PT-141 Signaling Pathway: Structural Comparison of Melanocortin Agonists
PT-141 (Bremelanotide) 2.9 nM 1.1 nM 2.7 cAMP elevation in PVN oxytocin neurons FDA-approved for HSDD (2019) Melanotan II (MT-II) 0.3 nM 0.4 nM 1.1 Broad MC1R–MC5R activation, non-selective Research-grade only, not approved α-MSH (endogenous) 2.0 nM 0.6 nM 0.0
This comparison does not assign a generated winner or score.
- PT-141 (Bremelanotide)
- 2.9 nM
- 1.1 nM
- 2.7
- cAMP elevation in PVN oxytocin neurons
- FDA-approved for HSDD (2019)
- Melanotan II (MT-II)
- 0.3 nM
- 0.4 nM
- 1.1
- Broad MC1R–MC5R activation, non-selective
- Research-grade only, not approved
- α-MSH (endogenous)
- 2.0 nM
- 0.6 nM
- 0.05
- Physiological melanocortin tone regulator
- Endogenous peptide hormone
- Setmelanotide
- >1000 nM
- 0.27 nM
- 2.5
- Selective MC4R agonism, minimal MC3R activity
- FDA-approved for POMC deficiency
- THIQ (synthetic)
- 50 nM
- 0.8 nM
- 4.2
- MC4R-selective, lipophilic blood-brain penetration
- Preclinical investigation only
- Professional Assessment
- PT-141's balanced MC3R/MC4R affinity with moderate selectivity against MC1R/MC2R provides sexual arousal effects without significant pigmentation or cortisol elevation. The clinical sweet spot for melanocortin-based therapies. Longer-acting analogs like THIQ may offer once-weekly dosing but lack human safety data.