title: Synthesis and pharmacological characterization of constrained analogues of Vestipitant as in vitro potent and orally active NK(1) receptor antagonists.
abstract: A focused exploration targeting conformationally restricted analogues of Vestipitant, resulted in the discovery of novel, in vitro potent NK(1) 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.
authors: Neurosciences Centre of Excellence for Drug Discovery and Molecular Discovery Research, GlaxoSmithKline Medicines Research Centre, Via A. Fleming 4, 37135 Verona, Italy. Fabio.M.Sabbatini@GSK.com
authors: Fabio M
authors: FM
authors: Sabbatini
authors: Romano
authors: R
authors: Di Fabio
authors: Cristiana
authors: C
authors: Griffante
authors: Giorgio
authors: G
authors: Pentassuglia
authors: Laura
authors: L
authors: Zonzini
authors: Sergio
authors: S
authors: Melotto
authors: Giuseppe
authors: G
authors: Alvaro
authors: Anna M
authors: AM
authors: Capelli
authors: Lara
authors: L
authors: Pippo
authors: Elisabetta
authors: E
authors: Perdona'
authors: Yves
authors: Y
authors: St Denis
authors: Silvano
authors: S
authors: Costa
authors: Mauro
authors: M
authors: Corsi
mesh_terms: D014151:Anti-Anxiety Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D015195:Drug Design; D005464:Fluorobenzenes; D006801:Humans; D008968:Molecular Conformation; D064729:Neurokinin-1 Receptor Antagonists; D010880:Piperidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D018040:Receptors, Neurokinin-1 / Q000378:metabolism
chemical_list: D014151:Anti-Anxiety Agents; D005464:Fluorobenzenes; D064729:Neurokinin-1 Receptor Antagonists; D010880:Piperidines; D018040:Receptors, Neurokinin-1; C534550:vestipitant