74 related articles for article (PubMed ID: 19963378)
1. Synthesis and pharmacological characterization of constrained analogues of Vestipitant as in vitro potent and orally active NK(1) receptor antagonists.
Sabbatini FM; Di Fabio R; Griffante C; Pentassuglia G; Zonzini L; Melotto S; Alvaro G; Capelli AM; Pippo L; Perdona' E; St Denis Y; Costa S; Corsi M
Bioorg Med Chem Lett; 2010 Jan; 20(2):623-7. PubMed ID: 19963378
[TBL] [Abstract][Full Text] [Related]
2. Discovery process and pharmacological characterization of 2-(S)-(4-fluoro-2-methylphenyl)piperazine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethylphenyl)ethyl]methylamide (vestipitant) as a potent, selective, and orally active NK1 receptor antagonist.
Di Fabio R; Griffante C; Alvaro G; Pentassuglia G; Pizzi DA; Donati D; Rossi T; Guercio G; Mattioli M; Cimarosti Z; Marchioro C; Provera S; Zonzini L; Montanari D; Melotto S; Gerrard PA; Trist DG; Ratti E; Corsi M
J Med Chem; 2009 May; 52(10):3238-47. PubMed ID: 19388677
[TBL] [Abstract][Full Text] [Related]
3. Discovery of potent, balanced and orally active dual NK1/NK3 receptor ligands.
Peters JU; Hoffmann T; Schnider P; Stadler H; Koblet A; Alker A; Poli SM; Ballard TM; Spooren W; Steward L; Sleight AJ
Bioorg Med Chem Lett; 2010 Jun; 20(11):3405-8. PubMed ID: 20430616
[TBL] [Abstract][Full Text] [Related]
4. Cellular and behavioural profile of the novel, selective neurokinin1 receptor antagonist, vestipitant: a comparison to other agents.
Brocco M; Dekeyne A; Mannoury la Cour C; Touzard M; Girardon S; Veiga S; de Nanteuil G; deJong TR; Olivier B; Millan MJ
Eur Neuropsychopharmacol; 2008 Oct; 18(10):729-50. PubMed ID: 18657401
[TBL] [Abstract][Full Text] [Related]
5. Piperazinyl oxime ethers as NK-1 receptor antagonists.
van den Hoogenband A; van Maarseveen JH; McCreary AC; Mulder AT; van Scharrenburg GJ; van Stuivenberg HH; Zethof TJ; Zijta B; Iwema Bakker WI
Bioorg Med Chem Lett; 2006 Feb; 16(4):1045-8. PubMed ID: 16289817
[TBL] [Abstract][Full Text] [Related]
6. Discovery of a series of potent, orally active α,α-disubstituted piperidine NK(1) antagonists.
Xiao D; Wang C; Palani A; Tsui HC; Reichard G; Paliwal S; Shih NY; Aslanian R; Duffy R; Lachowicz J; Varty G; Morgan C; Liu F; Nomeir A
Bioorg Med Chem Lett; 2010 Nov; 20(21):6313-5. PubMed ID: 20846861
[TBL] [Abstract][Full Text] [Related]
7. Senktide-induced gerbil foot tapping behaviour is blocked by selective tachykinin NK1 and NK3 receptor antagonists.
Sundqvist M; Kristensson E; Adolfsson R; Leffler A; Ahlstedt I; Engberg S; Drmota T; Sigfridsson K; Jussila R; de Verdier J; Novén A; Johansson A; Påhlman I; von Mentzer B; Lindström E
Eur J Pharmacol; 2007 Dec; 577(1-3):78-86. PubMed ID: 17920583
[TBL] [Abstract][Full Text] [Related]
8. Novel 3-phenylpiperidine-4-carboxamides as highly potent and orally long-acting neurokinin-1 receptor antagonists with reduced CYP3A induction.
Shirai J; Sugiyama H; Morimoto S; Maezaki H; Yamamoto Y; Okanishi S; Kamo I; Matsumoto S; Ishigami K; Inatomi N; Imanishi A; Kawamoto M; Tarui N; Hashimoto T; Ikeura Y
Bioorg Med Chem; 2012 Jan; 20(2):962-77. PubMed ID: 22189275
[TBL] [Abstract][Full Text] [Related]
9. Discovery and biological characterization of (2R,4S)-1'-acetyl-N-{(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl}-2-(4-fluoro-2-methylphenyl)-N-methyl-4,4'-bipiperidine-1-carboxamide as a new potent and selective neurokinin 1 (NK1) receptor antagonist clinical candidate.
Di Fabio R; Alvaro G; Griffante C; Pizzi DA; Donati D; Mattioli M; Cimarosti Z; Guercio G; Marchioro C; Provera S; Zonzini L; Montanari D; Melotto S; Gerrard PA; Trist DG; Ratti E; Corsi M
J Med Chem; 2011 Feb; 54(4):1071-9. PubMed ID: 21229983
[TBL] [Abstract][Full Text] [Related]
10. Identification, biological characterization and pharmacophoric analysis of a new potent and selective NK1 receptor antagonist clinical candidate.
Di Fabio R; Alvaro G; Braggio S; Carletti R; Gerrard PA; Griffante C; Marchioro C; Pozzan A; Melotto S; Poffe A; Piccoli L; Ratti E; Tranquillini E; Trower M; Spada S; Corsi M
Bioorg Med Chem; 2013 Nov; 21(21):6264-73. PubMed ID: 24075145
[TBL] [Abstract][Full Text] [Related]
11. The NK1 receptor antagonist NKP608 lacks anxiolytic-like activity in Swiss-Webster mice exposed to the elevated plus-maze.
Rodgers RJ; Gentsch C; Hoyer D; Bryant E; Green AJ; Kolokotroni KZ; Martin JL
Behav Brain Res; 2004 Sep; 154(1):183-92. PubMed ID: 15302124
[TBL] [Abstract][Full Text] [Related]
12. Design and synthesis of a novel, achiral class of highly potent and selective, orally active neurokinin-1 receptor antagonists.
Hoffmann T; Bös M; Stadler H; Schnider P; Hunkeler W; Godel T; Galley G; Ballard TM; Higgins GA; Poli SM; Sleight AJ
Bioorg Med Chem Lett; 2006 Mar; 16(5):1362-5. PubMed ID: 16332435
[TBL] [Abstract][Full Text] [Related]
13. Piperidyl amides as novel, potent and orally active mGlu5 receptor antagonists with anxiolytic-like activity.
Spanka C; Glatthar R; Desrayaud S; Fendt M; Orain D; Troxler T; Vranesic I
Bioorg Med Chem Lett; 2010 Jan; 20(1):184-8. PubMed ID: 19931453
[TBL] [Abstract][Full Text] [Related]
14. Neurokinin 1 receptor antagonists: correlation between in vitro receptor interaction and in vivo efficacy.
Lindström E; von Mentzer B; Påhlman I; Ahlstedt I; Uvebrant A; Kristensson E; Martinsson R; Novén A; de Verdier J; Vauquelin G
J Pharmacol Exp Ther; 2007 Sep; 322(3):1286-93. PubMed ID: 17575073
[TBL] [Abstract][Full Text] [Related]
15. 5-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-2,3'-bipyridine: a highly potent, orally active metabotropic glutamate subtype 5 (mGlu5) receptor antagonist with anxiolytic activity.
Roppe JR; Wang B; Huang D; Tehrani L; Kamenecka T; Schweiger EJ; Anderson JJ; Brodkin J; Jiang X; Cramer M; Chung J; Reyes-Manalo G; Munoz B; Cosford ND
Bioorg Med Chem Lett; 2004 Aug; 14(15):3993-6. PubMed ID: 15225713
[TBL] [Abstract][Full Text] [Related]
16. Rational design, synthesis, and structure-activity relationship of benzoxazolones: new potent mglu5 receptor antagonists based on the fenobam structure.
Ceccarelli SM; Jaeschke G; Buettelmann B; Huwyler J; Kolczewski S; Peters JU; Prinssen E; Porter R; Spooren W; Vieira E
Bioorg Med Chem Lett; 2007 Mar; 17(5):1302-6. PubMed ID: 17189691
[TBL] [Abstract][Full Text] [Related]
17. Tetrahydroindolizinone NK1 antagonists.
Bao J; Lu H; Morriello GJ; Carlson EJ; Wheeldon A; Chicchi GG; Kurtz MM; Tsao KL; Zheng S; Tong X; Mills SG; DeVita RJ
Bioorg Med Chem Lett; 2010 Apr; 20(7):2354-8. PubMed ID: 20188553
[TBL] [Abstract][Full Text] [Related]
18. N-heteroaryl-2-phenyl-3-(benzyloxy)piperidines: a novel class of potent orally active human NK1 antagonists.
Ladduwahetty T; Baker R; Cascieri MA; Chambers MS; Haworth K; Keown LE; MacIntyre DE; Metzger JM; Owen S; Rycroft W; Sadowski S; Seward EM; Shepheard SL; Swain CJ; Tattersall FD; Watt AP; Williamson DW; Hargreaves RJ
J Med Chem; 1996 Jul; 39(15):2907-14. PubMed ID: 8709125
[TBL] [Abstract][Full Text] [Related]
19. Discovery and stereoselective synthesis of the novel isochroman neurokinin-1 receptor antagonist 'CJ-17,493'.
Shishido Y; Wakabayashi H; Koike H; Ueno N; Nukui S; Yamagishi T; Murata Y; Naganeo F; Mizutani M; Shimada K; Fujiwara Y; Sakakibara A; Suga O; Kusano R; Ueda S; Kanai Y; Tsuchiya M; Satake K
Bioorg Med Chem; 2008 Aug; 16(15):7193-205. PubMed ID: 18640044
[TBL] [Abstract][Full Text] [Related]
20. Cyclic urea derivatives as potent NK1 selective antagonists. Part II: Effects of fluoro and benzylic methyl substitutions.
Shue HJ; Chen X; Schwerdt JH; Paliwal S; Blythin DJ; Lin L; Gu D; Wang C; Reichard GA; Wang H; Piwinski JJ; Duffy RA; Lachowicz JE; Coffin VL; Nomeir AA; Morgan CA; Varty GB; Shih NY
Bioorg Med Chem Lett; 2006 Feb; 16(4):1065-9. PubMed ID: 16290143
[TBL] [Abstract][Full Text] [Related]
[Next] [New Search]
