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Pharmacological properties of MK-3207, a potent and orally active calcitonin gene-related peptide receptor antagonist.
Salvatore CA, Moore EL, Calamari A, Cook JJ, Michener MS, O'Malley S, Miller PJ, Sur C, Williams DL Jr, Zeng Z, Danziger A, Lynch JJ, Regan CP, Fay JF, Tang YS, Li CC, Pudvah NT, White RB, Bell IM, Gallicchio SN, Graham SL, Selnick HG, Vacca JP, Kane SA. Salvatore CA, et al. Among authors: selnick hg. J Pharmacol Exp Ther. 2010 Apr;333(1):152-60. doi: 10.1124/jpet.109.163816. Epub 2010 Jan 11. J Pharmacol Exp Ther. 2010. PMID: 20065019
First demonstration of cerebrospinal fluid and plasma A beta lowering with oral administration of a beta-site amyloid precursor protein-cleaving enzyme 1 inhibitor in nonhuman primates.
Sankaranarayanan S, Holahan MA, Colussi D, Crouthamel MC, Devanarayan V, Ellis J, Espeseth A, Gates AT, Graham SL, Gregro AR, Hazuda D, Hochman JH, Holloway K, Jin L, Kahana J, Lai MT, Lineberger J, McGaughey G, Moore KP, Nantermet P, Pietrak B, Price EA, Rajapakse H, Stauffer S, Steinbeiser MA, Seabrook G, Selnick HG, Shi XP, Stanton MG, Swestock J, Tugusheva K, Tyler KX, Vacca JP, Wong J, Wu G, Xu M, Cook JJ, Simon AJ. Sankaranarayanan S, et al. Among authors: selnick hg. J Pharmacol Exp Ther. 2009 Jan;328(1):131-40. doi: 10.1124/jpet.108.143628. Epub 2008 Oct 14. J Pharmacol Exp Ther. 2009. PMID: 18854490
Novel CGRP receptor antagonists through a design strategy of target simplification with addition of molecular flexibility.
Wood MR, Schirripa KM, Kim JJ, Quigley AG, Stump CA, Bell IM, Bednar RA, Fay JF, Bruno JG, Moore EL, Mosser SD, Roller S, Salvatore CA, Kane SA, Vacca JP, Selnick HG. Wood MR, et al. Among authors: selnick hg. Bioorg Med Chem Lett. 2009 Oct 1;19(19):5787-90. doi: 10.1016/j.bmcl.2009.07.134. Epub 2009 Aug 6. Bioorg Med Chem Lett. 2009. PMID: 19703767
Identification of potent, highly constrained CGRP receptor antagonists.
Stump CA, Bell IM, Bednar RA, Fay JF, Gallicchio SN, Hershey JC, Jelley R, Kreatsoulas C, Moore EL, Mosser SD, Quigley AG, Roller SA, Salvatore CA, Sharik SS, Theberge CR, Zartman CB, Kane SA, Graham SL, Selnick HG, Vacca JP, Williams TM. Stump CA, et al. Among authors: selnick hg. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2572-6. doi: 10.1016/j.bmcl.2010.02.086. Epub 2010 Feb 25. Bioorg Med Chem Lett. 2010. PMID: 20299218
MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats.
Bell IM, Stump CA, Gallicchio SN, Staas DD, Zartman CB, Moore EL, Sain N, Urban M, Bruno JG, Calamari A, Kemmerer AL, Mosser SD, Fandozzi C, White RB, Zrada MM, Selnick HG, Graham SL, Vacca JP, Kane SA, Salvatore CA. Bell IM, et al. Among authors: selnick hg. Bioorg Med Chem Lett. 2012 Jun 15;22(12):3941-5. doi: 10.1016/j.bmcl.2012.04.105. Epub 2012 Apr 30. Bioorg Med Chem Lett. 2012. PMID: 22607672
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: selnick hg. 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.
Discovery of MK-3207: A Highly Potent, Orally Bioavailable CGRP Receptor Antagonist.
Bell IM, Gallicchio SN, Wood MR, Quigley AG, Stump CA, Zartman CB, Fay JF, Li CC, Lynch JJ, Moore EL, Mosser SD, Prueksaritanont T, Regan CP, Roller S, Salvatore CA, Kane SA, Vacca JP, Selnick HG. Bell IM, et al. Among authors: selnick hg. ACS Med Chem Lett. 2010 Jan 12;1(1):24-9. doi: 10.1021/ml900016y. eCollection 2010 Apr 8. ACS Med Chem Lett. 2010. PMID: 24900170 Free PMC article.
52 results