Bioorganic and Medicinal Chemistry Letters p. 599 - 602 (2005)
Update date:2022-08-02
Topics:
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
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.
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