Title of article
Studies on the structure–activity relationship of 2′,6′-dimethyl-l-tyrosine (Dmt) derivatives: bioactivity profile of H–Dmt–NH–CH3
Author/Authors
Yoshio Fujita، نويسنده , , Yuko Tsuda، نويسنده , , Takashi Motoyama، نويسنده , , Tingyou Li، نويسنده , , Anna Miyazaki، نويسنده , , Toshio Yokoi، نويسنده , , Yusuke Sasaki، نويسنده , , Akihiro Ambo، نويسنده , , Hideko Niizuma، نويسنده , , Yunden Jinsmaa، نويسنده , , Sharon D. Bryant، نويسنده , , Lawrence H. Lazarus، نويسنده , , Yoshio Okada، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2005
Pages
4
From page
599
To page
602
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–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.
Keywords
structure–activity relationship , DMT , ?-Opioid agonist
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2005
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
795250
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