Potent, orally bioavailable delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-4-(5-hydroxyspiro[chromene-2,4'-piperidine]-4-yl)benzamide (ADL5859).

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.
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
Journal	Journal of medicinal chemistry (J Med Chem) Vol. 51 Issue 19 Pg. 5893-6 (Oct 09 2008) ISSN: 1520-4804 [Electronic] United States
PMID	18788723 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References	Analgesics Benzamides Benzopyrans Ether-A-Go-Go Potassium Channels N,N-diethyl-4-(5-hydroxyspiro(chromene-2,4'-piperidine)-4-yl)benzamide Receptors, Opioid, delta
Topics	Administration, Oral Analgesics (administration & dosage, chemical synthesis, chemistry) Animals Benzamides (administration & dosage, chemical synthesis, chemistry) Benzopyrans (administration & dosage, chemical synthesis, chemistry) Biological Availability Dogs Dose-Response Relationship, Drug Drug Evaluation, Preclinical Drug-Related Side Effects and Adverse Reactions Ether-A-Go-Go Potassium Channels (drug effects) Humans Maximum Tolerated Dose Mice Molecular Structure Motor Activity (drug effects) Pain (drug therapy) Pain Measurement (drug effects) Rats Receptors, Opioid, delta (agonists) Toxicity Tests

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