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 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 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 1 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

Fingerprint Dive into the research topics of 'In vitro and in vivo evaluation of [<sup>18</sup>F]FHTP as a potential dopamine D<sub>4</sub> receptor PET imaging agent'. Together they form a unique fingerprint.

  • Cite this

    Li, G. C., Yin, D. Z., Cheng, D. F., Zheng, M. Q., Han, Y. J., Cai, H. C., Xia, J. Y., Liang, S., Xu, W. B., & Wang, Y. X. (2009). In vitro and in vivo evaluation of [18F]FHTP as a potential dopamine D4 receptor PET imaging agent. Journal of Radioanalytical and Nuclear Chemistry, 280(1), 15-20. https://doi.org/10.1007/s10967-008-7373-6