PT-141 Bremelanotide Review | Buy PT-141 PeptideAdmin
What is PT-141 or Bremelanotide?
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PT-141, also known as Bremelanotide is a cyclic 7-amino acid melanocortin receptor agonist. It is a synthetic analogue of alpha-melanocyte stimulating hormone (α-MSH) and is an active metabolite of Melanotan 2.
It belongs to the same family as that of Melanotan 2 and has the same structure, except that PT-141/Bremelanotide has a hydroxyl group at the end unlike MT2 which has an amide at the end.
Mechanism of Action
PT-141/Bremelanotide works by non-selectively stimulating the melanocortin receptors MC1, MC3, MC4, and MC5. However, it shows high infinity to the MC4 receptor.
Activation of the MC receptors is involved in a number of biological processes including skin pigmentation, sexual arousal, penile erection, appetite suppression, and pain reception.
PT-141/Bremelanotide side effects
The high affinity of PT-141/Bremelanotide to MC4 receptors makes it a viable candidate for treatment of hyposexual disorder, and erectile dysfunction.
A study involving hormone-primed female rats given PT-141/Bremelanotide have shown to have an increased appetitive sexual behaviors. The animal test subjects have been noted to exhibit solicitations, hops and darts, and mounting – all of which indicate sexual arousal.
Melanocortin agonists also increases dopamine release in the medial preoptic area of the brain that is involved in the sexual behavior of both male and female of several species.
A Phase2b clinical trial conducted in 2008 also showed positive effect of PT-141/Bremelanotide in both pre-menopausal and post-menopausal women. Significant improvement in their desire, sexual arousal, and satisfying sexual events (SSEs) have been noted.
As of 2019, Bremelanotide has been approved by the US FDA for treating acquired, generalized hypoactive sexual desire disorder (HSDD) in premenopausal women.
Melanocortin 4 receptors in the central nervous system is linked to modulating erectile dysfunction and sexual arousal. Preclinical experiments on male rats given with Bremelanotide showed consistent initiation of spontaneous penile erection.
Bremelanotide has exhibited pro-erectile effects in adult male rats even through different modes of drug delivery such as intranasal injection. Neuronal activation studies in male rats also suggest that the proerectile effect of Bremelanotide is due to its activity at the MC4 receptors located in the hypothalamus.
A phase 2b clinical trial, also showed that intranasal administration of Bremelanotide in male patients with mild to moderate erectile dysfunction. Bremelanotide showed a 3-fold increase in erectile activity compared to PDE-5 inhibitors such as Viagra.
One of the most documented side effect of Bremelanotide is its ability to increase blood pressure, thus, contraindicated in uncontrolled hypertension and cardiovascular diseases. Other side effects also include nausea, flushing, vomiting and, hyperpigmentation related with use of Bremelanotide for more than 2 months.
When buying Bremelanotide, it is important to choose a pure and high quality one. This will ensure that your research or experiment will yield correct and accurate data. Bremelanotide from Loti Labs are tested via High Performance Liquid Chromatography (HPLC) and Mass Spectrometry to test its purity and quality. Bremelanotide sold from Loti Labs is available in 10mg vials and lyophilized powder form.
Pfaus, J. et al. (2004). Selective facilitation of sexual solicitation in the female rat by a melanocortin receptor agonist. Proceedings of the National Academy of Sciences in the United States of America, 101(27): 10201-10204.
Levine, S. et al. (2008). Phase 2B bremelanotide study in pre- and postmenopausal women with female sexual arousal disorder. Presented at: American College of Obstetricians and Gynecologists 56th Annual Clinical Meeting. New Orleans, LA, USA.
Dhillon, S. & Keam, S. (2019). Bremelanotide: First approval. Drugs, (79): 1599-1606.
Clayton, A. et al. (2016). Bremelanotide for female sexual dysfunctions in premenopausal women: A randomized, placebo-controlled dose-finding trial. Women’s Health – London, 12(3): 325-337.
Diamond, L. et al. (2004). Double-blind, placebo-controlled evaluation of the safety, pharmacokinetic properties and pharmacodynamic effects of intranasal PT-141, a melanocortin receptor agonist, in healthy males and patients with mild-to-moderate erectile dysfunction. International Journal of Impotence Research, 16(1): 51-59.