176714-24-2Relevant articles and documents
Modification of the potent peptide FK888 with unusual aminoacids: Effects on activity on neurokinin receptors
Caliendo,Greco,Grieco,Perissutti,Santagada,Calignano,Mancuso,Novellino
, p. 197 - 201 (2007/10/03)
We report on the synthesis and the pharmacological properties of a new series of tachykinin antagonists based on the peptide N2-[(4R)-4-hydroxy-1-[(1-methyl-1H-indol-3-yl)carbonyl]-L-prolyl]-N-m ethyl-N-(phe-nylmethyl)-3-(2-naphthyl)-L-alaninamide (FK888) modified on the (2-naphthyl)-L-alanine and the [(1-methyl-1H-indol-3-yl)carbonyl] moieties. The compounds were tested on guinea pig ileum for NK-1, rat colon for NK-2 and rat portal vein for NK-3 receptors. The two most potent peptides of this series, 1b and 2d, were selective for the NK-2 receptor (pA2 = 7.5 and 7.3, respectively).