A novel super-potent neurokinin A receptor antagonist containing dehydroalanine.
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.
Lombardi
A
A
Centro Interuniveristario di Ricerca su Peptidi Bioattivi, Università di Napoli Federico II, Italy.
D'Agostino
B
B
Nastri
F
F
D'Andrea
L D
LD
Filippelli
A
A
Falciani
M
M
Rossi
F
F
Pavone
V
V
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
D010456:Peptides, Cyclic; D018041:Receptors, Neurokinin-2; C116640:neuronorm; C116639:neuronorm, delta-Ala(1)-; C090951:MEN 10627; C015102:dehydroalanine; D000409:Alanine