Výsledky vyhledávání - "Eckard, Weber"

Effects of the Acetylcholine Release Agent ST101 with Donepezil in Alzheimer’s Disease: A Randomized Phase 2 Study

Autor: Eckard Weber, Barbara Finn, Tilman Oltersdorf, Barbra LaPlante, Serge Gauthier, Susan Rountree

Publikováno v: Journal of Alzheimer's Disease. 48:473-481

Background and objective ST101, an acetylcholine release agent with efficacy in rodent memory and cognition models, was assessed for clinical safety and efficacy. Methods A phase 2 double blind, placebo-controlled study enrolled 210 AD patients (MMSE

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e78543a07636b815ab443f0bd3c09918
https://doi.org/10.3233/jad-150414

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Rational Design of a Combination Medication for the Treatment of Obesity

Autor: Maria Guttadauria, Eckard Weber, Kishore M. Gadde, Diane K. Smith, James W. Anderson, Michael A. Cowley, M.J. Whitehouse, Gary D. Tollefson, Alok Gupta, Ken Fujioka, Donald Schumacher, Patrick M. O'Neil, Richard L. Atkinson, Frank L. Greenway, Eduardo Dunayevich

Publikováno v: Obesity. 17:30-39

Existing obesity therapies are limited by safety concerns and modest efficacy reflecting a weight loss plateau. Here, we explore combination therapy with bupropion (BUP), a putative stimulator of melanocortin pathways, and an opioid antagonist, naltr

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::122d2c04998d0c9cc2e43abbeb098ef4
https://doi.org/10.1038/oby.2008.461

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Synthesis and SAR of novel di- and trisubstituted 1,4-dihydroquinoxaline-2,3-diones related to licostinel (Acea 1021) as NMDA/glycine site antagonists

Autor: Jon E. Hawkinson, John F. W. Keana, Stephen A. Espitia, Minhtam B. Tran, Sunil M. Kher, Sui Xiong Cai, Zhang-Lin Zhou, Richard M. Woodward, Eckard Weber, Edward R. Whittemore

Publikováno v: Bioorganic & Medicinal Chemistry. 11:1769-1780

A series of novel di- and trisubstituted 1,4-dihydroquinoxaline-2,3-diones (QXs) related to licostinel (Acea 1021) was synthesized and evaluated as antagonists for the glycine site of the N-methyl- d -asparate (NMDA) receptor. The in vitro potency of

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d4d930dcc85743e8f0c9f6ff36d050e6
https://doi.org/10.1016/s0968-0896(03)00059-2

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Design and synthesis of Rhodamine 110 derivative and Caspase-3 substrate for enzyme and cell-based fluorescent assay

Autor: John Drewe, Eckard Weber, Sui Xiong Cai, Wu Yang, John Guastella, Han-Zhong Zhang

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 11:39-42

N-Octyloxycarbonyl-R110 (1), with enhanced cell penetration and retention properties, was prepared from rhodamine 110. The tetrapeptide substrate N-Ac-DEVD-N'-octyloxycarbonyl-R110 (3) was prepared and shown to be efficiently cleaved by human recombi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1659db45e135bb896957e4ea54f40d94
https://doi.org/10.1016/s0960-894x(00)00590-4

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Structure−Activity Relationship of N-(Phenylalkyl)cinnamides as Novel NR2B Subtype-Selective NMDA Receptor Antagonists

Autor: Eckard Weber, Edward R. Whittemore, Zhang-Lin Zhou, Robert M. Schelkun, Sui Xiong Cai, John F. W. Keana, Richard M. Woodward, Amir P. Tamiz, Po-Wai Yuen

Publikováno v: Journal of Medicinal Chemistry. 42:3412-3420

A novel series of N-(phenylalkyl)cinnamides related to N-(4-phenylbutyl)-3,4-dihydroxy-beta-cyanocinnamide (6, an EGFR-K inhibitor with high antiproliferative activity) was synthesized and tested for antagonism at N-methyl-D-aspartate (NMDA) receptor

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b3e206081720dd472ea79c7e44fccaa8
https://doi.org/10.1021/jm990199u

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4-Hydroxy-1-[2-(4-hydroxyphenoxy)ethyl]-4-(4-methylbenzyl)piperidine: A Novel, Potent, and Selective NR1/2B NMDA Receptor Antagonist

Autor: Edward R. Whittemore, Minhtam Tran, David Rock, Richard M. Woodward, Zhang-Lin Zhou, Sui Xiong Cai, Christopher S. Konkoy, Stephen A. Espitia, Lawrence D. Wise, Christopher F. Bigge, John F. W. Keana, Jon E. Hawkinson, Eckard Weber, Peter A. Boxer, Linda L. Coughenour

Publikováno v: Journal of Medicinal Chemistry. 42:2993-3000

A structure-based search and screen of our compound library identified N-(2-phenoxyethyl)-4-benzylpiperidine (8) as a novel N-methyl-D-aspartate (NMDA) receptor antagonist that has high selectivity for the NR1/2B subunit combination (IC(50) = 0.63 mi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::43f0076ffe71bb601601d1cf2ac46fcd
https://doi.org/10.1021/jm990246i

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ACEA-1328, AN NMDA RECEPTOR ANTAGONIST, INCREASES THE POTENCY OF MORPHINE AND U50,488H IN THE TAIL FLICK TEST IN MICE

Autor: Kabirullah Lutfy, Peter Doan, Minh Nugyen, Eckard Weber

Publikováno v: Pharmacological Research. 38:453-460

The effect of 5-nitro-6,7-dimethyl-1,4-dihydro-2,3-quinoxalinedione (ACEA-1328), a competitive and systemically bioavailable NMDA receptor/glycine site antagonist, was examined on opioid-induced antinociception in the tail flick test. Swiss Webster m

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0212e2aec9313897954bf9feda9b2d56
https://doi.org/10.1006/phrs.1998.0396

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