| Popis: |
A series of twenty-nine new quinazoline-2,4-dione compounds were synthesized and their IC(50) values for binding toward sphingosine-1-phosphate receptor 2 (S1PR2) were determined using a [(32)P]S1P binding assay. Seven compounds 2a, 2g, 2h, 2i, 2j, 2k, and 5h exhibit high S1PR2 binding potencies (IC(50) values < 50 nM) and four of these new compounds 2g, 2i, 2j, and 2k have IC(50) values (98%), and high molar activity (153–222 GBq μmol(−1), at the end of bombardment). [(11)C]2a and [(11)C]2i were further evaluated by the ex vivo biodistribution study. The results showed that both tracers have low brain uptake, preventing their potential for neuroimaging application. Further explorations of this class of S1PR2 PET tracers in peripheral tissue diseases are underway. |
