Spirocyclic delta opioid receptor agonists for the treatment of pain: discovery of N, N-diethyl-3-hydroxy-4-(spiro [chromene-2, 4′-piperidine]-4-yl) benzamide ( …

B Le Bourdonnec, RT Windh, LK Leister…

文献索引：Bourdonnec, Bertrand Le; Windh, Rolf T.; Leister, Lara K.; Zhou, Q. Jean; Ajello, Christopher W.; Gu, Minghua; Chu, Guo-Hua; Tuthill, Paul A.; Barker, William M.; Koblish, Michael; Wiant, Daniel D.; Graczyk, Thomas M.; Belanger, Serge; Cassel, Joel A.; Feschenko, Marina S.; Brogdon, Bernice L.; Smith, Steven A.; Derelanko, Michael J.; Kutz, Steve; Little, Patrick J.; Dehaven, Robert N.; DeHaven-Hudkins, Diane L.; Dolle, Roland E. Journal of Medicinal Chemistry, 2009 , vol. 52, # 18 p. 5685 - 5702

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被引用次数: 46

摘要

Selective, nonpeptidic δ opioid receptor agonists have been the subject of great interest as potential novel analgesic agents. The discoveries of BW373U86 (1) and SNC80 (2) contributed to the rapid expansion of research in this field. However, poor drug-like properties and low therapeutic indices have prevented clinical evaluation of these agents. Doses of 1 and 2 similar to those required for analgesic activity produce convulsions in ...