Glossary

PT-141 (Bremelanotide)

Compound

PT-141 (Bremelanotide) — A synthetic cyclic heptapeptide melanocortin receptor agonist derived from Melanotan II, studied for melanocortin receptor signaling in research models.

What Is PT-141?

PT-141 (bremelanotide) is a synthetic cyclic heptapeptide with the sequence Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-OH₂. It was originally developed from the melanocortin peptide Melanotan II and has a molecular weight of 1025.18 Da. PT-141 is notable as the first peptide compound shown to activate melanocortin receptors centrally, specifically MC3R and MC4R in the hypothalamus.

Mechanism of Action

Unlike phosphodiesterase inhibitors that act on vascular smooth muscle, PT-141 operates through the central nervous system. It acts as an agonist at melanocortin-3 and melanocortin-4 receptors (MC3R/MC4R) in hypothalamic neurons. Activation of these receptors modulates dopaminergic and oxytocinergic pathways involved in arousal responses.

This central mechanism of action distinguishes PT-141 from peripherally acting compounds and represents a different pharmacological approach in sexual function research. The melanocortin system also plays roles in energy homeostasis, inflammation, and cardiovascular regulation.

Research Background

Melanocortin signaling: PT-141 has been used extensively as a pharmacological tool to study the role of MC3R/MC4R in central nervous system signaling
Sexual function: Preclinical studies demonstrated effects on erectile response in male rats and lordosis behavior in female rats through CNS pathways
Dose-response: Research has characterized dose-dependent activation of melanocortin receptors with documented selectivity profiles
Metabolic research: The melanocortin pathway involvement in energy balance has made PT-141 a tool for studying appetite and metabolism regulation

Storage and Handling

PT-141 is supplied as a white to off-white lyophilized powder. Store at -20°C prior to use. Reconstitute with bacteriostatic water. The peptide is stable in aqueous solution at 2-8°C for up to 14 days. Due to the cyclic structure, PT-141 shows greater stability against enzymatic degradation compared to linear peptides of similar size.

Frequently Asked Questions

What is PT-141 (Bremelanotide)?

A synthetic cyclic heptapeptide melanocortin receptor agonist derived from Melanotan II, studied for melanocortin receptor signaling in research models.

Why is PT-141 (Bremelanotide) important in peptide research?

PT-141 (Bremelanotide) is a fundamental concept in compound as it relates to peptide science. It directly influences experimental design, compound characterization, and the reliability of research outcomes across biochemistry and molecular biology disciplines.

Authority Sources

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