Synthesis and evaluation of a trace for peripheral benzodiazepine receptors

Bin Li*, Jian Feng Li, Lei Fu, Xiao Guang Sun, Jian Jun Liu, Gang Huang

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review


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.

Original languageEnglish
Pages (from-to)86-89
Number of pages4
JournalGaodeng Xuexiao Huaxue Xuebao/Chemical Journal of Chinese Universities
Issue number1
Publication statusPublished - Jan 2008
Externally publishedYes


  • Imidazol [1, 2-a] pyridine
  • Peripheral benzodiazepine receptor
  • Radioligand

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