Zobrazeno 1 - 10
of 29
pro vyhledávání: '"Philip A, Iredale"'
Autor:
Rebecca E. O’Connor, Steven R. Schneider, Denise Gautreau, Philip A. Carpino, Karen M. Ward, Jeffrey S. Lizano, John R. Hadcock, Philip A. Iredale, Dennis O. Scott, Robert L. Dow, Dawn Kelly-Sullivan
Publikováno v:
ACS Medicinal Chemistry Letters. 3:397-401
Antagonism of cannabinoid-1 (CB1) receptor signaling has been demonstrated to inhibit feeding behaviors in humans, but CB1-mediated central nervous system (CNS) side effects have halted the marketing and further development of the lead drugs against
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9bdcaa646cbb776cb05d86c09e6ede88
https://doi.org/10.1021/ml3000325
https://doi.org/10.1021/ml3000325
Autor:
Rama Y. Chandrasekaran, Jiri Aubrecht, Frederick R. Nelson, Linda A. Chatman, Hans Rollema, Frank M. Nedza, John M. Marcek, Philip A. Iredale, Jennifer B. Munzner, Betty Pettersen, Raggon Jeffrey W, David M. Rubitski, Julie Cianfrogna, Larry C. James, Karen W. Cook, Michael J. Banker, Diane F. Wong, Anne W. Schmidt, Michael Homiski, Howard Harry R, Daniel J. Lettiere, Butler Todd W, Scot Richard Mente, Jody Freeman, Travis T. Wager, Douglas K. Spracklin
Publikováno v:
Journal of Medicinal Chemistry. 54:7602-7620
The discovery of two histamine H3 antagonist clinical candidates is disclosed. The pathway to identification of the two clinical candidates, 6 (PF-03654746) and 7 (PF-03654764) required five hypothesis driven design cycles. The key to success in iden
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::7c253ef2a0b55c8bf1f6522eccc0c6ed
https://doi.org/10.1021/jm200939b
https://doi.org/10.1021/jm200939b
Autor:
Marlys Hammond, David A. Griffith, Philip A. Carpino, Steven R. Schneider, Robert L. Dow, Paul DaSilva-Jardine, John R. Hadcock, Philip A. Iredale, Dennis O. Scott, Ernest S. Paight
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:5351-5354
A new series of CB(1) receptor antagonists incorporating an imidazole-based isosteric replacement for the hydrazide moiety of rimonabant (SR141716) is disclosed. Members of this imidazole series possess potent/selective binding to the rCB(1) receptor
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e4fb2f93da026a0faa073ffb8e71095a
https://doi.org/10.1016/j.bmcl.2009.07.130
https://doi.org/10.1016/j.bmcl.2009.07.130
Autor:
Robert L. Dow, Paul DaSilva-Jardine, Ernest S. Paight, Philip A. Carpino, David A. Griffith, John R. Hadcock, Philip A. Iredale, Dennis O. Scott, Rebecca E. O’Connor, Chudy I. Nduaka, Shawn C Black, Steven R. Schneider
Publikováno v:
Journal of Medicinal Chemistry. 52:2652-2655
We report the design, synthesis, and structure-activity relationships of novel bicyclic lactam-based cannabinoid type 1 (CB(1)) receptor antagonists. Members of these series are potent, selective antagonists in in vitro/in vivo efficacy models of CB(
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::580a2e91a3010c35cb155a547b94543b
https://doi.org/10.1021/jm900255t
https://doi.org/10.1021/jm900255t
Autor:
Margaret S. Landis, Robert F. Day, Joseph DiBrino, David A. Griffith, Robert L. Dow, Rebecca E. O’Connor, Philip A. Carpino, Paul DaSilva-Jardine, Shawn C Black, John R. Hadcock, Philip A. Iredale, Dennis O. Scott
Publikováno v:
Journal of Medicinal Chemistry. 52:234-237
We report the structure-activity relationships, design, and synthesis of the novel cannabinoid type 1 (CB1) receptor antagonist 3a (CP-945,598). Compound 3a showed subnanomolar potency at human CB1 receptors in binding (Ki = 0.7 nM) and functional as
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4ba470e1e8e3b225cdb77ee42e6d7ec8
https://doi.org/10.1021/jm8012932
https://doi.org/10.1021/jm8012932
Autor:
Swick Andrew Gordon, Judith A. Siuciak, Janice A. Brown, Ravi B. Marala, Terrell A. Patterson, Victor Guanowsky, Phoebe Chiang, Patricia A. Seymour, Sheryl A. McCarthy, Douglas S. Chapin, Philip A. Iredale
Publikováno v:
Neuropharmacology. 52:279-290
CP-809,101 is a potent, functionally selective 5-HT(2C) agonist that displays approximately 100% efficacy in vitro. The aim of the present studies was to assess the efficacy of a selective 5-HT(2C) agonist in animal models predictive of antipsychotic
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d4e20b743108f580c2be0f583f8a35d4
https://doi.org/10.1016/j.neuropharm.2006.07.024
https://doi.org/10.1016/j.neuropharm.2006.07.024
Publikováno v:
Neuropsychopharmacology. 32:1805-1812
The observations that the cannabinoid(1)(CB(1)) receptor antagonist/inverse agonist, rimonabant, and the selective noncompetitive inhibitor of acetylcholinesterase (AChE), donepezil, improve performance in a variety of animal memory models, suggest t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b86c54df92d35016ebacbe70c5efd5f7
https://doi.org/10.1038/sj.npp.1301297
https://doi.org/10.1038/sj.npp.1301297
Autor:
Hans Rollema, Philip A. Iredale, Karen M. Ward, Anne W. Schmidt, Frank M. Nedza, Godek Dennis M, David E. Johnson, Douglas K. Spracklin
Publikováno v:
European Journal of Pharmacology. 506:209-219
Olanzapine and clozapine produce robust increases in hippocampal acetylcholine release during acetylcholinesterase inhibition, while other antipsychotics, including thioridazine, have only small effects. Since thioridazine binds with similar high aff
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::23a8ac5f76b8a6632fea17a1d3d7a907
https://doi.org/10.1016/j.ejphar.2004.11.015
https://doi.org/10.1016/j.ejphar.2004.11.015
Autor:
Eric J. Nestler, William H. Walker, Katherine L. Widnell, Philip A. Iredale, Jingshan Chen, Joel F. Habener, Ronald S. Duman
Publikováno v:
Journal of Neurochemistry. 66:1770-1773
We have recently demonstrated that mRNA expression of cyclic AMP (cAMP) response element-binding protein (CREB) is down-regulated in CATH.a cells (a neural-derived cell line) by activation of the cAMP pathway. We now demonstrate that this down-regula
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bd59dc4c7d454120b153efd93f6f2d05
https://doi.org/10.1046/j.1471-4159.1996.66041770.x
https://doi.org/10.1046/j.1471-4159.1996.66041770.x
Publikováno v:
Journal of Neurochemistry. 68:362-369
Noradrenergic neuronal networks originating in the locus coeruleus have been implicated in the stress response. In order to study this system in vitro, we have employed a locus coeruleus-like cell line, CATH.a, and have determined the effect of dexam
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d1fc4e9b3d3f0ea58e7c2f8f8143780e
https://doi.org/10.1046/j.1471-4159.1997.68010362.x
https://doi.org/10.1046/j.1471-4159.1997.68010362.x