CGRP ANTAGONIST ACTIVITY OF SHORT C-TERMINAL FRAGMENTS OF HUMAN ALPHA-CGRP, CGRP(23-37) AND CGRP(19-37)

被引：43

作者：

ROVERO, P ^{[1
]}

GIULIANI, S ^{[1
]}

MAGGI, CA ^{[1
]}

机构：

[1] A MENARINI PHARMACEUT,DEPT CHEM & PHARMACOL,VIA SETTE SANTI 3,I-50131 FLORENCE,ITALY

来源：

PEPTIDES | 1992年 / 13卷 / 05期

关键词：

CGRP; C-TERMINAL FRAGMENTS; CGRP ANTAGONIST;

D O I：

10.1016/0196-9781(92)90067-D

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：

The activity of short C-terminal fragments of human alpha calcitonin gene-related peptide (CGRP), CGRP(19-37), and CGRP(23-37), and of the N-terminally acetylated (Ac) derivative, AcCGRP(19-37), has been investigated in the guinea pig isolated left atria (electrically driven) for their ability to antagonize the positive inotropic effect of human alphaCGRP. All the peptides tested produced a rightward displacement of the curve to the agonist without depressing the maximal response: apparent pA2 Values were 5.39 and 4.81 for CGRP(19-37) and CGRP(23-37), respectively, as compared to 6.81 for CGRP(8-37). AcCGRP(19-37) was a more potent antagonist than the parent peptide, with an apparent pA2 value of 6.03.

引用

页码：1025 / 1027

页数：3

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