Portal de Periódicos da CAPES

Conformational rigidity versus flexibility in a novel peptidic neurokinin A receptor antagonist

1995; Wiley; Volume: 1; Issue: 4 Linguagem: Inglês

10.1002/psc.310010404

1099-1387

Vincenzo Pavone, Angela Lombardi, Carlo Alberto Maggi, Laura Quartara, Carlo Pedone,

Neuropeptides and Animal Physiology

Neurokinin A receptor antagonists have been proposed as a new class of drugs for several applications in humans (asthma, intestinal motility, etc.). The rational design, synthesis, structural characterization and biological activity evaluation of a new potent, highly selective, long-lasting, peptide-based receptor antagonist are reported. The structure-activity relationship indicates that the conformational rigidity determines potency, specificity and especially the long life of the molecule in the living body. MEN10627 is the prototype of a new class of cyclic, peptide-based, neurokinin A receptor antagonists and it is a suitable candidate for clinical testing in humans.