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153 results

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GPR139, an Orphan Receptor Highly Enriched in the Habenula and Septum, Is Activated by the Essential Amino Acids L-Tryptophan and L-Phenylalanine.
Liu C, Bonaventure P, Lee G, Nepomuceno D, Kuei C, Wu J, Li Q, Joseph V, Sutton SW, Eckert W, Yao X, Yieh L, Dvorak C, Carruthers N, Coate H, Yun S, Dugovic C, Harrington A, Lovenberg TW. Liu C, et al. Among authors: eckert w. Mol Pharmacol. 2015 Nov;88(5):911-25. doi: 10.1124/mol.115.100412. Epub 2015 Sep 8. Mol Pharmacol. 2015. PMID: 26349500
Characterization of 2-(2,6-dichloro-benzyl)-thiazolo[5,4-d]pyrimidin-7-yl]-(4-trifluoromethyl-phenyl)-amine (JNJ-39729209) as a novel TRPV1 antagonist.
Maher MP, Bhattacharya A, Ao H, Swanson N, Wu NT, Freedman J, Kansagara M, Scott B, Li DH, Eckert WA 3rd, Liu Y, Sepassi K, Rizzolio M, Fitzgerald A, Liu J, Branstetter BJ, Rech JC, Lebsack AD, Breitenbucher JG, Wickenden AD, Chaplan SR. Maher MP, et al. Eur J Pharmacol. 2011 Aug 1;663(1-3):40-50. doi: 10.1016/j.ejphar.2011.05.001. Epub 2011 May 10. Eur J Pharmacol. 2011. PMID: 21575625
Discovery of a novel series of selective HCN1 blockers.
McClure KJ, Maher M, Wu N, Chaplan SR, Eckert WA 3rd, Lee DH, Wickenden AD, Hermann M, Allison B, Hawryluk N, Breitenbucher JG, Grice CA. McClure KJ, et al. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5197-201. doi: 10.1016/j.bmcl.2011.07.051. Epub 2011 Jul 23. Bioorg Med Chem Lett. 2011. PMID: 21824780
The discovery and preclinical characterization of 6-chloro-N-(2-(4,4-difluoropiperidin-1-yl)-2-(2-(trifluoromethyl)pyrimidin-5-yl)ethyl)quinoline-5-carboxamide based P2X7 antagonists.
Rech JC, Bhattacharya A, Branstetter BJ, Love CJ, Leenaerts JE, Cooymans LP, Eckert WA 3rd, Ao H, Wang Q, Chaplan SR, Wickenden AD, Lebsack AD, Breitenbucher JG. Rech JC, et al. Bioorg Med Chem Lett. 2016 Oct 1;26(19):4781-4784. doi: 10.1016/j.bmcl.2016.08.029. Epub 2016 Aug 20. Bioorg Med Chem Lett. 2016. PMID: 27595421
Insensitivity to pain induced by a potent selective closed-state Nav1.7 inhibitor.
Flinspach M, Xu Q, Piekarz AD, Fellows R, Hagan R, Gibbs A, Liu Y, Neff RA, Freedman J, Eckert WA, Zhou M, Bonesteel R, Pennington MW, Eddinger KA, Yaksh TL, Hunter M, Swanson RV, Wickenden AD. Flinspach M, et al. Among authors: eckert wa. Sci Rep. 2017 Jan 3;7:39662. doi: 10.1038/srep39662. Sci Rep. 2017. PMID: 28045073 Free PMC article.
153 results