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Page 1
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. Among authors: chaplan sr. 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
Identification and biological evaluation of 4-(3-trifluoromethylpyridin-2-yl)piperazine-1-carboxylic acid (5-trifluoromethylpyridin-2-yl)amide, a high affinity TRPV1 (VR1) vanilloid receptor antagonist.
Swanson DM, Dubin AE, Shah C, Nasser N, Chang L, Dax SL, Jetter M, Breitenbucher JG, Liu C, Mazur C, Lord B, Gonzales L, Hoey K, Rizzolio M, Bogenstaetter M, Codd EE, Lee DH, Zhang SP, Chaplan SR, Carruthers NI. Swanson DM, et al. Among authors: chaplan sr. J Med Chem. 2005 Mar 24;48(6):1857-72. doi: 10.1021/jm0495071. J Med Chem. 2005. PMID: 15771431
Role of peripheral hyperpolarization-activated cyclic nucleotide-modulated channel pacemaker channels in acute and chronic pain models in the rat.
Luo L, Chang L, Brown SM, Ao H, Lee DH, Higuera ES, Dubin AE, Chaplan SR. Luo L, et al. Among authors: chaplan sr. Neuroscience. 2007 Feb 23;144(4):1477-85. doi: 10.1016/j.neuroscience.2006.10.048. Epub 2006 Dec 29. Neuroscience. 2007. PMID: 17196750
Previously, we documented that systemic administration of ZD7288, a specific blocker of pacemaker current (I(h)), decreased ectopic activity in dorsal root ganglion (DRG) and reversed tactile allodynia in spinal nerve ligated (SNL) rats [Chaplan SR, Guo HQ, Lee DH, …
Previously, we documented that systemic administration of ZD7288, a specific blocker of pacemaker current (I(h)), decreased ectopic activity …
Pharmacology and antitussive efficacy of 4-(3-trifluoromethyl-pyridin-2-yl)-piperazine-1-carboxylic acid (5-trifluoromethyl-pyridin-2-yl)-amide (JNJ17203212), a transient receptor potential vanilloid 1 antagonist in guinea pigs.
Bhattacharya A, Scott BP, Nasser N, Ao H, Maher MP, Dubin AE, Swanson DM, Shankley NP, Wickenden AD, Chaplan SR. Bhattacharya A, et al. Among authors: chaplan sr. J Pharmacol Exp Ther. 2007 Nov;323(2):665-74. doi: 10.1124/jpet.107.127258. Epub 2007 Aug 9. J Pharmacol Exp Ther. 2007. PMID: 17690251
Activation of TRPA1 by farnesyl thiosalicylic acid.
Maher M, Ao H, Banke T, Nasser N, Wu NT, Breitenbucher JG, Chaplan SR, Wickenden AD. Maher M, et al. Among authors: chaplan sr. Mol Pharmacol. 2008 Apr;73(4):1225-34. doi: 10.1124/mol.107.042663. Epub 2008 Jan 2. Mol Pharmacol. 2008. PMID: 18171730
Novel ketooxazole based inhibitors of fatty acid amide hydrolase (FAAH).
Timmons A, Seierstad M, Apodaca R, Epperson M, Pippel D, Brown S, Chang L, Scott B, Webb M, Chaplan SR, Breitenbucher JG. Timmons A, et al. Among authors: chaplan sr. Bioorg Med Chem Lett. 2008 Mar 15;18(6):2109-13. doi: 10.1016/j.bmcl.2008.01.091. Epub 2008 Jan 30. Bioorg Med Chem Lett. 2008. PMID: 18289847
Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.
Keith JM, Apodaca R, Xiao W, Seierstad M, Pattabiraman K, Wu J, Webb M, Karbarz MJ, Brown S, Wilson S, Scott B, Tham CS, Luo L, Palmer J, Wennerholm M, Chaplan S, Breitenbucher JG. Keith JM, et al. Bioorg Med Chem Lett. 2008 Sep 1;18(17):4838-43. doi: 10.1016/j.bmcl.2008.07.081. Epub 2008 Jul 25. Bioorg Med Chem Lett. 2008. PMID: 18693015
Identification and synthesis of 2,7-diamino-thiazolo[5,4-d]pyrimidine derivatives as TRPV1 antagonists.
Lebsack AD, Branstetter BJ, Hack MD, Xiao W, Peterson ML, Nasser N, Maher MP, Ao H, Bhattacharya A, Kansagara M, Scott BP, Luo L, Rynberg R, Rizzolio M, Chaplan SR, Wickenden AD, Guy Breitenbucher J. Lebsack AD, et al. Among authors: chaplan sr. Bioorg Med Chem Lett. 2009 Jan 1;19(1):40-6. doi: 10.1016/j.bmcl.2008.11.024. Epub 2008 Nov 13. Bioorg Med Chem Lett. 2009. PMID: 19038548
Biochemical and biological properties of 4-(3-phenyl-[1,2,4] thiadiazol-5-yl)-piperazine-1-carboxylic acid phenylamide, a mechanism-based inhibitor of fatty acid amide hydrolase.
Karbarz MJ, Luo L, Chang L, Tham CS, Palmer JA, Wilson SJ, Wennerholm ML, Brown SM, Scott BP, Apodaca RL, Keith JM, Wu J, Breitenbucher JG, Chaplan SR, Webb M. Karbarz MJ, et al. Among authors: chaplan sr. Anesth Analg. 2009 Jan;108(1):316-29. doi: 10.1213/ane.0b013e31818c7cbd. Anesth Analg. 2009. PMID: 19095868
64 results