Výsledky vyhledávání - "David W. Schulz"

3,5-Bicyclic aryl piperidines: A novel class of α4β2 neuronal nicotinic receptor partial agonists for smoking cessation

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

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::04dfd8d682666f8daba933d872fb0b4a
https://doi.org/10.1016/j.bmcl.2005.08.035

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Varenicline: An α4β2 Nicotinic Receptor Partial Agonist for Smoking Cessation

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

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::44d09a810f898eefeb7fda3442e4b30f
https://doi.org/10.1021/jm050069n

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Amygdaloid D1 receptors are not linked to stimulation of adenylate cyclase

Autor: David W. Schulz, Sarah K. Leonard, Carl M. Anderson, Richard B. Mailman, Clinton D. Kilts, Jean E. Lachowicz

Publikováno v: Synapse. 50:320-333

In contrast to the classic signal transduction of D1 dopamine receptors in striatum or molecular expression systems, it has been reported that D1 receptor agonists do not stimulate adenylate cyclase in homogenates of microdissected nuclei of the amyg

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3be3a24b3af8d2e06da4b0d61edf9fe9
https://doi.org/10.1002/syn.10272

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CP-154,526: a potent and selective nonpeptide antagonist of corticotropin releasing factor receptors

Autor: J P Braselton, Michael L. Corman, Judith L. Collins, A W Schmidt, J Heym, Patricia A. Seymour, David W. Schulz, F. D. Tingley, A. Dunaiskis, S Faraci, E N Winston, Robert S. Mansbach, T Seeger, Yuhpyng L. Chen, J Sprouse

Publikováno v: Proceedings of the National Academy of Sciences. 93:10477-10482

Here we describe the properties of CP-154,526, a potent and selective nonpeptide antagonist of corticotropin (ACTH) releasing factor (CRF) receptors. CP-154,526 binds with high affinity to CRF receptors (Ki < 10 nM) and blocks CRF-stimulated adenylat

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::42a0f15e8489903459ee8036cf4d276e
https://doi.org/10.1073/pnas.93.19.10477

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5-cyano-1-[3-(N-methylpyrrolidin-2R-ylmethyl)indol-5-yl] benzimidazole (CP-161,242): A potent, centrally active 5-HT1D receptor agonist and benzodiazepine partial agonist

Autor: Patricia A. Seymour, Desai Kishor A, B. Kenneth Koe, David H. Blank, Carol B. Fox, Macor John E, Anne W. Schmidt, David W. Schulz, Ronald J. Post, Lorraine A. Lebel

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 5:2391-2396

The discovery of CP-161,242 (5-cyano-1-[3-(N-methylpyrrolidin-2R-ylmethyl)indol-5-yl]benzimidazole), a potent, selective, orally active central serotonin (5-HT1D) agonist [IC50 (binding) = 1.3 nM, EC50 (inhibition of adenylate cyclase) = 42 pM] and b

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::babecb78f7d9c13cd636bdf0f868a836
https://doi.org/10.1016/0960-894x(95)00417-r

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2-aryloxy-4-alkylaminopyridines: discovery of novel corticotropin-releasing factor 1 antagonists

Autor: R. Scott Obach, Jody Freeman, F. David Tingley, Jeffrey Sprouse, Randall James Gallaschun, Michael L. Corman, John Braselton, James Forman, Anne W. Schmidt, Yuhpyng L. Chen, David W. Schulz, Elizabeth Winston, Robert S. Mansbach

Publikováno v: Journal of medicinal chemistry. 51(5)

An orally active clinical candidate of corticotropin-releasing factor 1 (CRF 1) antagonist 1 showed a significant positive food effect in dog and human after oral administration. Efforts to address the food effect issue led us to explore and discover

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d43541a27d2be09604cdd78b696d785a
https://pubmed.ncbi.nlm.nih.gov/18288792

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Synthesis and SAR of 2-aryloxy-4-alkoxy-pyridines as potent orally active corticotropin-releasing factor 1 receptor antagonists

Autor: Seeger Thomas Francis, Jeff S. Sprouse, Randall James Gallaschun, Elizabeth Winston, John Braselton, James Forman, Anne W. Schmidt, Yuhpyng L. Chen, David W. Schulz, F. David Tingley, Robert S. Mansbach

Publikováno v: Journal of medicinal chemistry. 51(5)

A series of 2-aryloxy-4-alkoxy-pyridines ( 1) was identified as novel, selective, and orally active antagonists of the corticotropin-releasing factor 1 (CRF 1) receptor. Among these, compound 2 (CP-316311) is a potent and selective CRF 1 receptor ant

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f4d860eb3157ed31669bd01e544ce501
https://pubmed.ncbi.nlm.nih.gov/18260619

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