Zobrazeno 1 - 10
of 37
pro vyhledávání: '"Lawrence W. Fitzgerald"'
Autor:
Joseph T. Repine, Lorraine Kathleen Fay, Favor David, Hyacinth Akunne, Kim Nicholls, Bradley Snyder, Liming Zhang, Kevin A. Serpa, Douglas S. Johnson, Lawrence W. Fitzgerald, Andrew D. White, Chung Choi, Steven Z. Whetzel
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:2621-2625
The synthesis and structure-activity relationship (SAR) of a novel series of aryl piperazine napthyridinone D(2) partial agonists is described. Our goal was to optimize the affinities for the D(2), 5-HT(2A) and 5-HT(1A) receptors, such that the D(2)/
Publikováno v:
Naunyn-Schmiedeberg's Archives of Pharmacology. 379:461-471
The type 2 serotonin (5-HT(2)) receptor subfamily is known to couple to phosphoinositide hydrolysis (PI) and the subsequent mobilization of intracellular Ca(2+), as well as the release of arachidonic acid (AA). Less is known of 5-HT(2)-mediated activ
Autor:
Gregory Gasic, Nils Brose, Lawrence W. Fitzgerald, Louis Trevisan, Eric J. Nestler, Ronald S. Duman, Stephen F. Heinemann
Publikováno v:
Journal of Neurochemistry. 62:1635-1638
We examined the effects of chronic ethanol exposure on the levels of N-methyl-D-aspartate receptor subunit 1 (NMDAR1) protein, an essential component of N-methyl-D-aspartate glutamate receptors, in rat brain. By immunoblotting procedures using a spec
Autor:
Lawrence W. Fitzgerald, Carol M. Krause, Anne P. Marshall, John P. Patterson, Deborah S. Conklin, Geeta Iyer, David P. Tran, Brian L. Largent, Paul R. Hartig, Walter A. Kostich
Publikováno v:
Journal of Neurochemistry. 72:2127-2134
Many modern models of receptor-G protein function assume that there is a direct relationship between high-affinity agonist binding and efficacy. The validity of this assumption has been recently questioned for the serotonin 5-HT2A receptor. We examin
Autor:
Mark R. Rauckhorst, Jeffrey W. Corbett, Lawrence W. Fitzgerald, Christopher S. Knauer, Fang Qian, Robert Louis Hoffman
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:6250-6256
Low nanomolar corticotropin releasing factor type-1 (CRF(1)) receptor antagonists containing unique indanylamines were identified from the heteroatom-linked pyrazine chemotype. The most potent indanylpyrazine had a K(i)=11+/-1 nM. The oxygen-linked p
Autor:
Harvey Wong, Mark D. Lindner, John F. McElroy, Robert Zaczek, Ge Zhang, Yu-Wen Li, Lawrence W. Fitzgerald, Nicholas J. Lodge, Paul J. Gilligan, Snjezana Lelas, Tanya L. Wallace
Publikováno v:
CNS Drug Reviews. 11:21-52
CRF(1) antagonists DMP696 and DMP904 were designed as drug development candidates for the treatment of anxiety and depression. Both compounds display nanomolar affinity for human CRF(1) receptors, and exhibit >1000‐fold selectivity for CRF(1) over
Autor:
Robert B McCall, Michael D. Ennis, Nabil B Ghazal, Deborah K Hyslop, Lawrence W Fitzgerald, Dac M. Dinh, Nanette F. Nichols, Michelle L Kagey, Christopher S Knauer, Robert L Hoffman, Chris L Chio, Rebecca M. Olson, Christopher L. Haber, Kjell A. Svensson, Jeffery E Campbell
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:2369-2372
The design and synthesis of the novel 2,3,4,5-tetrahydro-1H-[1,4]diazepino[1,7-a]indole 5 is described. This azepinoindole has excellent affinity for 5-HT(2C) (K(i) 4.8 nM) and modest selectivity over 5-HT(2A) ( approximately 4-fold). Several N- and
Autor:
Argyrios G, Arvanitis, Joseph T, Rescinito, Charles R, Arnold, Richard G, Wilde, Gary A, Cain, Jung Hui, Sun, Jia-Sheng, Yan, Christopher A, Teleha, Lawrence W, Fitzgerald, John, McElroy, Robert, Zaczek, Paul R, Hartig, Scott, Grossman, Stephen P, Arneric, Paul J, Gilligan, Richard E, Olson, David W, Robertson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:125-128
A series of high affinity CRF receptor ligands with an imidazo[4,5-b]pyridine core is described. Individual analogues were synthesized and tested in a rat CRF receptor binding assay. The best compounds were further tested in the dog N-in-1 pharmacoki
Autor:
Edward Guilmette, Mathew T. Pletcher, Thomas A. Lanz, Diane Stephenson, Lawrence W Fitzgerald, James E Fischer, Mark Gosink
Publikováno v:
Molecular Autism
Background Austism spectrum disorder (ASD) is a heterogeneous behavioral disorder or condition characterized by severe impairment of social engagement and the presence of repetitive activities. The molecular etiology of ASD is still largely unknown d
Publikováno v:
Bioorganic & Medicinal Chemistry. 7:2321-2328
Structure–activity studies around the 4-position of 2-anilinopyrimidine corticotropin releasing factor (CRF) antagonists suggest that there is a large lipophilic cavity in the rat CRF receptor, which can accommodate a wide variety of substituents a