New substance P receptor antagonists.: Conception, synthesis and biological evaluation of spirolactam derivatives and their tripeptide Cbz-Pro-Leu-Trp-OBzl(CF3)2 and lactam pseudopeptide derivatives

被引：8

作者：

Millet, R

Goossens, L

Bertrand-Caumont, K

Houssin, R

Rigo, B

Goossens, JF

Hénichart, JP

机构：

[1] Univ Lille 2, EA 2692, Inst Chim Pharmaceut Albert Lespagnol, F-59006 Lille, France

[2] Ecole Hautes Etud Ind, Lab Ingn Mol, F-59046 Lille, France

来源：

LETTERS IN PEPTIDE SCIENCE | 2000年 / 7卷 / 05期

关键词：

NK1; pseudopeptide; spirolactam; Substance P; tachykinins; tryptophan;

D O I：

10.1023/A:1011867801367

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

New chemical entities were designed from the C-terminal sequence of GR71251, an NK1 pseudopeptide antagonist. Three new NK1 antagonists were identified with high affinity and selectivity for NK1 receptors.

引用

页码：269 / 279

页数：11

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