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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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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
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container_end_page 1740
container_issue 13
container_start_page 1735
container_title Bioorganic & medicinal chemistry letters
container_volume 8
creator Lombardi, Angela
D'Agostino, Bruno
Filippelli, Amelia
Pedone, Carlo
Matera, Maria Gabriella
Falciani, Maddalena
De Rosa, Mario
Rossi, Francesco
Pavone, Vincenzo
description 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.
doi_str_mv 10.1016/S0960-894X(98)00282-0
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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
title Neuronorm is a potent and water soluble neurokinin A receptor antagonist
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