Studies on the structure-activity relationship of 2',6'-dimethyl-l-tyrosine (Dmt) derivatives: bioactivity profile of H-Dmt-NH-CH(3) |
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| Authors: | 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 |
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| Institution: | The Graduate School of Food and Medicinal Sciences, Kobe Gakuin University, Nishi-ku, Kobe 651-2180, Japan. |
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| 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. |
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