14β-Arylpropiolylamino-17-cyclopropylmethyl-7, 8-dihydronormorphinones and Related Opioids. Further Examples of Pseudoirreversible μ Opioid Receptor …

…, D Rennison, JH Broadbear, L Purington…

Index: Nieland, Nick P.R.; Rennison, David; Broadbear, Jillian H.; Purington, Lauren; Woods, James H.; Traynor, John R.; Lewis, John W.; Husbands, Stephen M. Journal of Medicinal Chemistry, 2009 , vol. 52, # 21 p. 6926 - 6930

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Citation Number: 5

Abstract

14β-4′-Chlorocinnamoylaminodihydronormorphino... (2a), and analogues, are selective pseudoirreversible antagonists of the μ opioid receptor (MOR). The preparation of analogues with ethynic bonds, replacing the ethenic bond of 2a, is described. The new ligands, in mouse antinociceptive assays, had pseudoirreversible MOR antagonist activity, which, in the case of 8b was of longer duration than that of 2a. The related codeinone (9b) ...