ANALOGS OF NEUROKININ-A(4-10) AFFORD PROTECTION AGAINST GASTRODUODENAL ULCERS IN RATS

被引：16

作者：

EVANGELISTA, S ^{[1
]}

MAGGI, CA ^{[1
]}

ROVERO, P ^{[1
]}

PATACCHINI, R ^{[1
]}

GIULIANI, S ^{[1
]}

GIACHETTI, A ^{[1
]}

机构：

[1] MENARINI PHARMACEUT,DEPT CHEM,I-50131 FLORENCE,ITALY

来源：

PEPTIDES | 1990年 / 11卷 / 02期

关键词：

Acetylsalicylic acid (ASA); Dulcerozine; Ethanol lesions; Gastric and duodenal ulcers; Indomethacin; Neurokinin A (NKA); NK-2; receptors; Peptides; Tachykinins (TKs);

D O I：

10.1016/0196-9781(90)90085-J

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：

We have developed a novel series of peptides, related to the NKA(4-10) sequence, in which substitution of selected amino acids determined variations in the affinity for the TK receptor subtypes. Subcutaneous pretreatment of rats with some peptides of this series reduced gastric ulcers induced by ethanol, indomethacin or acetylsalicylic acid (ASA) as well as duodenal ulcers induced by dulcerozine. In particular [Ala5]NKA(4-10) and [Ala5,βAla8]NKA(4-10) possess a broad spectrum of antiulcer activity which is long lasting and stronger than the precursor NKA(4-10). The observation that the prevention of ethanol-induced gastric lesions could be reversed by pretreatment with indomethacin favors the possible involvement of prostaglandins in the observed gastroprotection by TK analogs. © 1990.

引用

页码：293 / 297

页数：5

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