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Melanotan-I

Afamelanotide, MT-I, [Nle4-D-Phe7]-α-MSH, Scenesse, CUV-1647

Quick Stats
Studies 225
Trials 100
2003 pubmed

Stable expression of human melanocortin 3 receptor fused to EGFP in the HEK293 cells.

Rached. Mohamed M; Buronfosse. Anna A; Durand. Philippe P; Begeot. Martine M; Penhoat. Armelle A

Key Findings

  • Stable expression of hMC3R‑EGFP in HEK293 cells with visible surface fluorescence
  • Functional response to NDP‑MSH with EC50 of 0.3 nM and binding Kd of 2.24 nM
  • Agouti‑related protein acts as an antagonist at the hMC3R‑EGFP

Practical Outcomes

  • The study provides a research platform for studying MC3 receptor pharmacology, but it offers no actionable dosing or protocol information for individuals using melanotan‑i. Biohackers should view this as basic science rather than a guide for personal supplementation.

Summary

Scientists created a stable cell line that shows the human MC3 receptor with a fluorescent tag, proving it works like the natural receptor and reacts to specific peptides, but this is a lab tool and doesn’t give any direct advice for personal use of melanotan‑i.

Abstract

Among the melanocortins alpha-MSH is known to be involved in feeding behavior. These hormones mediate their effects through G protein-coupled receptors by stimulating adenylate cyclase. In this study, we have developed an in vitro expression model for human melanocortin 3 receptor (hMC3R) tagged at its C terminus with EGFP. The corresponding chimeric cDNA was stably expressed in HEK293 cells. The selected clones expressing the hMC3R-EGFP exhibited cell surface fluorescence and responded to NDP-MSH stimulation by producing cAMP in a dose-dependent manner (EC(50): 0.3 nM). Binding studies revealed a single class of binding sites with a K(D) of 2.24 nM. Moreover, Agouti-related protein was also demonstrated to be an antagonist of the hMC3R-EGFP. Thus, the hMC3R tagged with EGFP stably expressed in HEK293 cells, exhibiting the same characteristics than the wild-type hMC3R, is the only model of expression of this receptor allowing its direct localization inside living cells.

Study Information

Provider

pubmed

Year

2003

Date

2003-06-20T00:00:00.000Z

DOI

10.1016/s0006-291x(03)00934-3