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PT-141

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Description

PT-141 (Bremelanotide) description

PT-141 (Bremelanotide) is a cyclic heptapeptide lactam analogue of α-MSH (α-melanocyte-stimulating hormone) with amino acid sequence Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-OH and average elimination half-life 2.7 hours. It is an active metabolite of Melanotan 2 peptide that lacks the C-terminal amide group, however, PT-141 does not significantly stimulate melanogenesis (increased pigment formation) unlike Melanotan 2.

This peptide mainly strongly increases and stimulates libido, sexual arousal and sexual activity in both, men and women. PT-141 can be used as the treatment of generalized hypoactive sexual desire disorder (HSDD), erectile dysfunction (ED) in men (even in men who have not responded to other erectile dysfunction treatments such as Viagra, Cialis etc.) and similar sexual arousal disorders. PT-141 (Bremelanotide) is officially approved for medical use in USA from year 2019.

Mechanism of action and PT-141 (Bremelanotide) results

PT-141 acts as non-selective agonist of the melanocortin receptors, primarily as agonist of melanocortin receptors 3 & 4 (MC3 & MC4) and with the exception of melanocortin receptors 2 (MC2 – the receptor of ACTH). Its bioavailability at subcutaneous injection is about 100%, maximal levels occur after about 1 hour, with a range of 0.5 to 1.0 hours and the plasma protein binding of PT-141 is approx 21%. 

PT-141 (Bremelanotide) chemical structure
PT-141 (Bremelanotide) chemical structure

PT-141 (Bremelanotide) is metabolized via hydrolysis of its peptide bonds; its elimination half-life is about 2.7 hours (with a range of 1.9 to 4.0 hours), and is excreted from the body 64.8% in urine and 22.8% in feces. PT-141 (Bremelanotide) triggers sexual arousal in both men and women within a few minutes of administration, and has been shown its have significant results on male test patients in form of intense and frequent erections, lasting between 2-6 hours. It may also cause a temporary increase in blood pressure and decrease in heart rate after each dose.

PT-141 (Bremelanotide) Contraindications

Due to its effects on blood pressure (generally a transient increase in systolic blood pressure by 6 mmHg, and diastolic blood pressure by 3 mmHg), PT-141 is considered contraindicated in people with uncontrolled high blood pressure or cardiovascular disease. As long as PT-141 is not used more than once in one day, it is not expected to cause more severe increases in blood pressure. It does not meaningfully interact with alcohol (unlike flibanserin for which the interaction with alcohol is a major barrier to its use). Animal experiments, even at high doses, have not revealed any adverse effects of PT-141 on fertility.

Scientifically investigated possible benefits of PT-141

    • Increases libido, sexual desire and arousal in both, men and women
    • Can treat hypoactive sexual desire disorder (HSDD) or erectile dysfunction (ED)
    • Can help treat impotence and premature ejaculation in men
    • Supports intense/hard and long-term erection in men

PT-141 possible side-effects

PT-141 may increase blood pressure: This means that it should not be used by people with high blood pressure or cardiovascular diseases.

And performed clinical trials also have shown that the most commonly reported side effects were:

    • Nausea (40.0% of subjects tested)
    • Flushing, redness in face (20.3%)
    • Pain, irritation or itching at the site of injection (13.2%)
    • Headache (11.3%)
    • Vomiting (4.8%)
    • Cough (3.3%)
    • Fatigue (3.2%)
    • Hot flushes (2.7%)
    • Paresthesia (2.6%)
    • Dizziness (2.2%)

PT-141 (Bremelanotide) FAQ

How long does PT 141 stay in the body active?

Effects of PT-141 Bremelanotide may be felt up to 12 hours from the time of administration and have been known to last for up to 3 days, diminishing each day.

How often can i use PT 141?

The injections are only recommended for use once every 24 hours and no more than 8 times per month.

What can PT 141 treat in men?

In men, PT 141 can effectively treat premature ejaculation, impotence and erectile dysfunction.

Does PT 141 make me tan?

NO: PT-141 does not significantly stimulate melanogenesis (pigment formation) unlike Melanotan 2.

Increases PT-141 sexual desire for both men and women?

YES: PT-141 Bremelanotide increases sexual desire for both men and women.

Can I take PT-141 if I have high blood pressure?

NO: You should not use PT-141 Bremelanotide peptides if you have high blood pressure

Causes PT-141 redness in the face?

YES, MAY: Temporary flushing and redness in face is a relatively common temporary side effect after administration of PT-141 (20.3% reported in clinical studies)

PT-141 (Bremelanotide) dosage

PT-141 Bremelanotide use is only recommended in those who have the condition without an underlying cause, such as medical, psychiatric, or relationship problems; and it should not be used by people with high blood pressure or cardiovascular diseases.

PT-141 Bremelanotide should be used at least 30-40 minutes before anticipated sexual activity. In the scientific studies and clinical trials performed, these quantities are often mentioned:

    • 500 mcg of PT-141 as a test dose or on first use
    • 1000 mcg (1 mg) of PT-141 as a standard dose
    • 1500 mcg of PT-141 as a strong dose for a strong effect

Only 1 dose per 24 hours or no more than 8 doses per month is recommended, and it should be stopped after 8 weeks if there is no improvement in sexual desire and associated distress.

Effects of PT-141 Bremelanotide may be felt up to 12 hours from the time of administration and have been known to last for up to 3 days, diminishing each day.

Overview

Cyclic heptapeptide PT-141 (Bremelanotide) is analogue of α-MSH (α-melanocyte-stimulating hormone) derived from peptide Melanotan 2. However, PT-141 does not significantly stimulate melanogenesis (increased pigment formation) unlike Melanotan 2. PT-141 (Bremelanotide) peptide mainly strongly increases and stimulates libido and sexual arousal, and can be used as the treatment of sexual arousal disorders in both, men and women. It is officially approved for medical use in USA from year 2019. But due to its negative effects on blood pressure, PT-141 should not be used by people with high blood pressure or cardiovascular diseases.

Additional information

Synonyms

Bremelanotide, Vyleesi, Rekynda

Catalogue number

PT-7485621

Molecular formula

C50H68N14O10

Molecular weight

1025.2 g/mol

Amount of active substance

10 mg

Purity

> 98%

Format

Sterile filtered white lyophilized freeze-dried powder

Formulation

The protein/peptide was lyophilized with no additives

Source

Synthetic

Stability and storage

Stable at room temperature for 3 weeks. Recommended long-term storage dried below -18 °C, upon reconstitution peptide should be stored at 4°C between 3-10 days.

Solubility

Recommended to reconstitute the lyophilized peptide in 18MΩ-cm sterile water (not less than 100 µg/ml)

Restrictions

Sold for the scientific research use only

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