928195-92-0Relevant articles and documents
Studies on the structure-activity relationship of 2′,6′- dimethyl-l-tyrosine (Dmt) derivatives: Bioactivity profile of H-Dmt-NH-CH 3
Fujita, Yoshio,Tsuda, Yuko,Motoyama, Takashi,Li, Tingyou,Miyazaki, Anna,Yokoi, Toshio,Sasaki, Yusuke,Ambo, Akihiro,Niizuma, Hideko,Jinsmaa, Yunden,Bryant, Sharon D.,Lazarus, Lawrence H.,Okada, Yoshio
, p. 599 - 602 (2007/10/03)
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-CH3 showed the highest affinity (Kiμ = 7.45 nM) equal to that of morphine, partial μ-opioid agonism (Emax = 66.6%) in vitro and a moderate antinociception in mice.