A NOVEL SUPER-POTENT NEUROKININ-A RECEPTOR ANTAGONIST CONTAINING DEHYDROALANINE

Authors
LOMBARDI A DAGOSTINO B NASTRI F DANDREA LD FILIPPELLI A FALCIANI M ROSSI F PAVONE V
Citation
A. Lombardi et al., A NOVEL SUPER-POTENT NEUROKININ-A RECEPTOR ANTAGONIST CONTAINING DEHYDROALANINE, Bioorganic & medicinal chemistry letters, 8(10), 1998, pp. 1153-1156
Citations number
22
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
8
Issue
10
Year of publication
1998
Pages
1153 - 1156
Database
ISI
SICI code
0960-894X(1998)8:10<1153:ANSNRA>2.0.ZU;2-X
Abstract
We report here the synthesis and preliminary pharmacological character ization of a novel Neurokinin A receptor antagonist. This molecule con tains a dehydroalanine residue. It displays a high conformational rigi dity and possesses very high activity. Its pharmacological properties as a neurokinin A receptor antagonist were assessed in in vitro experi ments on rat vas deferens and were compared to those of Neuronorm and MEN10627. (C) 1998 Elsevier Science Ltd. All rights reserved.