Abstract: To investigate the radiosynthesis of 2-［¹⁸F］-A-85380 and its biodistribution in rat’s brain, 2-［¹⁸F］-A-85380 was synthesized with Me₃N⁺-Boc-A-85380•CF₃SO^-₃ as precursor. The radiolabeled compound was characterized by polymide TLC, in which the substratum of saline was used as developing agent. SD rats were sacrificed at 5, 60, 120 and 180 min after tail vein injection of 0.5 mL （1.48 MBq） freshly prepared 2-［¹⁸F］-A-85380. The heads were cut off and the brains were taken integrallty, then cut into slices and exposured with phosphor for 30 min, after that the phosphor was put into scan system and the digital images were obtained. The labeling yield of 2-［¹⁸F］-A-85380 is 93% and its radiochemical purity are exceeded 90% at 2, 4 and 6 h. Phosphor screen imaging show that the phosphor screen receives the highest radioactivity at 60 min after injection. The intensity of image is denser than that of 5, 120, 180 min. Accumulated radioactivity is greatest in thalamus, intermediate in the cortex, fewer in cerebellum and brainstem.