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Inhibition of capsaicin-induced increase in dermal blood flow by the oral CGRP receptor antagonist, telcagepant (MK-0974).
Sinclair SR, Kane SA, Van der Schueren BJ, Xiao A, Willson KJ, Boyle J, de Lepeleire I, Xu Y, Hickey L, Denney WS, Li CC, Palcza J, Vanmolkot FH, Depré M, Van Hecken A, Murphy MG, Ho TW, de Hoon JN. Sinclair SR, et al. Among authors: kane sa. Br J Clin Pharmacol. 2010 Jan;69(1):15-22. doi: 10.1111/j.1365-2125.2009.03543.x. Br J Clin Pharmacol. 2010. PMID: 20078608 Free PMC article. Clinical Trial.
Calcitonin gene-related peptide8-37 antagonizes capsaicin-induced vasodilation in the skin: evaluation of a human in vivo pharmacodynamic model.
Van der Schueren BJ, Rogiers A, Vanmolkot FH, Van Hecken A, Depré M, Kane SA, De Lepeleire I, Sinclair SR, de Hoon JN. Van der Schueren BJ, et al. Among authors: kane sa. J Pharmacol Exp Ther. 2008 Apr;325(1):248-55. doi: 10.1124/jpet.107.133868. Epub 2008 Jan 23. J Pharmacol Exp Ther. 2008. PMID: 18216286 Clinical Trial.
In vivo quantification of calcitonin gene-related peptide receptor occupancy by telcagepant in rhesus monkey and human brain using the positron emission tomography tracer [11C]MK-4232.
Hostetler ED, Joshi AD, Sanabria-Bohórquez S, Fan H, Zeng Z, Purcell M, Gantert L, Riffel K, Williams M, O'Malley S, Miller P, Selnick HG, Gallicchio SN, Bell IM, Salvatore CA, Kane SA, Li CC, Hargreaves RJ, de Groot T, Bormans G, Van Hecken A, Derdelinckx I, de Hoon J, Reynders T, Declercq R, De Lepeleire I, Kennedy WP, Blanchard R, Marcantonio EE, Sur C, Cook JJ, Van Laere K, Evelhoch JL. Hostetler ED, et al. Among authors: kane sa. J Pharmacol Exp Ther. 2013 Nov;347(2):478-86. doi: 10.1124/jpet.113.206458. Epub 2013 Aug 23. J Pharmacol Exp Ther. 2013. PMID: 23975906 Free article. Clinical Trial.
Pharmacological characterization of MK-0974 [N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide], a potent and orally active calcitonin gene-related peptide receptor antagonist for the treatment of migraine.
Salvatore CA, Hershey JC, Corcoran HA, Fay JF, Johnston VK, Moore EL, Mosser SD, Burgey CS, Paone DV, Shaw AW, Graham SL, Vacca JP, Williams TM, Koblan KS, Kane SA. Salvatore CA, et al. Among authors: kane sa. J Pharmacol Exp Ther. 2008 Feb;324(2):416-21. doi: 10.1124/jpet.107.130344. Epub 2007 Nov 26. J Pharmacol Exp Ther. 2008. PMID: 18039958
138 results