PT-141 (Bremelanotide)
Cyclic MC4R Agonist & CNS Signaling Research Peptide – HPLC Verified
Comprehensive Product Description
PT-141 (Bremelanotide) is a synthetic heptapeptide analogue of the endogenous alpha-melanocyte-stimulating hormone (α-MSH). Chemically identified as Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-OH, this peptide is a deaminated active metabolite of Melanotan 2. mindpeptides synthesizes this compound to provide a highly stable, lyophilized research reagent focused on the study of central nervous system (CNS) modulation.
Unlike phosphodiesterase type 5 (PDE5) inhibitors which act primarily on the vascular system to facilitate blood flow, PT-141 operates directly via the central nervous system. It is a non-selective melanocortin receptor agonist with significant affinity for the MC4R and MC1R receptors. This unique mechanism allows researchers to investigate the neural pathways governing sexual arousal, motivation, and appetite regulation, bypassing the vascular limitations of nitric oxide-dependent pathways.
Mechanism of Action & Signaling Pathways
Central MC4R Activation
The primary pharmacodynamic action of PT-141 involves the activation of Melanocortin-4 Receptors (MC4R) located in the hypothalamus, specifically within the medial preoptic area (mPOA) and the paraventricular nucleus. Upon binding, PT-141 triggers a G-protein coupled signaling cascade that modulates downstream neurotransmitter release, particularly dopamine.
This central activation suggests that PT-141 influences the “appetitive” or motivational aspects of behavior, rather than merely the “consummatory” or physiological mechanics. Furthermore, PT-141 exhibits affinity for MC1R, which is implicated in inflammatory modulation and pigmentation, and MC3R, which plays a role in energy homeostasis. This broad agonist profile makes it a versatile tool for mapping the complex integration of the melanocortinergic system.
Expanded Research Applications
- Hypoactive Sexual Desire Disorder (HSDD):
PT-141 is the primary peptide model for studying centrally mediated sexual dysfunction. It allows for the differentiation between vascular insufficiency and neural signaling deficits in both male and female animal models. - Acute Hemorrhage & Shock:
Research indicates that MC4R agonists like PT-141 can restore hemodynamic stability. Studies in hypovolemic shock models show that administration can elevate mean arterial pressure and heart rate via sympathetic nervous system activation, independent of fluid resuscitation. - Immunomodulation:
Through its interaction with MC1R, PT-141 is being investigated for its potential to modulate the immune system and reduce expression of pro-inflammatory cytokines in response to ischemic insults.
Laboratory Reconstitution Guidelines
mindpeptides supplies PT-141 as a sterile lyophilized powder which requires proper reconstitution prior to use in assays.
- Solvent: Bacteriostatic water or sterile 0.9% NaCl solution is recommended for stability.
- Procedure: Gently inject the solvent down the side of the vial. Do not shake vigorously. Allow the peptide to dissolve at room temperature or with gentle swirling to avoid destroying the cyclic peptide structure.
- Handling: Once reconstituted, keep the vial cold (4°C) if used within days, or freeze at -20°C/-80°C for long-term storage.
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