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

dmt-pro-phe-d-2-nal-nh2 (also known as [Dmt1, D-2-Nal4]endomorphin-2) is a synthetic tetrapeptide analog of the endogenous opioid ligand endomorphin-2. It features two key structural modifications: the substitution of tyrosine at the first position with 2',6'-dimethyl-L-tyrosine (Dmt) and the substitution of phenylalanine at the fourth position with D-2-naphthylalanine (D-2-Nal). While native endomorphins are highly selective agonists for the mu-opioid receptor (MOR), these specific modifications convert the peptide into a potent and selective MOR antagonist. This compound has been primarily utilized in preclinical research to investigate the regulation of MOR gene expression and receptor up-regulation. Studies in breast cancer cell lines, such as MCF-7, have demonstrated that this peptide can counteract the down-regulation of MOR expression induced by agonists and influence cell proliferation, suggesting potential applications in studying the intersection of opioid signaling and oncology.

Other names

Dmt-Pro-Phe-D-2-Nal-NH2Dmt-Pro-Phe-D2-Nal-NH2Dmt-Pro-Phe-D 2-Nal-NH2Dmt-Pro-Phe-D-Nal-NH2Dmt-Pro-Phe-D-Nal-NH-2Dmt-Pro-Phe-D-Nal-NH 2