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Since 1952, when Gates determined the stereo structure of morphine, numerous groups have focused on discovering a nonnarcotic opioid drug [1]. Although several natural, semisynthetic, and synthetic opioid ligands (alkaloids and peptides) have been developed in clinical studies, very few were nonnarcotic opioid drugs [2]. One of the most important studies in the opioid field appeared in 1976, when...
A highly selective nonpeptidic δ opioid receptor agonist TAN-67, (4aS*, 12aR*)-4a-(3-hydroxyphenyl)-2-methyl-1,2,3,4,4a,5,12,12a-octahydropyrido[3,4-b]acridine was designed on the basis of the message-address concept and the accessory site theory. (−)-TAN-67 is a potent and selective δ1 opioid receptor agonist and shows strong antinociceptive, cardioprotective, and...
We will describe eight interesting reactions using naltrexone derivatives. Almost all these reactions are characteristic of naltrexone derivatives, and can lead to the synthesis of many novel skeletons that provide new interesting pharmacological data. Some of the new reactions that were found with naltrexone derivatives were expanded into general reactions. For example, the reaction of 6α-hydroxyaldehyde...
Recent Advances in the Synthesis of Morphine and Related Alkaloids; by N. Chida * Opioids in Preclinical and Clinical Trials; by H. Nagase and H. Fujii * Synthesis of 14-Alkoxymorphinan Derivatives and Their Pharmacological Actions; by H. Schmidhammer and M. Spetea * 14-Amino-4,5-Epoxymorphinan Derivatives and Their Pharmacological Actions; by J. W. Lewis and S. M. Husbands * Nonpeptidic Delta (δ)...
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