Zobrazeno 1 - 10
of 38
pro vyhledávání: '"Patrick J. Little"'
Publikováno v:
Geomorphology. 202:86-100
The highly diverse shifting-mosaic of forest patches of an alluvial forest within the Carmanah River valley on the west coast of Vancouver Island, British Columbia was studied to examine the hydrogeomorphic disturbance regime that structures it. We u
Autor:
Patrick J. Little, Rolf T. Windh, Chihiro Nozaki, Bertrand Le Bourdonnec, Claire Gaveriaux-Ruff, David Reiss, Brigitte L. Kieffer, Roland E. Dolle
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 342:799-807
N,N-diethyl-4-(5-hydroxyspiro[chromene-2,4′-piperidine]-4-yl) benzamide (ADL5859) and N,N-diethyl-3-hydroxy-4-(spiro[chromene-2,4′-piperidine]-4-yl)benzamide (ADL5747) are novel δ-opioid agonists that show good oral bioavailability and analgesic
Autor:
Jonathan M. Brotchie, Patrick J. Little, Bertrand Le Bourdonnec, Tom H. Johnston, Roland E. Dolle, Susan H. Fox, Robert N. DeHaven, Diane L. DeHaven-Hudkins, James B. Koprich, Allan J. Goodman
Publikováno v:
Movement Disorders. 26:1225-1233
In Parkinson's disease (PD), dyskinesia develops following long-term treatment with 3,4-dihydroxyphenylalanine (L-dopa). Given the prominent role of the opioid system in basal ganglia function, nonselective opioid receptor antagonists have been teste
Autor:
Patrick J. Little, Joel A. Cassel, Allan J. Goodman, Lara K. Leister, Ian Sellitto, Markku A. Savolainen, Christopher J. LaBuda, Robert N. DeHaven, Karin Worm, Steven A. Smith, Christopher W. Ajello, Bertrand Le Bourdonnec, Roland E. Dolle, Christopher T. Saeui, Michael Koblish, Bernice L. Brogdon, Guo-Hua Chu
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:387-391
A lead optimization campaign in our previously reported sulfamoyl benzamide class of CB2 agonists was conducted to improve the in vitro metabolic stability profile in this series while retaining high potency and selectivity for the CB2 receptor. From
Autor:
Bertrand Le Bourdonnec, Patrick J. Little, Christopher W. Ajello, Bernice L. Brogdon, Markku A. Savolainen, Steven A. Smith, Michael Koblish, Allan J. Goodman, Christopher J. LaBuda, Robert N. DeHaven, Heather O’Hare, Roland E. Dolle, Joel A. Cassel, Karin Worm, Gabriel J. Stabley
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:309-313
Previous research within our laboratories identified sulfamoyl benzamides as novel cannabinoid receptor ligands. Optimization of the amide linkage led to the reverse amide 40. The compound exhibited robust antiallodynic activity in a rodent pain mode
Autor:
Guo-Hua Chu, William M. Barker, Rolf T. Windh, Patrick J. Little, Michael J. Derelanko, Bertrand Le Bourdonnec, Michael Koblish, Diane L. DeHaven-Hudkins, Minghua Gu, Thomas M. Graczyk, Daniel D. Wiant, Lara K. Leister, Bernice L. Brogdon, Robert N. DeHaven, Christopher W. Ajello, Steven A. Smith, Serge Belanger, David D. Christ, Paul A. Tuthill, Steve Kutz, Joel A. Cassel, Marina S. Feschenko, Roland E. Dolle
Publikováno v:
Journal of Medicinal Chemistry. 51:5893-5896
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 iden
Autor:
Roland E. Dolle, Diane L. DeHaven-Hudkins, Daniel D. Wiant, Joel A. Cassel, William M. Barker, Patrick J. Little, Bertrand Le Bourdonnec, Robert N. DeHaven, Serge Belanger, Nathalie Conway-James, Timothy J. O’Neill
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:2006-2012
A series of N-substituted trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidines, mu opioid receptor antagonists, analogs of alvimopan, were prepared using solid phase methodology. This study led to the identification of a highly selective mu opioid recep
Publikováno v:
Pharmacology & Therapeutics. 117:162-187
The localization of opioid receptors and their endogenous peptide ligands within the gastrointestinal (GI) tract and their role in the coordination of propulsion and secretion underscores the importance of opioid receptors in the maintenance of GI ho
Autor:
Michael Koblish, Minghua Gu, Thomas M. Graczyk, Patrick J. Little, Nathalie Conway-James, Robert N. DeHaven, Serge Belanger, Diane L. DeHaven-Hudkins, Guo-Hua Chu, Joel A. Cassel, Roland E. Dolle
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:1951-1955
A novel series of malonamide derivatives was synthesized. These amides were shown to be potent and selective kappa opioid receptor agonists.
Autor:
Erin Gauntner, Alan L. Maycock, Virendra Kumar, Patrick J. Little, Michael Koblish, Erik Mansson, Diane L. DeHaven-Hudkins, Susan L. Gottshall, Robert N. DeHaven, Joel A. Cassel, Susan L. Greiner, Jeffrey D. Daubert, Deqi Guo
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:1091-1095
A series of 3-substituted analogs (3) of the parent kappa agonist, 1, were prepared to limit access to the central nervous system. With the exception of compound 3j, all other compounds bound to the human kappa opioid receptor with high affinity (K(i