Synthesis and Evaluation of a Trace for Peripheral Benzodiazepine Receptors

Chem. J. Chinese Universities

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Synthesis and Evaluation of a Trace for Peripheral Benzodiazepine Receptors

LI Bin¹, LI Jian-Feng², FU Lei³, SUN Xiao-Guang¹, LIU Jian-Jun¹, HUANG Gang¹*

1. Department of Nuclear Medicine, Renji Hospital, Medical School of Shanghai Jiaotong University, Shanghai 200127, China;
2. Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai 201203, China;
3. School of Pharmacy, Shanghai Jiaotong University, Shanghai 200030, China

Received:2007-04-23 Revised:1900-01-01 Online:2008-01-10 Published:2008-01-10
Contact: HUANG Gang

Abstract

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.

Key words: Peripheral benzodiazepine receptor, Radioligand, Imidazol[1,2-a]pyridine

CLC Number:

O626
O657

TrendMD:

LI Bin¹, LI Jian-Feng², FU Lei³, SUN Xiao-Guang¹, LIU Jian-Jun¹, HUANG Gang¹*. Synthesis and Evaluation of a Trace for Peripheral Benzodiazepine Receptors[J]. Chem. J. Chinese Universities, doi: .

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Synthesis and Evaluation of a Trace for Peripheral Benzodiazepine Receptors

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