Neuronorm is a potent and water soluble neurokinin A receptor antagonist

We report here the synthesis and preliminary pharmacological characterization of a novel water soluble Neurokinin A receptor antagonist named Neuronorm. The synthesis was achieved in high yield by a combination of classical peptide synthesis methodologies, in both solution and solid phase. The pharm...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1998-07, Vol.8 (13), p.1735-1740
Main Authors: Lombardi, Angela, D'Agostino, Bruno, Filippelli, Amelia, Pedone, Carlo, Matera, Maria Gabriella, Falciani, Maddalena, De Rosa, Mario, Rossi, Francesco, Pavone, Vincenzo
Format: Article
Language:English
Subjects:
Animals
Biological and medical sciences
Guinea Pigs
In Vitro Techniques
Male
Medical sciences
Peptides, Cyclic - chemical synthesis
Peptides, Cyclic - pharmacology
Pharmacology. Drug treatments
Rats
Receptors, Neurokinin-2 - antagonists & inhibitors
Respiratory system
Trachea - drug effects
Vas Deferens - drug effects
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Summary:We report here the synthesis and preliminary pharmacological characterization of a novel water soluble Neurokinin A receptor antagonist named Neuronorm. The synthesis was achieved in high yield by a combination of classical peptide synthesis methodologies, in both solution and solid phase. The pharmacological properties as neurokinin A receptor antagonist were assessed in in vitro experiments on rat vas deferens and guinea pig trachea, and were compared to those of MEN 10627. The synthesis and preliminary pharmacological characterization of Neuronorm is reported. It represents a suitable candidate for therapeutic applications.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(98)00282-0