Melanocortin Receptor Biology
PT-141 activates MC3R and MC4R receptors in the hypothalamus and limbic system. Research has used PT-141 as a tool compound to study the melanocortin system's role in CNS-mediated physiological responses.
Overview
What is PT-141?
PT-141 (Bremelanotide) is a cyclic heptapeptide analogue of alpha-MSH that acts as a non-selective melanocortin receptor agonist. Unlike PDE5 inhibitors, PT-141 acts centrally through MC3R and MC4R receptors in the CNS. Research has examined its role in sexual function, appetite regulation, and melanocortin system biology in animal models.
PT-141 (Bremelanotide) is supplied strictly as a reference material for in vitro and preclinical investigation. All characterization data described here is drawn from peer-reviewed literature and laboratory analysis; nothing herein constitutes a claim of clinical effect in humans.
Investigational Scope
Documented Research Areas
The following domains summarize directions explored across published studies and laboratory models. Each reflects observations reported in rodent models, in vitro systems, or the peer-reviewed record.
Sexual Function Models
Animal model studies have examined PT-141's effects on sexual behavior via central MC4R activation, distinct from peripheral vascular mechanisms employed by PDE5 inhibitors.
Energy Balance Research
MC4R is a key regulator of energy homeostasis. Research has examined PT-141's effects on food intake and energy expenditure in rodent models as part of broader melanocortin system research.
Anti-Inflammatory Mechanisms
Melanocortin receptor activation has documented anti-inflammatory properties. Research has examined PT-141's effects on cytokine production in inflammatory models via MC3R-mediated pathways.
Proposed Mechanism
Mechanistic Pathway
Mechanistic steps below are hypothesized from in vitro assays and animal-model data reported in the literature. They describe biochemical interactions observed under controlled experimental conditions.
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1
MC3R & MC4R Agonism
PT-141 binds and activates MC3R and MC4R receptors in the CNS, particularly in the hypothalamus and limbic structures. Receptor activation triggers downstream cAMP signaling and neuronal excitability changes.
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2
Central vs. Peripheral Action
Unlike peripherally acting compounds, PT-141's primary activity is centrally mediated. Research has documented CNS-dependent physiological responses that are abolished by central MC4R antagonism in animal studies.
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3
Dopaminergic System Interaction
Studies have examined PT-141's interaction with dopaminergic pathways in the nucleus accumbens and ventral tegmental area, with observed effects on dopamine release markers in rodent models.
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4
Energy Homeostasis Regulation
MC4R activation by PT-141 reduces food intake and increases energy expenditure in rodent models, consistent with the known role of hypothalamic MC4R in body weight regulation.
Technical Data
Molecular Specifications
| Amino Acid Sequence | Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-OH |
|---|---|
| Molecular Weight | 1,025.2 g/mol |
| Molecular Formula | C₅₀H₆₈N₁₄O₁₀ |
| CAS Number | 189691-06-3 |
| Storage | −20°C long-term, 4°C short-term up to 4 weeks |
References
Selected Literature
The following peer-reviewed references informed the research summaries on this page. Citations are provided for scientific context only.
- Molinoff PB, et al. (2003). PT-141: a melanocortin agonist for the treatment of sexual dysfunction. Annals of the New York Academy of Sciences, 994, 96–102.
- Diamond LE, et al. (2004). A double-blind, placebo-controlled evaluation of the safety, pharmacokinetic properties and pharmacodynamic effects of intranasal PT-141. Journal of Sexual Medicine, 1(1), 10–17.
- Giuliano F, et al. (2010). Experimental evidences for the involvement of the melanocortinergic system in male sexual function. Journal of Andrology, 31(1), 39–44.
- Wikberg JE & Mutulis F. (2008). Targeting melanocortin receptors: an approach to treat weight disorders and sexual dysfunction. Nature Reviews Drug Discovery, 7(4), 307–323.
- King SH, et al. (2007). Melanocortin receptors, melanotropic peptides and penile erection. Current Topics in Medicinal Chemistry, 7(11), 1098–1106.
Research Disclaimer
This product is intended strictly for laboratory research purposes only. It is not a drug, food, cosmetic, or dietary supplement and is not intended to diagnose, treat, cure, or prevent any disease. It is not for human or animal consumption. All information presented is derived from published scientific literature and is provided for educational reference only. By purchasing, the buyer affirms they are a qualified researcher or institution and assume full responsibility for the safe and lawful handling of this material.