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 re...

Full description

Saved in:
Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1998-05, Vol.8 (10), p.1153-1156
Main Authors: Lombardi, Angela, D'Agostino, Bruno, Nastri, Flavia, D'Andrea, Luca D., Filippelli, Amelia, Falciani, Maddalena, Rossi, Francesco, Pavone, Vincenzo
Format: Article
Language:English
Subjects:
Alanine - analogs & derivatives
Amino Acid Sequence
Animals
Biological and medical sciences
Male
Medical sciences
Models, Molecular
Molecular Structure
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems
Peptides, Cyclic - chemical synthesis
Peptides, Cyclic - chemistry
Peptides, Cyclic - pharmacology
Pharmacology. Drug treatments
Protein Conformation
Rats
Receptors, Neurokinin-2 - antagonists & inhibitors
Structure-Activity Relationship
Vas Deferens - drug effects
Vas Deferens - physiology
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary: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. The synthesis and preliminary in vitro pharmacological characterization of Δ- Ala 1- Neuronorm, a highly constrained bicyclic hexa-peptide, are reported.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(98)00178-4