PT-141 (Bremelanotide) 10 mg

Research Focus: Melanocortin Signaling · MC3R/MC4R Pharmacology · Neuroendocrine Research
Compound Class: Synthetic Melanocortin Receptor Agonist

Mechanism of Action

PT-141, also known as bremelanotide, is a synthetic cyclic peptide and melanocortin receptor agonist derived from research involving α-melanocyte-stimulating hormone (α-MSH) analogs.

Its pharmacological activity is primarily associated with activation of melanocortin receptors, particularly MC4R and MC3R, which are G protein-coupled receptors expressed within multiple regions of the central nervous system.

Activation of melanocortin receptors initiates intracellular signaling primarily through Gs protein-mediated activation of adenylyl cyclase, resulting in increased cyclic adenosine monophosphate (cAMP) and downstream protein kinase A (PKA)-associated signaling.

The MC4 receptor is particularly important to PT-141 research because it participates in central neural circuits associated with autonomic regulation, motivational signaling, energy homeostasis and neuroendocrine physiology.

Unlike compounds that act primarily through peripheral vascular mechanisms, PT-141’s pharmacology is principally associated with central melanocortin signaling.

Product Overview

PT-141 (Bremelanotide) 10 mg is a synthetic cyclic melanocortin receptor agonist developed from research involving melanocortin peptide analogs.

PT-141 is structurally related to Melanotan II, but its development focused on melanocortin-mediated central nervous system signaling rather than pigmentation biology.

Bremelanotide has undergone extensive human clinical investigation and is the active pharmaceutical ingredient in an FDA-approved prescription drug for a specific indication. Its established receptor pharmacology makes PT-141 useful as a research compound for investigating MC3R and MC4R signaling.

Primary Biological Targets & Pathways

• Melanocortin-4 receptor (MC4R)
• Melanocortin-3 receptor (MC3R)
• Central melanocortin signaling
• Gs protein signaling
• Adenylyl cyclase
• Cyclic AMP (cAMP)
• Protein kinase A-associated signaling
• Hypothalamic neural circuitry
• Autonomic nervous system signaling
• Neuroendocrine pathways

Primary Research Applications

PT-141 has been investigated in research involving:

• Melanocortin receptor pharmacology
• MC4R signaling
• MC3R signaling
• Central nervous system peptide signaling
• Neuroendocrine physiology
• Hypothalamic signaling
• Autonomic regulation
• Behavioral neuroscience
• Motivational neural circuitry
• Structure-activity relationships of melanocortin peptides

Scientific Evidence

Evidence Level: ★★★★★ (5 of 5)

Bremelanotide has a considerably stronger human evidence base than most experimental research peptides. Its pharmacology has been characterized through preclinical research, controlled human studies and Phase 3 clinical development.

Bremelanotide is the active pharmaceutical ingredient in an FDA-approved prescription product for a specific medical indication.

However, evidence supporting an FDA-approved pharmaceutical containing bremelanotide should not be interpreted as establishing the safety, efficacy, quality or regulatory status of independently manufactured research-grade PT-141.

Research Highlights

Published research has established that PT-141/bremelanotide:

• Functions as a melanocortin receptor agonist.
• Demonstrates pharmacological activity at MC4R and MC3R.
• Acts primarily through central melanocortin signaling rather than as a peripheral vascular agent.
• Provides a research model for examining MC4R-associated neural circuitry.
• Has progressed through Phase 3 clinical development.

PT-141 vs. Melanotan Peptides

Although PT-141 shares its developmental history with melanocortin peptides such as Melanotan II, the compounds should not be treated as interchangeable. PT-141’s pharmacological emphasis is on MC3R/MC4R signaling and central nervous system activity; Melanotan analogs are more frequently studied in pigmentation and melanogenesis research. Melanocortin receptors perform substantially different functions depending on receptor subtype and tissue distribution.

Research Use Disclaimer

For Laboratory Research Use Only.

This product is intended exclusively for scientific, analytical, and laboratory research. Information presented describes the compound’s molecular biology and findings reported in scientific literature, and should not be interpreted as instructions for administration or as expected outcomes in individuals.

This product is not intended for human consumption, therapeutic administration, diagnosis, treatment, cure, or prevention of disease.

References

• U.S. Food and Drug Administration. Bremelanotide prescribing and regulatory information.
• Kingsberg SA, et al. Phase 3 clinical investigations of bremelanotide.
• Pfaus JG, et al. Research examining melanocortin receptor signaling and bremelanotide pharmacology.
• Molinoff PB, et al. Clinical and pharmacological characterization of PT-141.
• Peer-reviewed literature examining MC3R, MC4R and melanocortin signaling.