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)

Journal of Medicinal Chemistry

Volumn 51, Issue 19, 2008, Pages 5893-5896

  Le Bourdonnec, Bertrand ^a   Windh, Rolf T ^a   Ajello, Christopher W ^a   Leister, Lara K ^a   Gu, Minghua ^a   Chu, Guo Hua ^a   Tuthill, Paul A ^a   Barker, William M ^a   Koblish, Michael ^a   Wiant, Daniel D ^a   Graczyk, Thomas M ^a   Belanger, Serge ^a   Cassel, Joel A ^a   Feschenko, Marina S ^a   Brogdon, Bernice L ^a   Smith, Steven A ^a   Christ, David D ^a   Derelanko, Michael J ^a   Kutz, Steve ^a   Little, Patrick J ^a   DeHaven, Robert N ^a   DeHaven Hudkins, Diane L ^a   Dolle, Roland E ^a   more..

^a ADOLOR CORPORATION   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ADL 5859; BENZAMIDE DERIVATIVE; CHROMENE DERIVATIVE; DELTA OPIATE RECEPTOR AGONIST; N,N DIETHYL 4 [5 HYDROXYSPIRO(CHROMENE 2,4' PIPERIDINE) 4 YL]BENZAMIDE; PIPERIDINE DERIVATIVE; UNCLASSIFIED DRUG;

ARTICLE; DRUG ACTIVITY; DRUG INDICATION; DRUG STRUCTURE; DRUG SYNTHESIS; NONHUMAN; PAIN;

ADMINISTRATION, ORAL; ANALGESICS; ANIMALS; BENZAMIDES; BENZOPYRANS; BIOLOGICAL AVAILABILITY; DOGS; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG EVALUATION, PRECLINICAL; DRUG TOXICITY; ETHER-A-GO-GO POTASSIUM CHANNELS; HUMANS; MAXIMUM TOLERATED DOSE; MICE; MOLECULAR STRUCTURE; MOTOR ACTIVITY; PAIN; PAIN MEASUREMENT; RATS; RECEPTORS, OPIOID, DELTA; TOXICITY TESTS;

EID: 53549092761     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm8008986     Document Type: Article

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19. See Supporting Information for assay conditions.
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24. All housing conditions and experimental procedures were performed in accordance with the "Guide for the Care and Use of Laboratory Animals". Experimental procedures followed the ethical guidelines of the IASP and were approved by the Adolor Corporation Institutional Animal Care and Use Committee.
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26. Clinical studies with 20 are being conducted under open INDs, indicating FDA approval to conduct clinical studies.