[Dmt1, D-1-Nal4]endomorphin-2

[Dmt1, D-1-Nal4]endomorphin-2 is a synthetic peptide analogue of the endogenous mu-opioid receptor (MOR) ligand endomorphin-2. This compound is characterized by the substitution of tyrosine at the first position with 2',6'-dimethyl-L-tyrosine (Dmt) and phenylalanine at the fourth position with D-1-naphthylalanine (D-1-Nal), followed by C-terminal amidation. It serves as a potent and selective MOR antagonist. Research has demonstrated that this peptide can modulate opioid receptor expression and inhibit the proliferation of MCF-7 breast cancer cells, producing an upregulation of MOR gene expression, which is an opposite effect to that of MOR-selective agonists. It is primarily utilized as a pharmacological tool to study the regulation and signaling of opioid receptors in oncological and neurological research.

Other names

[Dmt1, D-1-Nal4]EM-2Dmt(1)-D-1-Nal(4)-endomorphin-2