| 19388677 |
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: 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. J Med Chem. 2009 May 28;52(10):3238-47.
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31(0,1,1,1) |
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| 12431064 |
MacKenzie AR, Marchington AP, Middleton DS, Newman SD, Jones BC: Structure-activity relationships of 1-alkyl-5-(3,4-dichlorophenyl)- 5-[2-[(3-substituted)-1-azetidinyl] ethyl]-2-piperidones. 1. J Med Chem. 2002 Nov 21;45(24):5365-77.
In addition, NK2 antagonist 33 (IC50 = 4 nM) showed excellent selectivity over both the related human neurokinin receptors h-NK1 (IC50 = 7.9 microM) and h-NK3 (IC50 = 1.8 microM) in radioligand binding studies. |
1(0,0,0,1) |
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