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Discovery of (1R,6S)-5-[4-(1-cyclobutyl-piperidin-4-yloxy)-phenyl]-3,4-diaza-bicyclo[4.1.0]hept-4-en-2-one (R,S-4a): histamine H(3) receptor inverse agonist demonstrating potent cognitive enhancing and wake promoting activity.
Hudkins RL, Josef KA, Becknell NC, Aimone LD, Lyons JA, Mathiasen JR, Gruner JA, Raddatz R. Hudkins RL, et al. Among authors: mathiasen jr. Bioorg Med Chem Lett. 2014 Mar 1;24(5):1303-6. doi: 10.1016/j.bmcl.2014.01.061. Epub 2014 Jan 30. Bioorg Med Chem Lett. 2014. PMID: 24513042
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.
Hudkins RL, Raddatz R, Tao M, Mathiasen JR, Aimone LD, Becknell NC, Prouty CP, Knutsen LJ, Yazdanian M, Moachon G, Ator MA, Mallamo JP, Marino MJ, Bacon ER, Williams M. Hudkins RL, et al. Among authors: mathiasen jr. J Med Chem. 2011 Jul 14;54(13):4781-92. doi: 10.1021/jm200401v. Epub 2011 Jun 2. J Med Chem. 2011. PMID: 21634396
Identification of pyridazin-3-one derivatives as potent, selective histamine H₃ receptor inverse agonists with robust wake activity.
Hudkins RL, Aimone LD, Bailey TR, Bendesky RJ, Dandu RR, Dunn D, Gruner JA, Josef KA, Lin YG, Lyons J, Marcy VR, Mathiasen JR, Sundar BG, Tao M, Zulli AL, Raddatz R, Bacon ER. Hudkins RL, et al. Among authors: mathiasen jr. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5493-7. doi: 10.1016/j.bmcl.2011.06.108. Epub 2011 Jun 30. Bioorg Med Chem Lett. 2011. PMID: 21782432
Synthesis and evaluation of pyridazinone-phenethylamine derivatives as selective and orally bioavailable histamine H3 receptor antagonists with robust wake-promoting activity.
Dandu RR, Gruner JA, Mathiasen JR, Aimone LD, Hostetler G, Benfield C, Bendesky RJ, Marcy VR, Raddatz R, Hudkins RL. Dandu RR, et al. Among authors: mathiasen jr. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6362-5. doi: 10.1016/j.bmcl.2011.08.104. Epub 2011 Sep 1. Bioorg Med Chem Lett. 2011. PMID: 21944855
CEP-26401 (irdabisant), a potent and selective histamine H₃ receptor antagonist/inverse agonist with cognition-enhancing and wake-promoting activities.
Raddatz R, Hudkins RL, Mathiasen JR, Gruner JA, Flood DG, Aimone LD, Le S, Schaffhauser H, Duzic E, Gasior M, Bozyczko-Coyne D, Marino MJ, Ator MA, Bacon ER, Mallamo JP, Williams M. Raddatz R, et al. Among authors: mathiasen jr. J Pharmacol Exp Ther. 2012 Jan;340(1):124-33. doi: 10.1124/jpet.111.186585. Epub 2011 Oct 14. J Pharmacol Exp Ther. 2012. PMID: 22001260
4,5-dihydropyridazin-3-one derivatives as histamine H₃ receptor inverse agonists.
Hudkins RL, Aimone LD, Dandu RR, Dunn D, Gruner JA, Huang Z, Josef KA, Lyons JA, Mathiasen JR, Tao M, Zulli AL, Raddatz R. Hudkins RL, et al. Among authors: mathiasen jr. Bioorg Med Chem Lett. 2012 Jan 1;22(1):194-8. doi: 10.1016/j.bmcl.2011.11.037. Epub 2011 Nov 16. Bioorg Med Chem Lett. 2012. PMID: 22142542
Novel brain penetrant benzofuropiperidine 5-HT₆ receptor antagonists.
Sundar BG, Bailey TR, Dunn DD, Bacon ER, Salvino JM, Morton GC, Aimone LD, Zeqi H, Mathiasen JR, Dicamillo A, Huffman MJ, McKenna BA, Kopec K, Lu LD, Brown R, Qian J, Angeles T, Connors T, Spais C, Holskin B, Galinis D, Duzic E, Schaffhauser H, Rosse GC. Sundar BG, et al. Among authors: mathiasen jr. Bioorg Med Chem Lett. 2012 Jan 1;22(1):120-3. doi: 10.1016/j.bmcl.2011.11.050. Epub 2011 Nov 22. Bioorg Med Chem Lett. 2012. PMID: 22153937
52 results