PT‑141 (Bremelanotide)

Overview

PT‑141 (bremelanotide) is a cyclic melanocortin receptor agonist derived from α‑MSH analog chemistry. It primarily targets MC4R (with some MC3R activity) within central neural circuits involved in sexual desire and arousal. Experimental and clinical programs have assessed outcomes in female sexual interest/arousal disorder (FSIAD/HSDD) and male erectile function research contexts.

Mechanism of Action (Research Context)

Through MC4R agonism in hypothalamic and limbic pathways, PT‑141 modulates pro‑sexual signaling and motivational states. Unlike agents that improve erection via peripheral nitric‑oxide vasodilation, PT‑141’s effects are centrally mediated, producing responses independent of endothelial function in some cohorts.

Potential Research Benefits (Reported in Literature)

• Desire/interest: Randomized, placebo‑controlled trials report that subjects experienced increased sexual desire and reductions in distress related to low desire.

• Arousal/response: Improvements in validated arousal metrics and satisfying sexual events were observed in selected cohorts; onset windows varied by format and protocol.

• Male erectile response (research contexts): Early studies described increased erectile rigidity and response; centrally mediated effects distinguished it from PDE‑5–based pathways.

• Quality‑of‑life: Several programs reported favorable shifts in patient‑reported outcomes aligned with desire/arousal domains.

• Central mechanism advantage: Activity via MC4R provides a mechanistic alternative where peripheral vasodilation is insufficient.

Potential Reported Side Effects / Adverse Events

The most common events reported by subjects include nausea, flushing, headache, and injection‑site reactions (for parenteral formats). Vomiting, dizziness, and fatigue have been reported; severity is dose‑related. Transient blood‑pressure increases and heart‑rate reductions were documented in controlled settings, leading protocols to exclude uncontrolled hypertension and to implement monitoring. Pigmentary changes are less frequent than with pigmentation‑focused analogs but have been described.

Reported Findings / Key Points

• MC4R‑driven central mechanism distinguishes PT‑141 from peripheral vasodilators.

• Placebo‑controlled data show improvements in desire/arousal outcomes among particular cohorts; effect sizes vary by study.

• Nausea is the most frequent adverse event; mitigation strategies in trials included timing and dose adjustments.

• Hemodynamic effects are typically transient but required protocolized screening/monitoring.

• Early intranasal work informed later subcutaneous programs.

Chemical / Physical Information

• Class: Cyclic heptapeptide melanocortin receptor agonist • Primary targets: MC4R > MC3R (CNS) • Representative sequence family: Nle‑c[Asp‑His‑D‑Phe‑Arg‑Trp‑Lys] (cyclized); terminal groups vary by analog/formulation • General handling (peptide guidance): store lyophilized material at −20 °C, protect from light/moisture; aliquot reconstituted solutions; avoid repeated freeze–thaw.

Notes on Formats Studied

PT‑141 has been explored using intranasal and subcutaneous formats in research. Dosing schedules, onset windows, and outcome measures differ across trials; interpret data within each protocol’s design and population.

Regulatory & Compliance Notes

PT‑141 has been evaluated within regulated frameworks for specific indications. Status, labeling, and risk information differ by jurisdiction and product. All activities should comply with applicable laws and institutional policies.

References (Selection)

• Randomized, placebo‑controlled trials in HSDD/FSIAD cohorts. • Early centrally acting melanocortin agonist studies in male erectile response. • MC4R pharmacology reviews detailing neural circuits of sexual motivation and arousal. • Safety profiles describing nausea, flushing, BP/HR effects, and post‑marketing observations.

Disclaimer

This is only intended for research purposes only. None of this is intended for human consumption. This is only for educational purposes.

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Selected References

PMID: 12831768 — Melanocortin receptor pathways in sexual arousal and neuroregulation

PMID: 16098075 — Bremelanotide (PT-141) mechanisms and MCR agonism

PMID: 19699752 — Central melanocortin signaling and sexual function

PMID: 21198980 — Peptide-based modulation of libido and hypothalamic pathways

Frontiers in Endocrinology — Melanocortin system and neuroendocrine regulation

Journal of Sexual Medicine — Clinical evaluation of melanocortin agonists

Frequently Asked Questions (FAQ)

Q1: What is PT-141 (Bremelanotide)?A1: PT-141, also known as Bremelanotide, is a melanocortin receptor agonist studied for its effects on sexual function pathways, particularly through MC3R and MC4R activity, in research models.

Q2: How does PT-141 work in research?A2: PT-141 is believed to act on central melanocortin receptors involved in arousal-related signaling, rather than directly affecting vascular nitric oxide pathways.

Q3: Is PT-141 approved for general consumer use?A3: Clinical formulations of Bremelanotide exist for specific indications, but the PT-141 discussed in research contexts is not intended for over-the-counter consumer use.

Q4: What are researchers investigating PT-141 for?A4: Research explores PT-141 in models of sexual function, central arousal signaling, and melanocortin-mediated pathways affecting behavior and autonomic responses.

Q5: How is PT-141 different from PDE5-focused compounds in research?A5: Unlike PDE5-focused agents that act mainly on vascular smooth muscle and nitric oxide, PT-141 targets central melanocortin receptors, allowing researchers to study upstream neural pathways.

Q6: How is PT-141 evaluated in studies?A6: PT-141 is assessed in preclinical and clinical research settings that monitor autonomic responses, self-reported endpoints, and melanocortin pathway activity.

Q7: Are there known side effects in PT-141 research?A7: Reported effects in studies can include nausea, flushing, or blood pressure changes, with details varying by dose, route, and protocol.

Related Research Compounds

• Melanotan II

• Dihexa

• GHK-Cu

• BPC-157

• TB-500

• Tesamorelin