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

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 journal › Article › peer-review

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.

Original language	English
Pages (from-to)	86-89
Number of pages	4
Journal	Gaodeng Xuexiao Huaxue Xuebao/Chemical Journal of Chinese Universities
Volume	29
Issue number	1
Publication status	Published - Jan 2008
Externally published	Yes

Keywords

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

Cite this

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title = "Synthesis and evaluation of a trace for peripheral benzodiazepine receptors",

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.",

keywords = "Imidazol [1, 2-a] pyridine, Peripheral benzodiazepine receptor, Radioligand",

author = "Bin Li and Li, {Jian Feng} and Lei Fu and Sun, {Xiao Guang} and Liu, {Jian Jun} and Gang Huang",

year = "2008",

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T1 - Synthesis and evaluation of a trace for peripheral benzodiazepine receptors

AU - Li, Bin

AU - Li, Jian Feng

AU - Fu, Lei

AU - Sun, Xiao Guang

AU - Liu, Jian Jun

AU - Huang, Gang

PY - 2008/1

Y1 - 2008/1

N2 - 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.

AB - 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.

KW - Imidazol [1, 2-a] pyridine

KW - Peripheral benzodiazepine receptor

KW - Radioligand

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SN - 0251-0790

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JO - Gaodeng Xuexiao Huaxue Xuebao/Chemical Journal of Chinese Universities

JF - Gaodeng Xuexiao Huaxue Xuebao/Chemical Journal of Chinese Universities

IS - 1

ER -

Synthesis and evaluation of a trace for peripheral benzodiazepine receptors

Abstract

Keywords

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