1060807-69-3Relevant academic research and scientific papers
Synthesis and pharmacological characterization of constrained analogues of Vestipitant as in vitro potent and orally active NK1 receptor antagonists
Sabbatini, Fabio M.,Fabio, Romano Di,Griffante, Cristiana,Pentassuglia, Giorgio,Zonzini, Laura,Melotto, Sergio,Alvaro, Giuseppe,Capelli, Anna M.,Pippo, Lara,Perdona', Elisabetta,Denis, Yves St.,Costa, Silvano,Corsi, Mauro
scheme or table, p. 623 - 627 (2010/06/12)
A focused exploration targeting conformationally restricted analogues of Vestipitant, resulted in the discovery of novel, in vitro potent NK1 antagonists. In particular, two of the compounds reported exhibited a good pharmacokinetic (PK) profile and produced anxiolytic-like effects in the gerbil foot tapping (GFT) in vivo model.
