Drug intelligence / Profile preview

DAMGO

Development stage
Unknown
Modality
Small Molecules, Peptides
Administration
Intracerebroventricular, Intrathecal, Intra-amygdala, Intravenous
01

Overview

**DAMGO** ([D-Ala², *N*-MePhe⁴, Gly-ol]-enkephalin) is a synthetic opioid peptide agonist with high selectivity for the μ-opioid receptor (MOR), designed as a stable analog of endogenous enkephalins. It exhibits a Kd of approximately 1-3 nM for MOR, with much lower affinity for δ- and κ-opioid receptors (Kd >200 nM), enabling precise study of μ-opioid signaling. Its chemical formula is C₂₆H₃₅N₅O₆ (MW 513.6 Da), and it is supplied as a water-soluble solid (>95% purity) for research use. DAMGO activates G-protein-coupled MOR to inhibit adenylate cyclase, hyperpolarize neurons via potassium channels, and suppress neurotransmitter release, mimicking opioid analgesia. It is widely used in neuroscience to investigate pain modulation, reward, tolerance, and withdrawal in models like rats and planarians, without clinical approval for human therapeutic use.[1][3][7][9]

Other names
[D-Ala2, N-MePhe4, Gly-ol]-enkephalin[D-Ala2,MePhe4,Gly-ol5]-enkephalin
02

Targets

MOR (Mu opioid receptor)

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