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ID: ALA1144275
Journal: Bioorg Med Chem Lett
Title: Studies on the structure-activity relationship of 2',6'-dimethyl-l-tyrosine (Dmt) derivatives: bioactivity profile of H-Dmt-NH-CH(3).
Authors: Fujita Y, Tsuda Y, Motoyama T, Li T, Miyazaki A, Yokoi T, Sasaki Y, Ambo A, Niizuma H, Jinsmaa Y, Bryant SD, Lazarus LH, Okada Y.
Abstract: The 2',6'-dimethyl-l-tyrosine (Dmt) enhances receptor affinity, functional bioactivity and in vivo analgesia of opioid peptides. To further investigate its direct influence on these opioid parameters, we developed a series of compounds (H-Dmt-NH-X). Among them, H-Dmt-NH-CH(3) showed the highest affinity (K(i)mu=7.45 nM) equal to that of morphine, partial mu-opioid agonism (E(max)=66.6%) in vitro and a moderate antinociception in mice.
CiteXplore: 15664820