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The discovery of 4-(3-pentylamino)-2,7-dimethyl-8-(2-methyl-4-methoxyphenyl)-pyrazolo-[1 ,5-a]-pyrimidine: a corticotropin-releasing factor (hCRF1) antagonist.
Gilligan PJ, Baldauf C, Cocuzza A, Chidester D, Zaczek R, Fitzgerald LW, McElroy J, Smith MA, Shen HS, Saye JA, Christ D, Trainor G, Robertson DW, Hartig P. Gilligan PJ, et al. Among authors: hartig p. Bioorg Med Chem. 2000 Jan;8(1):181-9. doi: 10.1016/s0968-0896(99)00271-0. Bioorg Med Chem. 2000. PMID: 10968277
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
Gilligan PJ, Clarke T, He L, Lelas S, Li YW, Heman K, Fitzgerald L, Miller K, Zhang G, Marshall A, Krause C, McElroy JF, Ward K, Zeller K, Wong H, Bai S, Saye J, Grossman S, Zaczek R, Arneric SP, Hartig P, Robertson D, Trainor G. Gilligan PJ, et al. Among authors: hartig p. J Med Chem. 2009 May 14;52(9):3084-92. doi: 10.1021/jm900025h. J Med Chem. 2009. PMID: 19361209
8-(4-Methoxyphenyl)pyrazolo[1,5-a]-1,3,5-triazines: selective and centrally active corticotropin-releasing factor receptor-1 (CRF1) antagonists.
Gilligan PJ, He L, Clarke T, Tivitmahaisoon P, Lelas S, Li YW, Heman K, Fitzgerald L, Miller K, Zhang G, Marshall A, Krause C, McElroy J, Ward K, Shen H, Wong H, Grossman S, Nemeth G, Zaczek R, Arneric SP, Hartig P, Robertson DW, Trainor G. Gilligan PJ, et al. Among authors: hartig p. J Med Chem. 2009 May 14;52(9):3073-83. doi: 10.1021/jm9000242. J Med Chem. 2009. PMID: 19361210
Imidazo[4,5-b]pyridines as corticotropin releasing factor receptor ligands.
Arvanitis AG, Rescinito JT, Arnold CR, Wilde RG, Cain GA, Sun JH, Yan JS, Teleha CA, Fitzgerald LW, McElroy J, Zaczek R, Hartig PR, Grossman S, Arneric SP, Gilligan PJ, Olson RE, Robertson DW. Arvanitis AG, et al. Among authors: hartig pr. Bioorg Med Chem Lett. 2003 Jan 6;13(1):125-8. doi: 10.1016/s0960-894x(02)00833-8. Bioorg Med Chem Lett. 2003. PMID: 12467631
Imidazo[4,5-c]pyridines as corticotropin releasing factor receptor ligands.
Arvanitis AG, Rescinito JT, Arnold CR, Wilde RG, Fitzgerald LW, Zaczek R, Hartig PR, Grossman S, Arneric SP, Gilligan PJ, Olson RE, Robertson DW. Arvanitis AG, et al. Among authors: hartig pr. Bioorg Med Chem Lett. 2003 Jan 6;13(1):129-31. doi: 10.1016/s0960-894x(02)00834-x. Bioorg Med Chem Lett. 2003. PMID: 12467632
Anxiolytic-like effects of the corticotropin-releasing factor1 (CRF1) antagonist DMP904 [4-(3-pentylamino)-2,7-dimethyl-8-(2-methyl-4-methoxyphenyl)-pyrazolo-[1,5-a]-pyrimidine] administered acutely or chronically at doses occupying central CRF1 receptors in rats.
Lelas S, Wong H, Li YW, Heman KL, Ward KA, Zeller KL, Sieracki KK, Polino JL, Godonis HE, Ren SX, Yan XX, Arneric SP, Robertson DW, Hartig PR, Grossman S, Trainor GL, Taub RA, Zaczek R, Gilligan PJ, McElroy JF. Lelas S, et al. Among authors: hartig pr. J Pharmacol Exp Ther. 2004 Apr;309(1):293-302. doi: 10.1124/jpet.103.058784. Epub 2004 Jan 23. J Pharmacol Exp Ther. 2004. PMID: 14742750
Presenilin-1 and -2 are molecular targets for gamma-secretase inhibitors.
Seiffert D, Bradley JD, Rominger CM, Rominger DH, Yang F, Meredith JE Jr, Wang Q, Roach AH, Thompson LA, Spitz SM, Higaki JN, Prakash SR, Combs AP, Copeland RA, Arneric SP, Hartig PR, Robertson DW, Cordell B, Stern AM, Olson RE, Zaczek R. Seiffert D, et al. Among authors: hartig pr. J Biol Chem. 2000 Nov 3;275(44):34086-91. doi: 10.1074/jbc.M005430200. J Biol Chem. 2000. PMID: 10915801 Free article.
145 results