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.
ASJC Scopus subject areas
- Analytical Chemistry
- Nuclear Energy and Engineering
- Radiology Nuclear Medicine and imaging
- Public Health, Environmental and Occupational Health
- Health, Toxicology and Mutagenesis