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A-425619 [1-isoquinolin-5-yl-3-(4-trifluoromethyl-benzyl)-urea], a novel transient receptor potential type V1 receptor antagonist, relieves pathophysiological pain associated with inflammation and tissue injury in rats.
Honore P, Wismer CT, Mikusa J, Zhu CZ, Zhong C, Gauvin DM, Gomtsyan A, El Kouhen R, Lee CH, Marsh K, Sullivan JP, Faltynek CR, Jarvis MF. Honore P, et al. Among authors: gauvin dm. J Pharmacol Exp Ther. 2005 Jul;314(1):410-21. doi: 10.1124/jpet.105.083915. Epub 2005 Apr 18. J Pharmacol Exp Ther. 2005. PMID: 15837818
A-740003 [N-(1-{[(cyanoimino)(5-quinolinylamino) methyl]amino}-2,2-dimethylpropyl)-2-(3,4-dimethoxyphenyl)acetamide], a novel and selective P2X7 receptor antagonist, dose-dependently reduces neuropathic pain in the rat.
Honore P, Donnelly-Roberts D, Namovic MT, Hsieh G, Zhu CZ, Mikusa JP, Hernandez G, Zhong C, Gauvin DM, Chandran P, Harris R, Medrano AP, Carroll W, Marsh K, Sullivan JP, Faltynek CR, Jarvis MF. Honore P, et al. Among authors: gauvin dm. J Pharmacol Exp Ther. 2006 Dec;319(3):1376-85. doi: 10.1124/jpet.106.111559. Epub 2006 Sep 18. J Pharmacol Exp Ther. 2006. PMID: 16982702
A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.
Jarvis MF, Honore P, Shieh CC, Chapman M, Joshi S, Zhang XF, Kort M, Carroll W, Marron B, Atkinson R, Thomas J, Liu D, Krambis M, Liu Y, McGaraughty S, Chu K, Roeloffs R, Zhong C, Mikusa JP, Hernandez G, Gauvin D, Wade C, Zhu C, Pai M, Scanio M, Shi L, Drizin I, Gregg R, Matulenko M, Hakeem A, Gross M, Johnson M, Marsh K, Wagoner PK, Sullivan JP, Faltynek CR, Krafte DS. Jarvis MF, et al. Proc Natl Acad Sci U S A. 2007 May 15;104(20):8520-5. doi: 10.1073/pnas.0611364104. Epub 2007 May 2. Proc Natl Acad Sci U S A. 2007. PMID: 17483457 Free PMC article.
Potentiation of analgesic efficacy but not side effects: co-administration of an α4β2 neuronal nicotinic acetylcholine receptor agonist and its positive allosteric modulator in experimental models of pain in rats.
Zhu CZ, Chin CL, Rustay NR, Zhong C, Mikusa J, Chandran P, Salyers A, Gomez E, Simler G, Lewis LG, Gauvin D, Baker S, Pai M, Tovcimak A, Brown J, Komater V, Fox GB, Decker MW, Jacobson PB, Gopalakrishnan M, Lee CH, Honore P. Zhu CZ, et al. Biochem Pharmacol. 2011 Oct 15;82(8):967-76. doi: 10.1016/j.bcp.2011.05.007. Epub 2011 May 17. Biochem Pharmacol. 2011. PMID: 21620806
P2X7-related modulation of pathological nociception in rats.
McGaraughty S, Chu KL, Namovic MT, Donnelly-Roberts DL, Harris RR, Zhang XF, Shieh CC, Wismer CT, Zhu CZ, Gauvin DM, Fabiyi AC, Honore P, Gregg RJ, Kort ME, Nelson DW, Carroll WA, Marsh K, Faltynek CR, Jarvis MF. McGaraughty S, et al. Among authors: gauvin dm. Neuroscience. 2007 Jun 8;146(4):1817-28. doi: 10.1016/j.neuroscience.2007.03.035. Epub 2007 May 3. Neuroscience. 2007. PMID: 17478048
TRPV1 receptors in the CNS play a key role in broad-spectrum analgesia of TRPV1 antagonists.
Cui M, Honore P, Zhong C, Gauvin D, Mikusa J, Hernandez G, Chandran P, Gomtsyan A, Brown B, Bayburt EK, Marsh K, Bianchi B, McDonald H, Niforatos W, Neelands TR, Moreland RB, Decker MW, Lee CH, Sullivan JP, Faltynek CR. Cui M, et al. J Neurosci. 2006 Sep 13;26(37):9385-93. doi: 10.1523/JNEUROSCI.1246-06.2006. J Neurosci. 2006. PMID: 16971522 Free PMC article.
36 results