PT141 10mg

Description

PT141: A History and Overview

PT-141, also known as Bremelanotide, is a synthetic peptide that has garnered attention for its potential in treating sexual dysfunction in both men and women. Unlike traditional treatments that focus on the vascular system, PT-141 operates through the central nervous system, offering a unique mechanism of action that has shown promise in clinical trials.

PT141 Chemical Composition

• Chemical Structure: PT-141 is a cyclic heptapeptide lactam derivative of alpha-MSH (Melanocyte-Stimulating Hormone). It includes the sequence Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-OH.
• Synonyms: PT 141;VALIDAMINE;6-amino-4-(hydroxymethyl)-4-cyclohexane-[4h,5h]-1,2,3-triol;(1R,2S,3S,4S,6R)-4-Amino-6-(hydroxymethyl)cyclohexane-1,2,3-triol;PT141 acetate (Bremelanotide);[(3S,5R)-2,3,4-trihydroxy-5-(hydroxymethyl)cyclohexyl]ammonium;Pt141 Acetate;Bremelanotide, PT141, Acetate
• CAS: 32780-32-8
• Molecular Formula: The molecular formula for PT-141 reflects its structure as a peptide, indicating the presence of carbon, hydrogen, nitrogen, oxygen, and possibly sulfur atoms.
• Stability: PT-141 is relatively stable at room temperature in its lyophilized (freeze-dried) form. Once reconstituted with sterile water or saline, it should be stored in the refrigerator and used within a few days to maintain its potency.
• Solubility: It is soluble in water and saline, facilitating its administration through subcutaneous injection or nasal spray.
• Mechanism of Action: PT-141 acts on the melanocortin receptors, specifically MC1R and MC4R, in the brain. This action is believed to enhance sexual desire through the central nervous system, a mechanism different from that of PDE5 inhibitors like sildenafil (Viagra).
• Therapeutic Use: It is primarily used for the treatment of sexual dysfunction, including erectile dysfunction in men and sexual arousal disorder in women.
• Efficacy: Clinical trials have demonstrated PT-141’s ability to significantly improve sexual desire and arousal in both men and women, with effects noticeable within minutes to hours after administration.
• Side Effects: Common side effects may include nausea, flushing, headache, and hypertension. The incidence of side effects varies among individuals.
• Legal Status and Availability: As of my last update in April 2023, PT-141 was approved by the FDA in June 2019 under the brand name Vyleesi for the treatment of hypoactive sexual desire disorder (HSDD) in premenopausal women. Its availability and approval status may vary in other countries.
• Shelf Life: 36 months
• Appearance: White lipolyzed powder puck

Discovery and Mechanism

Originally derived from the peptide hormone Melanotan II, which was developed to stimulate melanogenesis, researchers discovered PT-141’s effects on sexual arousal by accident. PT-141 acts on the melanocortin receptors in the brain, specifically the MC4R and MC1R, which play a role in controlling mood and sexual arousal, thereby offering an entirely different approach from PDE5 inhibitors like Viagra and Cialis, which work by increasing blood flow to the genital area.

Clinical Trials and FDA Approval

Clinical trials have demonstrated PT-141’s effectiveness in treating erectile dysfunction (ED) in men and sexual arousal disorder in women. The U.S. Food and Drug Administration (FDA) approved Bremelanotide (PT-141) for premenopausal women with hypoactive sexual desire disorder (HSDD) in June 2019, marking a significant milestone in sexual health treatment options.

How PT141 is Administered

PT-141 is administered via subcutaneous injection, ensuring rapid absorption and effectiveness. Its effects can be noticed within minutes to hours after administration, providing a timely solution for those seeking to enhance their sexual experience.

Potential Benefits

The primary benefit of PT-141 is its ability to enhance sexual desire and arousal without directly affecting the vascular system. This characteristic makes it a viable option for individuals who cannot take traditional ED medications due to contraindications or side effects. Furthermore, its ability to treat sexual dysfunction in women represents a breakthrough in addressing a long-neglected area of sexual health.

Considerations and Side Effects

While PT-141 offers promising benefits, it is not without potential side effects. Commonly reported side effects include nausea, flushing, headache, and temporary increases in blood pressure. These side effects are generally mild and subside on their own. However, as with any medication, it is essential to consult a healthcare provider before starting treatment.

Conclusion

PT-141 represents a novel and exciting approach to treating sexual dysfunction, with the potential to benefit a wide range of individuals. Its unique mechanism of action, effectiveness in both men and women, and FDA approval underscore its potential as a significant advancement in sexual health. As research continues, PT-141 may pave the way for more inclusive and effective treatments for sexual dysfunction.

Referenced Citations

1. PT-141 as a melanocortin agonist for sexual dysfunction treatment: This study discusses PT-141’s mechanism of action through melanocortin receptors MC3-R and MC4-R, primarily expressed in the central nervous system, and its effects on sexual arousal.(https://pubmed.ncbi.nlm.nih.gov/12851303/)
2. Double-blind, placebo-controlled evaluation of PT-141: Focuses on its safety, pharmacokinetic properties, and pharmacodynamic effects in healthy males and patients with mild-to-moderate erectile dysfunction. (https://www.nature.com/articles/3901139)
3. Evaluation of PT-141 in patients unresponsive to Viagra: This research assessed the safety, pharmacokinetics, and pharmacodynamic effects of subcutaneously administered PT-141 in healthy male subjects and ED patients with an inadequate response to Viagra. (https://www.nature.com/articles/3901200)
4. Exploring PT-141 benefits in women’s sexual health: Reviews key research studies on PT-141’s effects on female sexual dysfunction, suggesting its potential as a treatment option. (https://propeptidesource.com/exploring-the-benefits-of-pt-141-in-women%CA%BCs-sexual-health-a-review-of-research-studies/)
5. Co-administration with sildenafil enhances erectile response: Investigated the enhanced erectile response when low doses of PT-141 were administered alongside sildenafil to men with erectile dysfunction. (https://pubmed.ncbi.nlm.nih.gov/15833522/)
6. Erectile Dysfunction Research Trials for PT-141: Describes research trials conducted to determine PT-141’s effectiveness in treating erectile dysfunction, including dosage and side effects. (https://paradigmpeptides.com/2022/05/23/pt-141-erectile-dysfunction-research-trials-for-peptide-therapy/)
7. PT-141 Benefits and Research Applications: Summarizes known research into PT-141, detailing its FDA approval for treating hypoactive sexual desire disorder (HSDD) in women and exploring other potential benefits. (https://www.peptides.org/pt-141-benefits/)