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


Reference:

Nieland, N. P. R., Rennison, D., Broadbear, J. H., Purington, L., Woods, J. H., Traynor, J. R., Lewis, J. W. and Husbands, S. M., 2009. 14β-Arylpropiolylamino-17-cyclopropylmethyl-7,8-dihydronormorphinones and Related Opioids. Further Examples of Pseudoirreversible μ Opioid Receptor Antagonists. Journal of Medicinal Chemistry, 52 (21), pp. 6926-6930.

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http://dx.doi.org/10.1021/jm901074a

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Abstract

14β-4’-Chlorocinnamoylaminodihydronormorphinone (2a), and analogues, are selective pseudoirreversible antagonists of the mu 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) had only antagonist activity in vivo, in contrast to 2a’s codeinone equivalent 3a, which had potent antinociceptive activity.

Details

Item Type Articles
CreatorsNieland, N. P. R., Rennison, D., Broadbear, J. H., Purington, L., Woods, J. H., Traynor, J. R., Lewis, J. W. and Husbands, S. M.
DOI10.1021/jm901074a
Related URLs
URLURL Type
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2788771/PubMedCentral
DepartmentsFaculty of Science > Pharmacy & Pharmacology
RefereedYes
StatusPublished
ID Code25049

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