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Journal of Radioanalytical and Nuclear Chemistry
Authors: 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, and Yong-Xian Wang

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 D4 receptor.

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