 Acetate
CAS #: 189691-06-3
Molecular Formula: C50H68N14O10
Molecular Mass: 1025.2 Da (g/mol)
Amino Acid Sequence: Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-OH
Purity
PT-141 has a peptide purity level that exceeds 99.0% as determined by HPLC and MS. This peptide was synthesized with no additives and is supplied as a white lyophilized (freeze-dried) powder.
Usage
Bremelanotide, similarly to its analogues α-MSH and melanotan II, acts as a non-selective agonist of all of the melanocortin receptors except MC2, where it lacks significant affinity. Reported activity of the drug is as follows:
MC1 (Ki = 0.68 nM)
MC2 (Ki > 1000 nM)
MC3 (Ki = 72.07 nM)
MC4 (Ki = 19.25 nM)
MC5 (Ki = 166.8 nM)
Bremelanotide appears to stimulate sexual desire and arousal completely or mostly via activation of the MC4 receptor (the MC3 receptor may also be involved). It modulates inflammation and limits ischemia via activation of the MC1 and MC4 receptors.
According to Palatin Technologies' original 2003 patent for bremelanotide, it possesses approximately 50 times the potency of melanotan II as an inducer of erection in male rats. In addition, it was stated in the patent that the therapeutic window of bremelanotide in animals (specifically, the range of induction of the desired sexual arousal relative to the induction of side effects including nausea, yawning, stretching, and decreased appetite) was >1,000-fold, whereas that of melanotan II was only 3- to 4-fold. They concluded that bremelanotide would be more tolerable than melanotan II.
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