Evaluation of [18F]VUF 5000 as a potential PET ligand for brain imaging of the histamine H3 receptor

被引：31
作者：
Windhorst, AD
Timmerman, H
Klok, RP
Menge, WMPB
Leurs, R
Herscheid, JDM
机构：
[1] Vrije Univ Amsterdam, Radionuclide Ctr, NL-1081 HV Amsterdam, Netherlands
[2] Vrije Univ Amsterdam, Div Med Chem, Leiden Amsterdam Ctr Drug Res, NL-1081 HV Amsterdam, Netherlands
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 1999年 / 7卷 / 09期
关键词：
histamine H-3 receptor; VUF; 5000; thioperamide; F-18; biodistribution; positron emission tomography;
D O I：
10.1016/S0968-0896(99)00108-X
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：
[F-18]VUF 5000 was evaluated as a potential PET ligand for the histamine H-3 receptor. In the rat a high uptake of [F-18]VUF 5000 was observed in liver, lung and kidney and a low uptake in the brain. In order to explain these findings we determined the LogD(oct,7.2) of [F-18]VUF 5000, studied the biodistribution in the presence of carrier VUF 5000, modified [F-18]VUF 5000 chemically and studied the binding of [F-18]VUF 5000 to human serum albumin. From the results of these experiments it was concluded that [F-18]VUF 5000 is not suitable as a PET ligand for brain imaging of the histamine H-3 receptor, since [F-18]VUF 5000 hardly penetrates into the brain. (C) 1999 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：1761 / 1767
页数：7
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