THE ROLE OF THE VAL(353) RESIDUE IN ANTAGONIST BINDING TO RAT CCK-B RECEPTORS

被引：4

作者：

MALATYNSKA, E

KNAPP, RJ

STROPOVA, D

VARGA, E

YAMAMURA, HI

机构：

[1] UNIV ARIZONA,ARIZONA HLTH SCI CTR,DEPT PHARMACOL,TUCSON,AZ 85724

[2] UNIV ARIZONA,ARIZONA HLTH SCI CTR,DEPT BIOCHEM,TUCSON,AZ 85724

[3] UNIV ARIZONA,ARIZONA HLTH SCI CTR,DEPT PSYCHIAT,TUCSON,AZ 85724

[4] UNIV ARIZONA,ARIZONA HLTH SCI CTR,PROGRAM NEUROSCI,TUCSON,AZ 85724

来源：

NEUROREPORT | 1995年 / 6卷 / 09期

关键词：

SITE-DIRECTED MUTAGENESIS; UNIQUE SITE ELIMINATION METHOD; RECEPTORS; SNF-8702; PEPTOID ANTAGONISTS; CAM-1028; ASPERLICINE DERIVATIVES; DEVAZEPIDE; L-365,260;

D O I：

10.1097/00001756-199506090-00024

中图分类号：

Q189 [神经科学];

学科分类号：

071006 ;

摘要：

THE Val(353) residue of the rat cholecystokinin-B (CCK-B) receptor was mutated to Leu to test whether this residue is part of a binding site for antagonists having different chemical structures. The agonist radioligand [H-3]SNF 8702 showed similar affinity for both wild-type and mutant receptors. Mutation of the CCK-B receptor reversed the order of affinities for the asperlicin derivatives from L-365,260 > devazepide (wild-type) to devazepide > L-365,260 (mutant) but had no effect on the affinity of the peptoid CCK-B receptor antagonist Cam-1028. The results show that Val(353) is not part of a general CCK-B receptor antagonist recognition site and that Cam-1028 is recognized at a receptor site distinct from that binding asperlicin derivatives.

引用

页码：1325 / 1329

页数：5

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