In vitro and in vivo evaluation of [18F]FHTP as a potential dopamine D4 receptor PET imaging agent

Gu Cai Li; Duan Zhi Yin; Deng Feng Cheng; Ming Qiang Zheng; Yan Jiang Han; Han Chen Cai; Jiao Yun Xia; Sheng Liang; Wan Bang Xu; Yong Xian Wang

doi:10.1007/s10967-008-7373-6

In vitro and in vivo evaluation of [¹⁸F]FHTP as a potential dopamine D₄ receptor PET imaging agent

Gu Cai Li, Duan Zhi Yin, Deng Feng Cheng, Ming Qiang Zheng, Yan Jiang Han, Han Chen Cai, Jiao Yun Xia, Sheng Liang, Wan Bang Xu, Yong Xian Wang

Research output: Contribution to journal › Article › peer-review

4 Scopus citations

Abstract

3-(4-[¹⁸F]fluorobenzyl)-8-hydroxy-1,2,3,4-tetrahydrochromeno[3, 4-c]pyridin-5-one ([¹⁸F]FHTP) was in vitro and in vivo evaluated as a putative dopamine D₄ receptor radioligand. Its inhibition constant (K _i ) for cloned human dopamine D_4.2 receptor was determined to be 2.9 nM and it displayed a 2000-fold D₄-selectivity over the D_2long subtype. Its partition coefficient (logP) was measured to be 1.11. Biodistribution, blocking distribution and metabolism studies in rats demonstrated that the specific distribution of [ ¹⁸F]FHTP in brain regions, suggesting that [¹⁸F]FHTP may be a suitable PET imaging agent for in vivo studies of the dopamine D ₄ receptor.

Original language	English (US)
Pages (from-to)	15-20
Number of pages	6
Journal	Journal of Radioanalytical and Nuclear Chemistry
Volume	280
Issue number	1
DOIs	https://doi.org/10.1007/s10967-008-7373-6
State	Published - Apr 2009

ASJC Scopus subject areas

Analytical Chemistry
Nuclear Energy and Engineering
Radiology Nuclear Medicine and imaging
Pollution
Spectroscopy
Public Health, Environmental and Occupational Health
Health, Toxicology and Mutagenesis

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title = "In vitro and in vivo evaluation of [18F]FHTP as a potential dopamine D4 receptor PET imaging agent",

abstract = "3-(4-[18F]fluorobenzyl)-8-hydroxy-1,2,3,4-tetrahydrochromeno[3, 4-c]pyridin-5-one ([18F]FHTP) was in vitro and in vivo evaluated as a putative dopamine D4 receptor radioligand. Its inhibition constant (K i ) for cloned human dopamine D4.2 receptor was determined to be 2.9 nM and it displayed a 2000-fold D4-selectivity over the D2long subtype. Its partition coefficient (logP) was measured to be 1.11. Biodistribution, blocking distribution and metabolism studies in rats demonstrated that the specific distribution of [ 18F]FHTP in brain regions, suggesting that [18F]FHTP may be a suitable PET imaging agent for in vivo studies of the dopamine D 4 receptor.",

author = "Li, {Gu Cai} and Yin, {Duan Zhi} and Cheng, {Deng Feng} and Zheng, {Ming Qiang} and Han, {Yan Jiang} and Cai, {Han Chen} and Xia, {Jiao Yun} and Sheng Liang and Xu, {Wan Bang} and Wang, {Yong Xian}",

note = "Funding Information: The authors thank Prof. JIN GUO-ZHANG (Shanghai Institute of Materia Medica, Chinese Academy of Sciences) and his research group for their help and guide in this work. This project was supported by the National Natural Science Foundation of China (No. 30371634) and by Hunan Provincial Natural Science Foundation of China (No. 07JJ6014).",

year = "2009",

month = apr,

doi = "10.1007/s10967-008-7373-6",

language = "English (US)",

volume = "280",

pages = "15--20",

journal = "Journal of Radioanalytical and Nuclear Chemistry",

issn = "0236-5731",

publisher = "Springer Netherlands",

number = "1",

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TY - JOUR

T1 - In vitro and in vivo evaluation of [18F]FHTP as a potential dopamine D4 receptor PET imaging agent

AU - Li, Gu Cai

AU - Yin, Duan Zhi

AU - Cheng, Deng Feng

AU - Zheng, Ming Qiang

AU - Han, Yan Jiang

AU - Cai, Han Chen

AU - Xia, Jiao Yun

AU - Liang, Sheng

AU - Xu, Wan Bang

AU - Wang, Yong Xian

N1 - Funding Information: The authors thank Prof. JIN GUO-ZHANG (Shanghai Institute of Materia Medica, Chinese Academy of Sciences) and his research group for their help and guide in this work. This project was supported by the National Natural Science Foundation of China (No. 30371634) and by Hunan Provincial Natural Science Foundation of China (No. 07JJ6014).

PY - 2009/4

Y1 - 2009/4

N2 - 3-(4-[18F]fluorobenzyl)-8-hydroxy-1,2,3,4-tetrahydrochromeno[3, 4-c]pyridin-5-one ([18F]FHTP) was in vitro and in vivo evaluated as a putative dopamine D4 receptor radioligand. Its inhibition constant (K i ) for cloned human dopamine D4.2 receptor was determined to be 2.9 nM and it displayed a 2000-fold D4-selectivity over the D2long subtype. Its partition coefficient (logP) was measured to be 1.11. Biodistribution, blocking distribution and metabolism studies in rats demonstrated that the specific distribution of [ 18F]FHTP in brain regions, suggesting that [18F]FHTP may be a suitable PET imaging agent for in vivo studies of the dopamine D 4 receptor.

AB - 3-(4-[18F]fluorobenzyl)-8-hydroxy-1,2,3,4-tetrahydrochromeno[3, 4-c]pyridin-5-one ([18F]FHTP) was in vitro and in vivo evaluated as a putative dopamine D4 receptor radioligand. Its inhibition constant (K i ) for cloned human dopamine D4.2 receptor was determined to be 2.9 nM and it displayed a 2000-fold D4-selectivity over the D2long subtype. Its partition coefficient (logP) was measured to be 1.11. Biodistribution, blocking distribution and metabolism studies in rats demonstrated that the specific distribution of [ 18F]FHTP in brain regions, suggesting that [18F]FHTP may be a suitable PET imaging agent for in vivo studies of the dopamine D 4 receptor.

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In vitro and in vivo evaluation of [¹⁸F]FHTP as a potential dopamine D₄ receptor PET imaging agent

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