Background:
DAMGO is a selective peptide agonist of the µ-opioid receptor (Kis = 1.18, 1,430, and 213 nM for human µ-, δ-, and κ-opioid receptors, respectively).1,2 DAMGO displays higher efficacy than morphine for µ-opioid-induced nociception in rats.3,4
1.Hirning, L.D., Mosberg, H.I., Hurst, R., et al.Studies in vitro with ICI 174,864, [D-Pen2, D-Pen5]-enkephalin (DPDPE) and [D-Ala2, NMePhe4, Gly-ol]-enkephalin (DAGO)Neuropeptides5(4-6)383-386(1985) 2.Zhao, G.-M., Qian, X., Schiller, P.W., et al.Comparison of [Dmt1]DALDA and DAMGO in binding and G protein activation at μ, δ, and κ opioid receptorsJ. Pharmacol. Exp. Ther.307(3)947-954(2003) 3.Fang, F.G., Haws, C.M., Drasner, K., et al.Opioid peptides (DAGO-enkephalin, dynorphin A(1-13), BAM 22P) microinjected into the rat brainstem: Comparison of their antinociceptive effect and their effect on neuronal firing in the rostral ventromedial medullaBrain Res.501(1)116-128(1989) 4.Kelly, E.Efficacy and ligand bias at the μ-opioid receptorBr. J. Pharmacol.169(7)1430-1446(2013)
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