Zobrazeno 1 - 10
of 18
pro vyhledávání: '"Theresa A Kuntzweiler"'
Autor:
Patrick Shum, Thomas Licher, John L. Kane, Carolin Gerbeth-Kreul, Gerhard Hessler, Antje Pommereau, Sven Ruf, Christian Engel, Linli Wei, Joerg Czech, Theresa A Kuntzweiler
Publikováno v:
SLAS Discovery. 26:783-797
Classical high-throughput screening (HTS) technologies for the analysis of ionic currents across biological membranes can be performed using fluorescence-based, radioactive, and mass spectrometry (MS)-based uptake assays. These assays provide rapid r
Autor:
Roy J. Vaz, Donglai Yang, Hong Shen, Xin Chen, Stephan Reiling, Raymond Kosley, Theresa A. Kuntzweiler, Joseph D. Batchelor, Ying Zhang, Yi Li, Vinolia Chellaraj, Larry R. McLean
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 28:3194-3196
This work describes the rational amelioration of Cytochrome P450 4/5 (CYP3A4/5) induction through the Pregnane-X Receptor (PXR) pathway in a series of compounds that modulate the metabotropic glutamate Receptor 2 (mGluR2) via an allosteric mechanism.
Autor:
Mark W. Holladay, Michael Williams, Theresa A. Kuntzweiler, Pamela S. Puttfarcken, Diana L. Donnelly-Roberts, Clark A. Briggs, Anthony W. Bannon, Peter Curzon, Stephen P. Arneric, Michael W. Decker, Arthur L. Nikkel, R. Scott Bitner
Publikováno v:
Journal of Physiology-Paris. 92:221-224
ABT-594, a nicotinic acetylcholine receptor agonist, has antinociceptive effects in rat models of acute thermal, persistent chemical, and neuropathic pain. Direct injection of ABT-594 into the nucleus raphe magnus (NRM) is antinociceptive in a therma
Publikováno v:
Drug Development Research. 44:14-20
Due to the complex mechanism of cation transport by neuronal nicotinic acetylcholine receptors (nAChR), potential ligands of these receptors must be characterized with respect to functional activity and corresponding subtype selectivity. Conventional
Autor:
Stephen P. Arneric, David E. Gunn, Diana L. Donnelly-Roberts, Hao Bai, David J. Anderson, Jeffrey E. Campbell, Yun He, Nan-Horng Lin, James P. Sullivan, Mark W. Holladay, Yihong Li, Theresa A. Kuntzweiler, Keith B. Ryther
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 8:249-254
Analogs of 3-[2-((S)-pyrrolidinyl)methoxy]pyridine (A-84543, 1) with 2-, 4-, 5-, and 6-substituents on the pyridine ring were synthesized. These analogs exhibited Ki values ranging from 0.15 to > 9,000 nM when tested in vitro for neuronal nicotinic a
Autor:
Stephen P. Arneric, Michael Williams, David J.B. Kim, David J. Anderson, Yun He, Michael W. Decker, Diana L. Donnelly-Roberts, Theresa A. Kuntzweiler, Clark A. Briggs, Mark W. Holladay, Anthony W. Bannon, James T. Wasicak, Jeffrey E. Campbell, Keith B. Ryther, Nan-Horng Lin, Marietta Piattoni-Kaplan, Michael J. Buckley
Publikováno v:
Journal of Medicinal Chemistry. 41:407-412
New members of a previously reported series of 3-pyridyl ether compounds are disclosed as novel, potent analgesic agents acting through neuronal nicotinic acetylcholine receptors. Both (R)-2-chloro-5-(2-azetidinylmethoxy)pyridine (ABT-594, 5) and its
Autor:
Stephen P. Arneric, David J. Anderson, Mark W. Holladay, Marietta Piattoni-Kaplan, Keith B. Ryther, Theresa A. Kuntzweiler, Diana L. Donnelly-Roberts, Richard L. Elliott
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 7:2703-2708
A novel series of 2-(2′-furo[3,2-b]pyridinyl) pyrrolidines has been synthesized and evaluated as novel nicotinic acetylcholine receptor ligands. Changing the pyrrolidine stereochemistry and N-substitution pattern afforded analogs with Ki values ran
Publikováno v:
FEBS Letters. 389:179-185
At two intramembrane carboxyl-containing amino acids of the sheep alpha1 isoform of Na,K-ATPase (Asp804 and Asp808), both charge-conserving (Asp to Glu) and charge-deleting (Asp to Asn, Leu and Ala) replacements were made and the altered enzymes stud
Publikováno v:
ResearcherID
Cardiac glycosides such as ouabain and digoxin specifically inhibit the Na,K-ATPase. Three new residues in the carboxyl half of the Na,K-ATPase, Phe-786, Leu-793 (PFLIF786IIANIPL793PLGT797), and Phe-863 (FTYF863VIM) have been identified as ouabain se
Autor:
Jeffrey E. Campbell, Yun He, Mark W. Holladay, Yihong Li, Nan-Horng Lin, Stephen P. Arneric, Theresa A. Kuntzweiler, David J. Anderson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 11:631-633
In an effort to probe the steric influence of C5 substitution of the pyridine ring on CNS binding affinity, analogues of 1 substituted with a bulky moiety—such as phenyl, substituted phenyl, or heteroaryl—were synthesized and tested in vitro for