A HIGHLY SELECTIVE NK-2 TACHYKININ RECEPTOR ANTAGONIST CONTAINING D-TRYPTOPHAN

被引：47

作者：

ROVERO, P

PESTELLINI, V

MAGGI, CA

PATACCHINI, R

REGOLI, D

GIACHETTI, A

机构：

[1] A MENARINI PHARMACEUT,DEPT PHARMACOL,DIV SMOOTH MUSCLE,I-50131 FLORENCE,ITALY

[2] UNIV SHERBROOKE,SCH MED,DEPT PHARMACOL,SHERBROOKE J1H 5N4,QUEBEC,CANADA

来源：

EUROPEAN JOURNAL OF PHARMACOLOGY | 1990年 / 175卷 / 01期

关键词：

Tachykinin receptor antagonists; Tachykinins;

D O I：

10.1016/0014-2999(90)90161-X

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The classical approach used in the development of substance P (SP) antagonists, i.e. the introduction of multiple 3-tryptophan (D-Trp), was successfully extended to neurokinin A (NKA). Thus, a new NK-2-selective tachykinin receptor antagonist, namely [Tyr5, D-Trp6,8,9,Arg10]NKA-(4-10), was developed that had pA2 values of 5.2, 7.9 and 4.9 in three monoreceptor in vitro assays for NK-1, NK-2 and NK-3 tachykinin receptors, respectively. © 1990.

引用

页码：113 / 115

页数：3

共 7 条

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