Zobrazeno 1 - 10
of 46
pro vyhledávání: '"Bruce R Bianchi"'
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 341:360-368
The transient receptor potential ankyrin-1 (TRPA1) channel has emerged as an attractive target for development of analgesic and anti-inflammatory drugs. However, drug discovery efforts targeting TRPA1 have been hampered by differences between human a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::370396d49a0293f7e20bda9d0621cc7c
https://doi.org/10.1124/jpet.111.189902
https://doi.org/10.1124/jpet.111.189902
Autor:
Heath A. McDonald, Bruce R. Bianchi, Connie R. Faltynek, James S. Polakowski, Guo Zhu Zheng, Ryan G. Keddy, Kennan C. Marsh, Robert G. Schmidt, John R. Koenig, Prisca Honore, Brian S. Brown, Michael F. Jarvis, Chih-Hung Lee, Carol S. Surowy
Publikováno v:
Bioorganic & Medicinal Chemistry. 16:8516-8525
A series of 1,2,3,6-tetrahydropyridyl-4-carboxamides, exemplified by 6, have been synthesized and evaluated for in vitro TRPV1 antagonist activity, and in vivo analgesic activity in animal pain models. The tetrahydropyridine 6 is a novel TRPV1 recept
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f448fc511e60c32bec5d4c117e9c376a
https://doi.org/10.1016/j.bmc.2008.08.005
https://doi.org/10.1016/j.bmc.2008.08.005
Autor:
Carol S. Surowy, Katharine L. Chu, Prisca Honore, Rachid El Kouhen, Connie R. Faltynek, Bruce R. Bianchi, Ping Han, James P. Sullivan, Steve McGaraughty, Wende Niforatos, Arthur Gomtsyan, Erol K. Bayburt, Chih-Hung Lee, Torben R. Neelands, Heath A. McDonald, Melissa H. Vos, Michael F. Jarvis
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 326:879-888
The transient receptor potential vanilloid (TRPV) 1 receptor, a nonselective cation channel expressed on peripheral sensory neurons and in the central nervous system, plays a key role in pain. TRPV1 receptor antagonism is a promising approach for pai
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d345e34dd8700b32db5ac00c4d0fbd47
https://doi.org/10.1124/jpet.108.138511
https://doi.org/10.1124/jpet.108.138511
Autor:
Sriajan N. Vaidyanathan, Bruce R. Bianchi, Torben R. Neelands, Robert B. Moreland, Bruce Surber, Carol S. Surowy, Rachid El Kouhen, Michael F. Jarvis, Chih-Hung Lee, Shirish N. Raja, Connie R. Faltynek, Arthur Gomtsyan, Heath A. McDonald, Pamela S. Puttfarcken
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 323:285-293
1-((R)-5- tert -Butyl-indan-1-yl)-3-isoquinolin-5-yl-urea (A-778317) is a novel, stereoselective, competitive antagonist that potently blocks transient receptor potential vanilloid-1 (TRPV1) receptor-mediated changes in intracellular calcium concentr
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2d56c87efa9cefdc29bae60c6ca62103
https://doi.org/10.1124/jpet.107.124305
https://doi.org/10.1124/jpet.107.124305
Modulation of human TRPV1 receptor activity by extracellular protons and host cell expression system
Autor:
Chih-Hung Lee, Michael F. Jarvis, Pamela S. Puttfarcken, Robert B. Moreland, Rachid El Kouhen, Bruce R. Bianchi, Connie R. Faltynek
Publikováno v:
European Journal of Pharmacology. 537:20-30
The transient receptor potential vanilloid 1 (TRPV1) receptor is a ligand-gated cation channel that can be activated by capsaicin, heat, protons and cytosolic lipids. We compared activation of recombinant human TRPV1 receptors stably expressed in hum
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e7aa8540c8b90cc2536fc8021a0007a4
https://doi.org/10.1016/j.ejphar.2006.03.003
https://doi.org/10.1016/j.ejphar.2006.03.003
Autor:
Joseph P. Mikusa, Michael F. Jarvis, Carol T. Wismer, Connie R. Faltynek, Chang Z. Zhu, Bruce R. Bianchi, Prisca Honore, Steve McGaraughty, Heath A. McDonald
Publikováno v:
British Journal of Pharmacology. 146:180-188
P2X3/P2X2/3 receptors have emerged as important components of nociception. However, there is limited information regarding the neurochemical systems that are affected by antagonism of the P2X3/P2X2/3 receptor and that ultimately contribute to the ens
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::3f81bd00e003ac9fe60ab08ef43d119e
https://doi.org/10.1038/sj.bjp.0706346
https://doi.org/10.1038/sj.bjp.0706346
Autor:
Connie R. Faltynek, Chih-Hung Lee, Wende Niforatos, James P. Sullivan, Michael F. Jarvis, Bruce R. Bianchi, Prisca Honore, Arthur Gomtsyan, Rachid El Kouhen, Carol S. Surowy, Heath A. McDonald, Torben R. Neelands
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 314:400-409
The vanilloid receptor transient receptor potential type V1 (TRPV1) integrates responses to multiple stimuli, such as capsaicin, acid, heat, and endovanilloids and plays an important role in the transmission of inflammatory pain. Here, we report the
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a4b4c5ce8babbf25816d89f0f8110c1d
https://doi.org/10.1124/jpet.105.084103
https://doi.org/10.1124/jpet.105.084103
Autor:
Prisca Honore, Joseph P. Mikusa, Heath A. McDonald, Jayne Cartmell, Michael F. Jarvis, Connie R. Faltynek, Bruce R. Bianchi
Publikováno v:
Pain. 96:99-105
Exogenous ATP has been shown to be algogenic in both animal and humans. Research has focused on the P2X3 ligand-gated ion channel, as it is preferentially expressed on nociceptive C-fibers. In addition, P2X3 receptor gene disrupted mice show decrease
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e0297c68f409b44b97c8d5ee1cd5b6f7
https://doi.org/10.1016/s0304-3959(01)00434-1
https://doi.org/10.1016/s0304-3959(01)00434-1
Autor:
Bruce R. Bianchi, Connie R. Faltynek, Edward C. Burgard, Clark A. Briggs, Michael F. Jarvis, Kevin J. Lynch, Katharine L. Chu, Heath A. McDonald, David G. McKenna, Jayne Cartmell
Publikováno v:
European Journal of Pharmacology. 435:135-142
In this study, the receptor desensitizing effects of diadenosine polyphosphates at recombinant human P2X3 (hP2X3) receptors were examined. Administration of Ap3A, Ap4A, Ap5A or Ap6A inhibited the hP2X3 receptor-mediated response to a subsequent appli
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e6b489068512c9d7c54d7b3c0e87d8a2
https://doi.org/10.1016/s0014-2999(01)01568-0
https://doi.org/10.1016/s0014-2999(01)01568-0
Autor:
Richard A. Nelson, Richard J. Perner, Andrew J. King, Robert G. Schmidt, Torben R. Neelands, Bruce R. Bianchi, Erol K. Bayburt, Eric A. Voight, Jason A. Segreti, S.K. Joshi, LaGeisha R. Lewis, Zhi Su, Heath A. McDonald, Jun Chen, Joseph P. Mikusa, Stanley Didomenico, Pamela S. Puttfarcken, Philip R. Kym, Ping Han, Donna Gauvin, Jerome F. Daanen, Connie R. Faltynek, Regina M. Reilly, Arthur Gomtsyan, Pamela H. Franklin, James S. Polakowski, Michael E. Kort, Scott J. Baker
Publikováno v:
Journal of medicinal chemistry. 57(17)
The synthesis and characterization of a series of selective, orally bioavailable 1-(chroman-4-yl)urea TRPV1 antagonists is described. Whereas first-generation antagonists that inhibit all modes of TRPV1 activation can elicit hyperthermia, the compoun
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::348e986dc77d986d6f8812eb33102527
https://pubmed.ncbi.nlm.nih.gov/25100568
https://pubmed.ncbi.nlm.nih.gov/25100568