Zobrazeno 1 - 10 of 63 pro vyhledávání: '"David J Behm"'
1
Akademický článek
Effects of urotensin II receptor antagonist, GSK1440115, in asthma
Autor: Alison D Portnoy, Sanjay eKumar, David J Behm, Kelly M Mahr, Robert B Noble, John eThroup, Steven F Russ
Publikováno v: Frontiers in Pharmacology, Vol 4 (2013)
Background: Urotensin II (U-II) is highly expressed in the human lung and has been implicated in regulating respiratory physiology in preclinical studies. Our objective was to test antagonism of the urotensin receptor (UT) by GSK1440115, a novel, com
Externí odkaz: https://doaj.org/article/6464b7f4f5a54965914d203a037451d0
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2
Akademický článek
Comparison of soluble guanylate cyclase stimulators and activators in models of cardiovascular disease associated with oxidative stress
Autor: Melissa H Costell, Nicolas eAncellin, Roberta E Bernard, Shufang eZhao, John J Upson, Lisa A Morgan, Kristeen eHauk, Alan R Olzinski, Victoria L T Ballard, Kenny eHerry, Pascal eGrondin, Nerina eDodic, Olivier eMirguet, Anne eBouillot, Francoise eGellibert, Robert W Coatney, John J Lepore, Beat M. Jucker, Larry J Jolivette, Robert N Willette, Christine G Schnackenberg, David J Behm
Publikováno v: Frontiers in Pharmacology, Vol 3 (2012)
Soluble guanylate cyclase (sGC), the primary mediator of nitric oxide (NO) bioactivity, exists as reduced (NO-sensitive) and oxidized (NO-insensitive) forms. We tested the hypothesis that the cardiovascular protective effects of NO-insensitive sGC ac
Externí odkaz: https://doaj.org/article/7de0d838ef7f45aba69ae237f3a44947
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3
Targeting pulmonary capillary permeability to reduce lung congestion in heart failure: a randomized, controlled pilot trial
Autor: Glenn M. Stewart, Dennis L. Sprecher, Bruce D. Johnson, Christina Fillmore, Brad Bart, David J. Behm, Barry A. Borlaug, Anna Oughton, Steven R. Goldsmith, Masaru Obokata, Yogesh N.V. Reddy
Publikováno v: European Journal of Heart Failure. 22:1641-1645
Aims Lung congestion in patients with heart failure (HF) has traditionally been treated using interventions that reduce pulmonary capillary hydrostatic pressure. The transient receptor potential vanilloid 4 (TRPV4) channel regulates fluid transit acr
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::486d3acac82bd5f92b895132569b317b
https://doi.org/10.1002/ejhf.1809
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5
Identification, Synthesis, and Characterization of a Major Circulating Human Metabolite of TRPV4 Antagonist GSK2798745
Autor: John J. McAtee, Jacques Briand, David J. Behm, Karl F. Erhard, Andrew D. Roberts, Ralph A. Rivero, Brian G. Lawhorn, Joseph E. Pero, Grazyna Graczyk-Millbrandt, Dennis A. Holt
Publikováno v: ACS Med Chem Lett
[Image: see text] GSK2798745, an antagonist of the transient receptor potential vanilloid 4 (TRPV4) ion channel, was recently investigated in clinical trials for the treatment of cardiac and respiratory diseases. Human plasma and urine samples collec
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5b6d51b5ede72ceaac42c737d6c5900d
https://europepmc.org/articles/PMC8436415/
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6
Adaptive study design to assess effect of TRPV4 inhibition in patients with chronic cough
Autor: Valerie J. Ludbrook, James L. Kreindler, Misba Beerahee, Joanna Marks-Konczalik, Lorcan McGarvey, Jaclyn A. Smith, Nick P. Bird, SM Parker, Surinder S. Birring, Kate E Hanrott, David J. Behm, Alyn H. Morice, Debbie A Hewens
Publikováno v: Ludbrook, V J, Hanrott, K E, Kreindler, J L, Marks-Konczalik, J E, Bird, N P, Hewens, D A, Beerahee, M, Behm, D J, Morice, A, McGarvey, L, Parker, S M, Birring, S S & Smith, J 2021, ' Adaptive study design to assess effect of TRPV4 inhibition in patients with chronic cough ', ERJ Open Research, vol. 7, no. 3 . https://doi.org/10.1183/23120541.00269-2021
ERJ Open Research, Vol 7, Iss 3 (2021)
ERJ Open Research
article-version (VoR) Version of Record
Objective Airway sensory nerves involved in the cough reflex are activated by adenosine triphosphate (ATP) agonism of P2X purinoceptor 3 (P2X3) receptors. Transient receptor potential vanilloid 4 (TRPV4) channel activation causes ATP release from air
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dd3833a0555ff8bfff77b9a02a3d1dd6
https://www.research.manchester.ac.uk/portal/en/publications/adaptive-study-design-to-assess-effect-of-trpv4-inhibition-in-patients-with-chronic-cough(3d1d9e41-0831-44cc-bee7-6632854417f2).html
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7
Discovery of GSK3527497: A Candidate for the Inhibition of Transient Receptor Potential Vanilloid-4 (TRPV4)
Autor: Joseph E. Pero, Dennis A. Holt, Carl Brooks, Matthews Jay M, Melissa H. Costell, Raynold Shenje, John J. McAtee, David J. Behm, Ralph A. Rivero, Larry J. Jolivette, Sanchez Robert, Brent W. Mccleland, Lamont Roscoe Terrell, Jaclyn R. Patterson, Edward J. Brnardic, Theresa J. Roethke, Brian G. Lawhorn, Linda S. Barton
Publikováno v: Journal of Medicinal Chemistry. 62:9270-9280
GSK3527497, a preclinical candidate for the inhibition of TRPV4, was identified starting from the previously reported pyrrolidine sulfonamide TRPV4 inhibitors 1 and 2. Optimization of projected human dose was accomplished by specifically focusing on
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5651a745bf69cfd3239b6d132d9cebae
https://doi.org/10.1021/acs.jmedchem.9b01247
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8
Discovery of GSK2798745: A Clinical Candidate for Inhibition of Transient Receptor Potential Vanilloid 4 (TRPV4)
Autor: Eidam Hilary Schenck, Theresa J. Roethke, Linda S. Barton, Fox Ryan Michael, Steve Zhao, Kevin S. Thorneloe, David J. Behm, Guosen Ye, Patrick Stoy, Mui Cheung, Tram H. Hoang, Dennis A. Holt, Krista B. Goodman, Brian G. Lawhorn, Marlys Hammond, Mark A. Hilfiker, Carl Brooks, Jaclyn R. Patterson
Publikováno v: ACS Med Chem Lett
[Image: see text] GSK2798745, a clinical candidate, was identified as an inhibitor of the transient receptor potential vanilloid 4 (TRPV4) ion channel for the treatment of pulmonary edema associated with congestive heart failure. We discuss the lead
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4a9fa0019b6d3c13ef62367e4364c46c
https://doi.org/10.1021/acsmedchemlett.9b00274
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9
TRPV4 antagonists: a patent review (2015-2020)
Autor: Brian G. Lawhorn, Edward J. Brnardic, David J. Behm
Publikováno v: Expert opinion on therapeutic patents. 31(9)
Introduction: Transient receptor potential vanilloid 4 (TRPV4) is an ion channel that is widely expressed and is activated by numerous chemical, osmotic and mechanical stimuli. By modulating Ca2+ e...
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2df174d61b286a551dea195f73405e07
https://pubmed.ncbi.nlm.nih.gov/33724130
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10
Identification of a Human Whole Blood-Based Endothelial Cell Impedance Assay for Assessing Clinical Transient Receptor Potential Vanilloid 4 Target Engagement Ex Vivo
Autor: Kevin S. Thorneloe, Theresa J. Roethke, Krista B. Goodman, Jaclyn R. Patterson, Dennis L. Sprecher, Navin Goyal, Melissa H. Costell, David J. Behm, Christian H. James, Patrick Stoy, Xiaoping Xu
Publikováno v: The Journal of pharmacology and experimental therapeutics. 376(3)
Transient receptor potential vanilloid 4 (TRPV4) channels expressed on pulmonary endothelial cells are activated by elevated pulmonary vascular pressure, resulting in endothelial shape change, pulmonary barrier disruption, and edema. As such, TRPV4 b
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::50663aab15250e2bcb3f8a1a370e399c
https://pubmed.ncbi.nlm.nih.gov/33376150
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