Potent, Orally Bioavailable Delta Opioid Receptor Agonists for the Treatment of Pain: Discovery ofN,N-Diethyl-4-(5-hydroxyspiro[chromene-2,4′-piperidine]-4-yl)benzamide (ADL5859)
Year: 2008
Type: article
Abstract: Selective delta opioid receptor agonists are promising potential therapeutic agents for the treatment of various types of pain conditions. A spirocyclic derivative was identified as a promising hit through screening. Subsequent lead optimization identified compound 20 (ADL5859) as a potent, selective, and orally bioavailable delta agonist. Compound 20 was selected as a clinical candidate for the treatment of pain.
Source: Journal of Medicinal Chemistry
DOI: 10.1021/jm8008986
Authors: Bertrand Le Bourdonnec, Rolf T. Windh, Christopher W. Ajello, Lara K. Leister, Minghua Gu, Guo-Hua Chu, Paul A. Tuthill, William M. Barker, Michael Koblish, Daniel D. Wiant, Thomas M. Graczyk, Serge Belanger, Joel A. Cassel, Marina S. Feschenko, Bernice L. Brogdon, Steven A. Smith, David D. Christ, Michael J. Derelanko, Steve Kutz, Patrick J. Little, Robert N. DeHaven, Diane L. DeHaven-Hudkins, Roland E. Dolle
Language: English
Subfield: Cellular and Molecular Neuroscience
Field: Neuroscience
Domain: Life Sciences
Open Access status: green
OpenAlex ID: W2005492665