Zobrazeno 1 - 10
of 21
pro vyhledávání: '"Thomas Allen Chappie"'
Publikováno v:
Frontiers in Neuroscience, Vol 14 (2021)
Frontiers in Neuroscience
Frontiers in Neuroscience
PDE10A, a phosphodiesterase that inactivates both cAMP and cGMP, is a unique signaling molecule in being highly and nearly exclusively expressed in striatal medium spiny neurons. These neurons dynamically integrate cortical information with dopamine-
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::090ae25e5aea52e5090d314374453bbf
https://doi.org/10.3389/fnins.2020.600178
https://doi.org/10.3389/fnins.2020.600178
Autor:
Nandini Chaturbhai Patel, Richard V. Coelho, Christopher John Helal, Chewah Lee, Anabella Villalobos, Shawn D. Doran, Joseph Michael Young, Robert J. Mather, Simone Sciabola, Erik Alphie Lachapelle, John T. Lazzaro, Thomas Allen Chappie, Patrick Robert Verhoest, Zoë A. Hughes, Marc B. Skaddan, Elizabeth Mary Beck, John M. Humphrey, Kyle Kuszpit, Laigao Chen, Lei Zhang, Kenneth R. Zasadny, Kuo-Hsien Fan
Publikováno v:
Journal of Medicinal Chemistry. 60:8538-8551
As part of our effort in identifying phosphodiesterase (PDE) 4B-preferring inhibitors for the treatment of central nervous system (CNS) disorders, we sought to identify a positron emission tomography (PET) ligand to enable target occupancy measuremen
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e7f5ba940556ef8664e507811b6fb86d
https://doi.org/10.1021/acs.jmedchem.7b01050
https://doi.org/10.1021/acs.jmedchem.7b01050
Autor:
Kimberly F. Fennell, Zhijun Kang, Hirokazu Ueno, William E. Hoffman, Mihály Hajós, Thomas Allen Chappie, Mary Piotrowski, Noha Maklad, Jayvardhan Pandit, John M. Humphrey, Anne W. Schmidt, Edward X. Yang, Patrick Robert Verhoest, Bethany L. Kormos, Jiemin Lu, Eric P. Arnold, Cheng Chang, Christopher J. Schmidt, Robin J. Kleiman, Rebecca E. O’Connor, John F. Harms, Scot Richard Mente, Christopher John Helal, Tracey Boyden, Chewah Lee, Laura McDowell, Michael D. Forman
Publikováno v:
Journal of Medicinal Chemistry. 60:5673-5698
Phosphodiesterase 2A (PDE2A) inhibitors have been reported to demonstrate in vivo activity in preclinical models of cognition. To more fully explore the biology of PDE2A inhibition, we sought to identify potent PDE2A inhibitors with improved brain pe
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d146c156bc1785305e9a93e6cd8b6147
https://doi.org/10.1021/acs.jmedchem.7b00397
https://doi.org/10.1021/acs.jmedchem.7b00397
Autor:
Mark J. Majchrzak, Aarti Sawant-Basak, Christopher J. Schmidt, Nawshaba Nawreen, Thomas Allen Chappie, Rebecca E. O’Connor, Michelle Vanase-Frawley, Keith Dlugolenski, David Horton, David P. Nguyen, Bethany L. Kormos, Ramalakshmi Yegna Chandrasekaran, Travis T. Wager, Nancy C. Stratman, Elizabeth R. Dunn-Sims, Brian Samas, Andy N. Mead, Cathleen Hsu
Publikováno v:
ACS Chemical Neuroscience. 8:165-177
Dopamine receptor antagonism is a compelling molecular target for the treatment of a range of psychiatric disorders, including substance use disorders. From our corporate compound file, we identified a structurally unique D3 receptor (D3R) antagonist
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::233def4cf409b94edafff8b7059d5f86
https://doi.org/10.1021/acschemneuro.6b00297
https://doi.org/10.1021/acschemneuro.6b00297
Autor:
Eddie Yang, Jennifer L. Liras, Christine C. Orozco, Christopher W. am Ende, Matthew A. Movsesian, Jayvardhan Pandit, John M. Humphrey, Stephen Jenkinson, Frank S. Menniti, Thomas Allen Chappie, Spiros Liras, Stacey L. Becker, Felix Vajdos, Fabrice Vandeput
Publikováno v:
Journal of medicinal chemistry. 61(10)
We disclose the discovery and X-ray cocrystal data of potent, selective quinazoline inhibitors of PDE1. Inhibitor (S)-3 readily attains free plasma concentrations above PDE1 IC50 values and has restricted brain access. The racemic compound 3 inhibits
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::aad70863e6c50adf198b09386b95c77c
https://pubmed.ncbi.nlm.nih.gov/29718668
https://pubmed.ncbi.nlm.nih.gov/29718668
Autor:
Mihály Hajós, William E. Hoffman, John F. Harms, Mary Piotrowski, Christopher J. Schmidt, Eric P. Arnold, Robin J. Kleiman, Edward X. Yang, Adam Ogden, Patricia A. Seymour, Jiemin Lu, Ethan Lawrence Fisher, Nichole Vansell, Patrick Robert Verhoest, Jayvardhan Pandit, Zhijun Kang, Hirokazu Ueno, John M. Humphrey, Bethany L. Kormos, Dina McGinnis, Thomas Allen Chappie, Noha Maklad, Laura McDowell, Cheng Chang, Rebecca E. O’Connor, Chewah Lee, Tracey Boyden, Christopher J. O’Donnell, Christopher John Helal
Publikováno v:
Journal of medicinal chemistry. 61(3)
Computational modeling was used to direct the synthesis of analogs of previously reported phosphodiesterase 2A (PDE2A) inhibitor 1 with an imidazotriazine core to yield compounds of significantly enhanced potency. The analog PF-05180999 (30) was subs
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::408cc7b21c310fe120ce681146fe8fb5
https://pubmed.ncbi.nlm.nih.gov/29293004
https://pubmed.ncbi.nlm.nih.gov/29293004
Autor:
Christopher J. Schmidt, Thomas Allen Chappie, Douglas S. Johnson, Nicholas J. Brandon, Kieran F. Geoghegan, Patrick Robert Verhoest, Laura A. McAllister, Vinod D. Parikh, Jan-Philip Schülke
Publikováno v:
ACS Chemical Biology. 9:2823-2832
Phosphodiesterases (PDEs) regulate the levels of the second messengers cAMP and cGMP and are important drug targets. PDE10A is highly enriched in medium spiny neurons of the striatum and is an attractive drug target for the treatment of basal ganglia
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0085568a27c9391d146d6701a582553d
https://doi.org/10.1021/cb500671j
https://doi.org/10.1021/cb500671j
Publikováno v:
Phosphodiesterases and Their Inhibitors
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::1289e8b6d28c974e5b1c7d3d4fda95ad
https://doi.org/10.1002/9783527682348.ch05
https://doi.org/10.1002/9783527682348.ch05
Publikováno v:
Phosphodiesterases and Their Inhibitors
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::25ae2d55b3c75cf7b959080d95b8d303
https://doi.org/10.1002/9783527682348.ch04
https://doi.org/10.1002/9783527682348.ch04
Publikováno v:
Journal of Medicinal Chemistry. 55:7299-7331
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::69fc24768747f907122419d0980acf70
https://doi.org/10.1021/jm3004976
https://doi.org/10.1021/jm3004976