Zobrazeno 1 - 10
of 64
pro vyhledávání: '"Roy D. Schwarz"'
Autor:
Jurgen Wess, Celine Valant, Andrew B. Tobin, David Thal, Roy D. Schwarz, Neil M. Nathanson, Ernst Mutschler, Fred Mitchelson, Chris Langmead, Günter Lambrecht, Heinz J. Kilbinger, Rudolf Hammer, Christian C. Felder, Frederick Ehlert, Richard M. Eglen, Arthur Christopoulos, R.A. John Challiss, Noel J. Buckley, David A. Brown, Sophie Bradley, Nigel J. M. Birdsall
Publikováno v:
IUPHAR/BPS Guide to Pharmacology CITE. 2023
Muscarinic acetylcholine receptors (mAChRs) (nomenclature as agreed by the NC-IUPHAR Subcommittee on Muscarinic Acetylcholine Receptors [53]) are activated by the endogenous agonist acetylcholine. All five (M1-M5) mAChRs are ubiquitously expressed in
Autor:
Neil M. Nathanson, Jürgen Wess, Rudolf Hammer, R. A. John Challiss, Richard M. Eglen, Fred Mitchelson, David Brown, Sophie J. Bradley, Celine Valant, Heinz Kilbinger, Chris Langmead, Frederick J. Ehlert, Andrew B. Tobin, Noel J. Buckley, Ernst Mutschler, Günter Lambrecht, Arthur Christopoulos, David M. Thal, Roy D. Schwarz, Nigel J. M. Birdsall, Christian C. Felder
Publikováno v:
IUPHAR/BPS Guide to Pharmacology CITE. 2021
Muscarinic acetylcholine receptors (mAChRs) (nomenclature as agreed by the NC-IUPHAR Subcommittee on Muscarinic Acetylcholine Receptors [50]) are activated by the endogenous agonist acetylcholine. All five (M1-M5) mAChRs are ubiquitously expressed in
Autor:
Frederick J. Ehlert, Nigel J. M. Birdsall, Ernst Mutschler, Heinz Kilbinger, Günter Lambrecht, Neil M. Nathanson, Roy D. Schwarz, Sophie J. Bradley, Richard M. Eglen, Christian C. Felder, David M. Thal, R. A. John Challiss, Rudolf Hammer, Andrew B. Tobin, Jürgen Wess, Arthur Christopoulos, Celine Valant, Noel J. Buckley, Fred Mitchelson, David Brown, Chris Langmead
Publikováno v:
IUPHAR/BPS Guide to Pharmacology CITE. 2021
Muscarinic acetylcholine receptors (mAChRs) (nomenclature as agreed by the NC-IUPHAR Subcommittee on Muscarinic Acetylcholine Receptors [50]) are activated by the endogenous agonist acetylcholine. All five (M1-M5) mAChRs are ubiquitously expressed in
Autor:
Celine Valant, Fred Mitchelson, Noel J. Buckley, David Brown, Neil M. Nathanson, Roy D. Schwarz, Nigel J. M. Birdsall, Christian C. Felder, Rudolf Hammer, Chris Langmead, Arthur Christopoulos, Günter Lambrecht, Frederick J. Ehlert, Richard M. Eglen, Jürgen Wess, Sophie J. Bradley, Ernst Mutschler, Heinz Kilbinger, Andrew B. Tobin, R. A. John Challiss
Publikováno v:
IUPHAR/BPS Guide to Pharmacology CITE. 2019
Muscarinic acetylcholine receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on Muscarinic Acetylcholine Receptors [45]) are GPCRs of the Class A, rhodopsin-like family where the endogenous agonist is acetylcholine. In addition to the age
Autor:
Jack J. Kinsora, Jared B.J. Milbank, Rachel M. Brooker, Christopher S. Knauer, Kenneth S. Kilgore, Cleo J. C. Connolly, John A. Wendt, Corinne E. Augelli-Szafran, Koji Yamagata, Susan E. Bove, Mickelson John, Paul Galatsis, Roy D. Schwarz
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:6525-6528
We describe three novel regioisomeric series of aryl naphthyridine analogs, which are potent antagonists of the Class III GPCR mGlu5 receptor. The synthesis and in vitro and in vivo pharmacological activities of these analogs are discussed.
Autor:
Koji Yamagata, Jack J. Kinsora, Paul Galatsis, Kristin Knapp Lin, Abdul E. Mutlib, Zhuang Nian, John A. Wendt, Corinne E. Augelli-Szafran, Christopher S. Knauer, Susan M. Lotarski, Korana Stakich, Wing Lam, Jared B.J. Milbank, Kristen K. Gillespie, John W. Thomas, Jennifer K. Hoffman, Mickelson John, Annette T. Sakkab-Tan, Roy D. Schwarz
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:4415-4418
Rational replacement of the alkyne linker of mGluR5 antagonist MPEP gave 7-arylquinolines. SAR optimization gave an orally active compound with high affinity for the MPEP binding site.
Autor:
T. A. Pugsley, Hussein Hallak, Thomas M. Böhme, Kevin A. Serpa, Corinne E. Augelli-Szafran, Roy D. Schwarz
Publikováno v:
Journal of Medicinal Chemistry. 45:3094-3102
Previously, we reported on PD 102807 (41) as being the most selective synthetic M(4) muscarinic antagonist identified to date. Synthesized analogues of 41 showed no improvement in affinity and selectivity at that time. However, several newly synthesi
Publikováno v:
Trends in Pharmacological Sciences. 22:215-219
The Ninth International Symposium on Subtypes of Muscarinic Receptors 1 1The proceedings of the meeting will be published: Birdsall, N.J.M. et al. Life Sciences (Vol. 68). was held on 31 October – 4 November 2000 in Houston, Texas, USA.
Autor:
D.W. Moreland, Juan C. Jaen, Penvose-Yi, Roy D. Schwarz, C.E. Augelli-Szafran, C. J. Blankley, Anthony Jerome Thomas, C.B. Nelson
Publikováno v:
Journal of Medicinal Chemistry. 42:356-363
A series of esters of 1,4-disubstituted tetrahydropyridine carboxylic acids (I) has been synthesized and characterized as potential m1 selective muscarinic receptor antagonists. The affinity of these compounds for the five human muscarinic receptor s
Publikováno v:
Drug Development Research. 40:133-143
Clinical trials in Alzheimer's disease (AD) with first generation muscarinic agonists (e.g., arecoline, oxotremorine, pilocarpine) produced inconsistent results due to poor pharmacokinetic properties and a lack of separation between central and perip