描述
PT-141（Bremelanotide）是α-MSH的高效合成肽类似物，可通过刺激黑皮质素受体引起壮阳药效应。 PT-141（Bremeranotide）由7个氨基酸组成，是一种α - 黑素激素激素（α-MSH）的循环，缩短的内酰胺变体，它是调节广泛生理功能的多功能肽。在研究中，bremelanotide被证明在动物模型中诱发脊柱前凸，并且也有效治疗男性（勃起功能障碍或阳ence）和女性（性唤起性障碍）的性功能障碍。al disorder).

规范
名称：PT-141
同义词：Bremelanotide，PT-141 Acetate
cas＃：189691-06-3
分子式：C50H68N14O10
分子质量：1025.2Da（g / mol）
氨基酸序列：Ac-Nle-cyclo'Asp-His-D-Phe-Arg-Trp-Lys'-OH

纯度
通过HPLC和MS测定，PT-141的肽纯度水平超过99.0％。该肽不用添加剂合成，并以白色冻干（冷冻干燥）粉末的形式提供。

用法
Bremeranotide类似于其类似物α-MSH和黑素素II，作为除MC2之外的所有黑皮质素受体的非选择性激动剂，其缺乏显着的亲和力。报告的药物活动如下：ollows：ollows:
mc1（ki = 0.68nm）
mc2（ki> 1000nm）nm）
mc3（ki = 72.07nm）
mc4（ki = 19.25nm）
mc5（ki = 166.8nm）
Bremelanotide似乎完全或主要通过激活MC4受体刺激性欲和唤醒（也可能涉及MC3受体）。它通过激活MC1和MC4受体来调节炎症并限制缺血。
根据Palatin Technologies的原始2003年的褐豆黄素专利，它具有大约50倍黑色素II作为雄性大鼠勃起诱导剂的效力。此外，专利中还指出，布鲁梅肽在动物中的治疗窗口（具体地说，相对于包括恶心，打呵欠，拉伸和食欲降低的副作用诱发的期望的性唤起的诱导范围）大于1,000而黑素II的浓度仅为3-4倍。他们得出的结论是，黑曲霉素可能比黑色素II更耐受。 II。

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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).al disorder).al 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:ollows:ollows:
MC1 (Ki = 0.68 nM)
MC2 (Ki ﹥ 1000 nM) 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. II.

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