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 journalArticle

3 Citations (Scopus)

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.

Original languageEnglish (US)
Pages (from-to)15-20
Number of pages6
JournalJournal of Radioanalytical and Nuclear Chemistry
Volume280
Issue number1
DOIs
StatePublished - Apr 2009

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Dopamine D4 Receptors
Dopamine Receptors
Metabolism
Rats
Dopamine
Brain
Imaging techniques
In Vitro Techniques

ASJC Scopus subject areas

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

Cite this

In vitro and in vivo evaluation of [18F]FHTP as a potential dopamine D4 receptor PET imaging agent. / Li, Gu Cai; Yin, Duan Zhi; Cheng, Deng Feng; Zheng, Ming Qiang; Han, Yan Jiang; Cai, Han Chen; Xia, Jiao Yun; Liang, Sheng; Xu, Wan Bang; Wang, Yong Xian.

In: Journal of Radioanalytical and Nuclear Chemistry, Vol. 280, No. 1, 04.2009, p. 15-20.

Research output: Contribution to journalArticle

Li, Gu Cai ; Yin, Duan Zhi ; Cheng, Deng Feng ; Zheng, Ming Qiang ; Han, Yan Jiang ; Cai, Han Chen ; Xia, Jiao Yun ; Liang, Sheng ; Xu, Wan Bang ; Wang, Yong Xian. / In vitro and in vivo evaluation of [18F]FHTP as a potential dopamine D4 receptor PET imaging agent. In: Journal of Radioanalytical and Nuclear Chemistry. 2009 ; Vol. 280, No. 1. pp. 15-20.
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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

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