title: A novel super-potent neurokinin A receptor antagonist containing dehydroalanine.
abstract: We report here the synthesis and preliminary pharmacological characterization of a novel Neurokinin A receptor antagonist. This molecule contains a dehydroalanine residue. It displays a high conformational rigidity and possesses very high activity. Its pharmacological properties as a neurokinin A receptor antagonist were assessed in in vitro experiments on rat vas deferens and were compared to those of Neuronorm and MEN10627.
authors.affiliation: Centro Interuniveristario di Ricerca su Peptidi Bioattivi, Università di Napoli Federico II, Italy.
authors.forename: A
authors.initials: A
authors.lastname: Lombardi
authors.forename: B
authors.initials: B
authors.lastname: D'Agostino
authors.forename: F
authors.initials: F
authors.lastname: Nastri
authors.forename: L D
authors.initials: LD
authors.lastname: D'Andrea
authors.forename: A
authors.initials: A
authors.lastname: Filippelli
authors.forename: M
authors.initials: M
authors.lastname: Falciani
authors.forename: F
authors.initials: F
authors.lastname: Rossi
authors.forename: V
authors.initials: V
authors.lastname: Pavone
mesh_terms: D000409:Alanine / Q000031:analogs & derivatives*; D000595:Amino Acid Sequence; D000818:Animals; D008297:Male; D008958:Models, Molecular; D015394:Molecular Structure; D010456:Peptides, Cyclic / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D011487:Protein Conformation; D051381:Rats; D018041:Receptors, Neurokinin-2 / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D014649:Vas Deferens / Q000187:drug effects / Q000502:physiology
chemical_list: D010456:Peptides, Cyclic; D018041:Receptors, Neurokinin-2; C116640:neuronorm; C116639:neuronorm, delta-Ala(1)-; C090951:MEN 10627; C015102:dehydroalanine; D000409:Alanine