dalardenol

Dalardenol is a synthetic tetrapeptide analog that functions as a potent agonist of the mu-opioid receptor (MOR). Chemically, it is a modified peptide (D-alanyl-L-arginyl-L-phenylalanyl-L-lysinol) where the C-terminal residue is lysinol, an alcohol derivative of lysine. This structural modification was designed to enhance metabolic stability against enzymatic degradation compared to endogenous opioid peptides. Dalardenol was primarily investigated for its analgesic properties, particularly for the management of severe pain. By selectively binding to mu-opioid receptors in the central nervous system, it inhibits the transmission of pain signals and modulates the perception of pain. Although it demonstrated high potency in preclinical antinociceptive models, particularly via intrathecal administration, the drug has not progressed through late-stage clinical development or achieved regulatory approval.

Other names

D-Alanyl-L-arginyl-L-phenylalanyl-L-lysinoldalardenolum