Zobrazeno 1 - 10
of 23
pro vyhledávání: '"Marie E. Uchic"'
Autor:
Daria Darczak, Rachel Davis-Taber, Michael F. Jarvis, Victoria E. Scott, Marie E. Uchic, Xenia Beebe, Andrew O. Stewart
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:2162-2166
Potent small molecule antagonists for the PAC(1)-R have been discovered. Previously known antagonists for the PAC(1)-R were slightly truncated peptide ligands. The hydrazides reported here are the first small molecule antagonists ever reported for th
Autor:
Paul L. Richardson, Victoria E. Scott, Marie E. Uchic, Larry Solomon, Edward T. Olejniczak, Karl A. Walter, Rachel Davis-Taber, Danying Song, Chaohong Sun, Leo W. Barrett, Ana Pereda-Lopez, Philip J. Hajduk, Marc R. Lake
Publikováno v:
Proceedings of the National Academy of Sciences. 104:7875-7880
The pituitary adenylate cyclase-activating polypeptide (PACAP) receptor is a class II G protein-coupled receptor that contributes to many different cellular functions including neurotransmission, neuronal survival, and synaptic plasticity. The soluti
Autor:
Brenda Martino, Diana L. Donnelly-Roberts, Jill M. Wetter, Marie E. Uchic, Kennan C. Marsh, Ahmed A. Hakeem, Sherry Nelson, Teodozyj Kolasa, Gin C. Hsieh, Odile F. El-Kouhen, Kathleen H. Mortell, Rohde Jeffrey J, Meena V. Patel, Ruth L. Martin, Marlon D. Cowart, Peter R. Hollingsworth, Marc A. Terranova, Andrew O. Stewart, Robert B. Moreland, and Jorge D. Brioni, Mark A. Matulenko, Loan N. Miller, Gary A. Gintant, James P. Sullivan, Marian T. Namovic, John F. Darbyshire, Renjie Chang, Masaki Nakane
Publikováno v:
Journal of Medicinal Chemistry. 49:7450-7465
The goal of this study was to identify a structurally distinct D(4)-selective agonist with superior oral bioavailability to our first-generation clinical candidate 1a (ABT-724) for the potential treatment of erectile dysfunction. Arylpiperazines such
Autor:
Scott J. Baker, Loan N. Miller, Meena V. Patel, Marie E. Uchic, Kennan C. Marsh, Prisca Honore, Renjie Chang, Odile F. El Kouhen, Guo Zhu Zheng, Pramila Bhatia, Jorge D. Brioni, Robert B. Moreland, Sonya G. Lehto, Jill M. Wetter, Andrew O. Stewart, Teodozyj Kolasa
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:4936-4940
We have discovered a novel, potent, and selective triazafluorenone series of metabotropic glutamate receptor 1 (mGluR1) antagonists with efficacy in various rat pain models. Pharmacokinetic and pharmacodynamic profiles of these triazafluorenone analo
Autor:
Meena V. Patel, Marie E. Uchic, Marie P. Honore, Jerome F. Daanen, Loan N. Miller, Renjie Chang, Andrew O. Stewart, Masaki Nakane, Steven P. Latshaw, Pramila Bhatia, Sonya G. Lehto, Teodozyj Kolasa, Odile F. El Kouhen, Jorge D. Brioni, Robert B. Moreland, Guo Zhu Zheng
Publikováno v:
Journal of Medicinal Chemistry. 48:7374-7388
SAR (structure-activity relationship) studies of triazafluorenone derivatives as potent mGluR1 antagonists are described. The triazafluorenone derivatives are non-amino acid derivatives and noncompetitive mGluR1 antagonists that bind at a putative al
Autor:
Masaki Nakane, Bryan F. Cox, Robert B. Moreland, Jorge D. Brioni, Mark A. Osinski, Terese Seifert, Marie E. Uchic, Loan N. Miller, Thomas K. Shaughnessy
Publikováno v:
Pharmacology Biochemistry and Behavior. 81:211-219
Agents that activate the dopamine D2-like family of receptors elicit emesis in humans and other species with a vomiting/emetic reflex; however, the lack of dopamine receptor subtype selective agonists has hampered an understanding of which dopamine D
Autor:
Renjie Chang, Marc A. Terranova, Masaki Nakane, Andrew O. Stewart, Leimin Fan, Marian T. Namovic, Loan N. Miller, Robert B. Moreland, Teodozyi Kolasa, Diana L. Donnelly-Roberts, Bruce Surber, Marie E. Uchic, Jorge D. Brioni, Mark A. Matulenko
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:5095-5098
The first selective dopamine D4 agonist radioligand is described. The synthesis of these piperazine radioligands relied on the transformation of brominated precursors 4a and 4b with tritium gas in the presence of a sensitive cyano functional group. T
Autor:
Earl J. Gubbins, Loan N. Miller, Marc A. Terranova, Robert B. Moreland, Jeffrey N. Masters, Odile F. El-Kouhen, Diana L. Donnelly-Roberts, Marie E. Uchic, Jorge D. Brioni, Marian T. Namovic, Rosalind J. Helfrich, Renjie Chang, Masaki Nakane
Publikováno v:
Biochemical Pharmacology. 68:761-772
The goal of this study was to develop a new approach to study the pharmacology of the dopamine D 4 receptor that could be used in comparative studies with dopamine D 2 and D 3 receptors. Stable HEK-293 cell lines co-expressing recombinant human D 2L
Autor:
Renjie Chang, Marie E. Uchic, Jorge D. Brioni, Bruce W. Surber, Andrew O. Stewart, Marc A. Terranova, Robert B. Moreland, Mark A. Matulenko
Publikováno v:
European Journal of Pharmacology. 497:147-154
Tritiation of the dopamine D(4) receptor selective agonist A-369508 ([2-[4-(2-cyanophenyl)-1-piperazinyl]-N-(3-methylphenyl) acetamide) has provided a radioligand for the characterization of dopamine D(4) receptors. [(3)H] A-369508 binds with high af
Autor:
Michael F. Jarvis, Kevin J. Lynch, Connie R. Faltynek, Torben R. Neelands, Marie E Uchic, Wende Niforatos, Heath A. McDonald, Edward C. Burgard
Publikováno v:
British Journal of Pharmacology. 140:202-210
Rapid desensitization of ligand-gated ion channel receptors can alter the apparent activity of receptor modulators, as well as make detection of fast-channel activation difficult. Investigation of the antagonist pharmacology of ATP-sensitive homomeri