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A Z Ronai

Publications and source records attributed to A Z Ronai.

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Orientation of the oxygen atom at C-6 as a determinant of agonistic activity in the oxymorphone series.

The kinetics of various oxymorphones, their 6-methylene analogs and the 6-hydroxy-epimers corresponding to naloxone and naltrexone have been studied in the longitudinal muscle strip of the guinea-pig ileum. Substitution of the oxygen at C-6 by amethylene group slightly increased antagonistic activity of the resulting structures, without significantly influencing agonistic activity relative to the parent compound. The alpha-orientation of the hydroxy group at C-6 enhanced the agonistic property of both naloxone and naltrexone. The beta-compounds, however, were pure antagonists, with potencies similar to those of the parent keto structures.

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