Assuntos
Pericardite/complicações , Feminino , Hospitalização , Humanos , Masculino , Pessoa de Meia-Idade , Pericardite/patologia , Fatores de RiscoRESUMO
Non peptide products have been found to show nanomolar binding and functional affinities at the human tachykinin NK-2 receptor. The new antagonists do not possess stereogenic centers and their thermal behaviour in solution is featured by a peculiar set of conformational stereoisomers. A macroscopic viewpoint is preferentially adopted to rationalize the obtained results.
Assuntos
Peptídeos/farmacologia , Receptores da Neurocinina-2/antagonistas & inibidores , Cromatografia Líquida de Alta Pressão , Humanos , Ligantes , Espectrometria de Massas , Peptídeos/química , Peptídeos Cíclicos/farmacologia , Receptores da Neurocinina-2/química , Espectrofotometria Ultravioleta , EstereoisomerismoRESUMO
A series of cyclic pseudopeptides were synthesized containing the sequence -Trp-Phe-(D)-PhePsiCH2NH-, the terminal ends of which were bound to 2-carboxy succinate or enantiomerically enriched tricarballylic acid to give the final cyclic structures. These two molecules and their subsequent derivatives were screened for h-NK2 receptor binding and functional antagonist activity on the rabbit urinary bladder.