Synthesis and evaluation of a trace for peripheral benzodiazepine receptors

Document Type

Article

Publication Date

1-1-2008

Abstract

The 2-iodophenyl-imidazo[1, 2-a]-pyridines tirfluoromethyl derivative (ITFZOL) was prepared to study the PBR. The [125I] analogue was prepared via iododestannylation reaction in radiochemical yields of 75%-85% and a specific activity >76 GBq/μmol. After injection of [125I] ITFZOL into mice through the tail vein, high accumulations of radioactivity were found in PBR-rich tissues such as adrenal, lung, kidney, heart, olfactory bulb and cerebellum. Per-administration of PBR-selective PK11195 displayed a significant reduction of radioactivity, suggesting a high specific binding of [125I] ITFZOL to PBR. The biological data reveal that [125I] ITFZOL is a potential and selective single photo emitting radioligand for PBR.

Publication Source (Journal or Book title)

Gaodeng Xuexiao Huaxue Xuebao/Chemical Journal of Chinese Universities

First Page

86

Last Page

89

This document is currently not available here.

Share

COinS