Synthesis and biological characterisation of [3H]BBL454, a new CCK2 selective radiolabelled agonist displaying original pharmacological properties

被引：5

作者：

Bellier, B

Dugave, C

Etivant, F

Genet, R

Gigoux, V

Garbay, C

机构：

[1] INSERM, U266,FRE CNRS 2463, UFR Sci Pharmaceut & Biol, Lab Pharmacochim Mol & Struct, F-75270 Paris 06, France

[2] Ctr Etud Nucl Saclay, Dept Ingn & Etud Prot, F-91191 Gif Sur Yvette, France

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 02期

关键词：

D O I：

10.1016/j.bmcl.2003.11.001

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

[H-3]BBL454, a new CCK2 selective tritiated agonist was prepared via the reductive tritiation of a 5-aminopentyn-1-yl moiety introduced on the N-terminal end of a pentapeptide derivative of cholecystokinin. The binding properties of this labelled compound were determined on CHO cells transfected with the rat CCK2 receptor. [H-3]BBL454 is able to discriminate two affinity states of the CCK2 receptor a supplementary indication of its validity for further exploring the heterogeneity of this receptor. (C) 2003 Elsevier Ltd. All rights reserved.

引用

页码：369 / 372

页数：4

共 20 条

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