Selectivity · fingerprint

Bremelanotide: receptor selectivity

Bremelanotide binds MC4R most tightly of the five melanocortin receptors — about 0.25 nM — and prefers it over MC1R by roughly 25×, a selective fingerprint.

By melanocortin.com editorialLast updated 2026
BremelanotideApproved drug
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MC4R-preferring

Primary targetMC4Rappetite · satiety
Selectivity window25×over MC1R
Selective
MC1Rskin · pigment
8.2≈6.3 nM
MC2Radrenal · cortisol
no curated value
MC3Renergy balance
7.3≈50 nM
MC4Rappetite · satiety
9.6≈0.25 nMprimary
MC5Rexocrine glands
7.8≈16 nM

Bars are sized by binding strength (p-value, on a fixed MC1R–MC5R scale);ᵐ marks a mouse value.

A genuine single-receptor lean — one of the few melanocortins that is not broadly promiscuous.

The selectivity window is the fold-gap between a ligand's tightest and second-tightest receptor — a compact measure of how cleanly it picks a target. One caveat it cannot capture: binding is not function. These bars show how tightly Bremelanotide holds each receptor, not what the receptor then does downstream. To put this ligand next to the others, use the selectivity visualizer; for every value with its citation, the binding matrix.

Affinity values from the IUPHAR/BPS Guide to PHARMACOLOGY; the selectivity window is derived from them. Educational resource, not medical advice — see the editorial standards.