Dimethyltyrosine, the Viagra of Opioids

作     者：Lawrence H. Lazarus Sharon D. Bryant Severo Salvadori Remo Geurrini Gianfranco Balboni Yuko Tsuda Yoshio Okada 

作者机构：Peptide Neurochemistry LCBRA National Institute of Environmental Health Sciences Research Triangle Park NC 27709 USA Department of Pharmaceutical Science University of Ferrara I-44100 Ferrara Italy Department of Pharmaceutical Science University of Ferrara I-44100 Ferrara Italy Department of Toxicology University of Cagliary Cagliary 109126 Italy Faculty of Pharmaceutical Science Kobe Gakuin University Nishi-ku Kobe 651-2180 Japan 

出 版 物：《Chemical Research in Chinese Universities》 (高等学校化学研究（英文版）)

年 卷 期：2006年第22卷第2期

页      面：258-262页

核心收录：

学科分类：081704[工学-应用化学] 07[理学] 08[工学] 0817[工学-化学工程与技术] 070303[理学-有机化学] 0703[理学-化学] 

主　　题：Dimethyltryrosine Opioid Agonist 

摘      要：Introduction The introduction of 2＇ ,6＇-dimethyl-L＇tyrosine （Dmt） at the N-terminus of Tyr-Tic （1,2,3,4-tetra-hydroisoquinoline-3-carboxylic acid ）-containing δ-opioid antagonists enhances receptor affinity and in vitro bioactivity to several orders of magnitude and its application in the formation of ligands with new properties, such as potent inverse agonism. For example, the δ2 agonist,