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In vitro and in vivo characterization of JNJ-31020028 (N-(4-{4-[2-(diethylamino)-2-oxo-1-phenylethyl]piperazin-1-yl}-3-fluorophenyl)-2-pyridin-3-ylbenzamide), a selective brain penetrant small molecule antagonist of the neuropeptide Y Y(2) receptor.
Shoblock JR, Welty N, Nepomuceno D, Lord B, Aluisio L, Fraser I, Motley ST, Sutton SW, Morton K, Galici R, Atack JR, Dvorak L, Swanson DM, Carruthers NI, Dvorak C, Lovenberg TW, Bonaventure P. Shoblock JR, et al. Among authors: morton k. Psychopharmacology (Berl). 2010 Feb;208(2):265-77. doi: 10.1007/s00213-009-1726-x. Epub 2009 Dec 2. Psychopharmacology (Berl). 2010. PMID: 19953226
Pre-clinical characterization of aryloxypyridine amides as histamine H3 receptor antagonists: identification of candidates for clinical development.
Letavic MA, Aluisio L, Atack JR, Bonaventure P, Carruthers NI, Dugovic C, Everson A, Feinstein MA, Fraser IC, Hoey K, Jiang X, Keith JM, Koudriakova T, Leung P, Lord B, Lovenberg TW, Ly KS, Morton KL, Motley ST, Nepomuceno D, Rizzolio M, Rynberg R, Sepassi K, Shelton J. Letavic MA, et al. Among authors: morton kl. Bioorg Med Chem Lett. 2010 Jul 15;20(14):4210-4. doi: 10.1016/j.bmcl.2010.05.041. Epub 2010 May 16. Bioorg Med Chem Lett. 2010. PMID: 20561786
The discovery and synthesis of JNJ 31020028, a small molecule antagonist of the Neuropeptide Y Y₂ receptor.
Swanson DM, Wong VD, Jablonowski JA, Shah C, Rudolph DA, Dvorak CA, Seierstad M, Dvorak LK, Morton K, Nepomuceno D, Atack JR, Bonaventure P, Lovenberg TW, Carruthers NI. Swanson DM, et al. Among authors: morton k. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5552-6. doi: 10.1016/j.bmcl.2011.06.136. Epub 2011 Jul 18. Bioorg Med Chem Lett. 2011. PMID: 21802951
Novel substituted pyrrolidines are high affinity histamine H3 receptor antagonists.
Stocking EM, Aluisio L, Atack JR, Bonaventure P, Carruthers NI, Dugovic C, Everson A, Fraser I, Jiang X, Leung P, Lord B, Ly KS, Morton KL, Nepomuceno D, Shah CR, Shelton J, Soyode-Johnson A, Letavic MA. Stocking EM, et al. Bioorg Med Chem Lett. 2010 May 1;20(9):2755-60. doi: 10.1016/j.bmcl.2010.03.071. Epub 2010 Mar 20. Bioorg Med Chem Lett. 2010. PMID: 20382018
Indole- and benzothiophene-based histamine H3 antagonists.
Santillan A Jr, McClure KJ, Allison BD, Lord B, Boggs JD, Morton KL, Everson AM, Nepomuceno D, Letavic MA, Lee-Dutra A, Lovenberg TW, Carruthers NI, Grice CA. Santillan A Jr, et al. Bioorg Med Chem Lett. 2010 Nov 1;20(21):6226-30. doi: 10.1016/j.bmcl.2010.08.103. Epub 2010 Aug 27. Bioorg Med Chem Lett. 2010. PMID: 20843691
Novel benzamide-based histamine h3 receptor antagonists: the identification of two candidates for clinical development.
Letavic MA, Aluisio L, Apodaca R, Bajpai M, Barbier AJ, Bonneville A, Bonaventure P, Carruthers NI, Dugovic C, Fraser IC, Kramer ML, Lord B, Lovenberg TW, Li LY, Ly KS, Mcallister H, Mani NS, Morton KL, Ndifor A, Nepomuceno SD, Pandit CR, Sands SB, Shah CR, Shelton JE, Snook SS, Swanson DM, Xiao W. Letavic MA, et al. ACS Med Chem Lett. 2015 Mar 13;6(4):450-4. doi: 10.1021/ml5005156. eCollection 2015 Apr 9. ACS Med Chem Lett. 2015. PMID: 25893048 Free PMC article.
Synthesis and Pharmacological Characterization of Two Novel, Brain Penetrating P2X7 Antagonists.
Letavic MA, Lord B, Bischoff F, Hawryluk NA, Pieters S, Rech JC, Sales Z, Velter AI, Ao H, Bonaventure P, Contreras V, Jiang X, Morton KL, Scott B, Wang Q, Wickenden AD, Carruthers NI, Bhattacharya A. Letavic MA, et al. ACS Med Chem Lett. 2013 Mar 12;4(4):419-22. doi: 10.1021/ml400040v. eCollection 2013 Apr 11. ACS Med Chem Lett. 2013. PMID: 24900687 Free PMC article.
503 results