Zobrazeno 1 - 10
of 26
pro vyhledávání: '"Steven B Sands"'
Autor:
Ann J. Barbier, Steven B Sands, Lilian Y Li, Anthony Ndifor, Chandra R. Shah, Kirsten L. Morton, Michael A. Letavic, Timothy W. Lovenberg, Anne Bonneville, Heather McAllister, Neelakandha S. Mani, Ian Fraser, Kiev S. Ly, Richard Apodaca, Nicholas I. Carruthers, Manoj Bajpai, Swanson Devin M, Michelle Kramer, Christine Dugovic, Sandra S Snook, Chennagiri R. Pandit, Jonathan Shelton, Wei Xiao, Leah Aluisio, Pascal Bonaventure, Brian Lord, S Diane Nepomuceno
Publikováno v:
ACS Medicinal Chemistry Letters. 6:450-454
The preclinical characterization of novel phenyl(piperazin-1-yl)methanones that are histamine H3 receptor antagonists is described. The compounds described are high affinity histamine H3 antagonists. Optimization of the physical properties of these h
Autor:
Amy B. Jakowski, F. David Tingley, Amy C. Shen, Michael R. Elwell, Steven B. Sands, Jenny Hon Cai, Martin Finkelstein, Dominique Brees
Publikováno v:
Toxicologic Pathology. 36:568-575
In a two-year carcinogenicity study with administration of high doses of the partial nicotinic agonist varenicline (recently approved for smoking cessation), mediastinal hibernomas occurred in three male rats. To investigate potential mechanisms for
Autor:
Arneric Sp, Karen K. Cook, Thomas J. Raub, Bruce N. Rogers, Mark L. Wolfe, Eric Jon Jacobsen, Vincent E. Groppi, Carey G, Brian A. Staton, Daniel P. Walker, Raymond S. Hurst, Luz A. Cortes-Burgos, Rodney R. Walters, Donn G. Wishka, Theron M. Wall, Jia S, Hanchar Aj, Karen M. Yates, Steven B. Sands, Bruce A. Thornburgh, Gold Lh, Soglia, Jason K. Myers, Franklin S, Steven Charles Reitz, Sabrina X. Zhao, Amit S. Kalgutkar, Nicole R. Higdon, Olson Kl, Erik H. F. Wong, Mihály Hajós, William E. Hoffmann
Publikováno v:
Journal of Medicinal Chemistry. 49:4425-4436
N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide (14, PHA-543,613), a novel agonist of the alpha7 neuronal nicotinic acetylcholine receptor (alpha7 nAChR), has been identified as a potential treatment of cognitive deficits in sch
Autor:
Thomas I. Davis, Carol B. Fox, Michael C. Wirtz, Michael G. Vetelino, F. David Tingley, Krista E. Bianco, Robert S. Mansbach, David W. Schulz, Jotham Wadsworth Coe, Crystal G. Bashore, Hans Rollema, Eric P. Arnold, Paige Roanne Palmer Brooks, Steven B. Sands, Brian T. O’Neill, Lorraine A. Lebel
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:4889-4897
3,5-Bicyclic aryl piperidines are a new class of high-affinity alpha4beta2 nicotinic receptor agents. We have sought nicotinic receptor partial agonists of the alpha4beta2 nicotinic acetylcholine receptor for smoking cessation, and a number of compou
Autor:
Yi Lu, Jotham Wadsworth Coe, Thomas I. Davis, David W. Schulz, Lorraine A. Lebel, Robert S. Mansbach, Paige Roanne Palmer Brooks, Michael C. Wirtz, Alka Shrikhande, Michael G. Vetelino, Leslie K. Chambers, Eric P. Arnold, Eric Schaeffer, Brian T. O’Neill, Steven B. Sands, and F. David Tingley, James Heym, Carol B. Fox, Huang Jianhua, Charles C. Rovetti, Hans Rollema
Publikováno v:
Modern Drug Synthesis
Herein we describe a novel series of compounds from which varenicline (1, 6,7,8,9-tetrahydro-6,10-methano-6H-pyrazino[2,3-h][3]benzazepine) has been identified for smoking cessation. Neuronal nicotinic acetylcholine receptors (nAChRs) mediate the dep
Autor:
Steven B. Sands
Publikováno v:
Science. 275:1401-1404
Autor:
Alka Shrikhande, Eric P. Arnold, Lorraine A. Lebel, Langu Peng, Frank M. Nedza, Brian T. O’Neill, Douglas K. Spracklin, Robert J. Mather, Steven B. Sands, Christopher J. O’Donnell
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(16)
The synthesis and SAR studies about the bicyclic amine, carbamate linker and aromatic ring of a 1,4-diazabicyclo[3.2.2]nonane phenyl carbamate series of alpha7 nAChR agonists is described. The development of the medicinal chemistry strategy and SAR w
Autor:
Michael E. Barish, Steven B. Sands
Publikováno v:
Brain Research. 560:38-42
The conductance properties of neuronal nicotinic acetylcholine receptors (neuronal nAChR channels) in PC12 cells were studied using single channel and whole cell gigaohm seal voltage clamp techniques. Acetylcholine receptor agonists were applied usin
Autor:
Steven B. Sands, Leslie K. Chambers, Eric Schaeffer, Raymond S. Hurst, Robert S. Mansbach, J. Glowa, Hans Rollema, F. D. Tingley, Charles C. Rovetti, Yi Lu, David W. Schulz, Robert J. Mather, Jotham Wadsworth Coe, Lorraine A. Lebel, Kathryn E. Williams
Publikováno v:
Neuropharmacology. 52(3)
The preclinical pharmacology of the alpha4beta2 nicotinic acetylcholine receptor (nAChR) partial agonist varenicline, a novel smoking cessation agent is described. Varenicline binds with subnanomolar affinity only to alpha4beta2 nAChRs and in vitro f
Autor:
Michael C. Wirtz, Eric P. Arnold, Paige Roanne Palmer Brooks, Michael G. Vetelino, Lorraine A. Lebel, Carol B. Fox, David W. Schulz, Brian T. O’Neill, Crystal G. Bashore, Jotham Wadsworth Coe, Thomas I. Davis, Hans Rollema, Steven B. Sands, F. David Tingley
Publikováno v:
Bioorganicmedicinal chemistry letters. 15(12)
The preparation and biological activity of analogs of (-)-cytisine, an alpha4beta2 nicotinic receptor partial agonist, are discussed. All-carbon-containing phenyl ring replacements of the pyridone ring system, generated via Heck cyclization protocols