A novel super-potent neurokinin A receptor antagonist containing dehydroalanine

被引：10
|
作者：
Lombardi, A
D'Agostino, B
Nastri, F
D'Andrea, LD
Filippelli, A
Falciani, M
Rossi, F
Pavone, V
机构：
[1] Univ Naples Federico II, CNR, Ctr Interuniv Ric Peptidi Bioattivi, I-80134 Naples, Italy
[2] Univ Naples Federico II, CNR, Ctr Studio Biocristallog, I-80134 Naples, Italy
[3] Univ Naples 2, Ist Farmacol & Tossicol, I-80100 Naples, Italy
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 10期
关键词：
D O I：
10.1016/S0960-894X(98)00178-4
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
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. (C) 1998 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：1153 / 1156
页数：4
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