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Review | Regular issue | Vol 85, No. 8, 2012, pp.1821-1867
Published online, 1st May, 2012
DOI: 10.3987/REV-12-738
Design and Synthesis of Novel Opioid Ligands and Their Pharmacologies

Hiroshi Nagase* and Hideaki Fujii

*School of Pharmaceutical Sciences, Kitasato University, 5-9-1, Shirokane, Minato-ku, Tokyo 108-8641, Japan


We describe the recent progress of our investigations in the opioid field in this review, which includes interesting reactions using naltrexone derivatives and pharmacological properties of the synthesized derivatives. Some reactions utilized the characteristic structural features of the morphinan skeleton, and others were applicable to general compounds. Some derivatives were expected to be lead compounds for developing novel ligands selective for the individual opioid receptor types. Triplet drugs consisting of three pharmacophore units in one molecule exhibited interesting pharmacological profiles and would be expected to be a useful tool for clarifying the pharmacology of receptor oligomerization.