Fluorine-18 labeled galactosyl-neoglycoalbumin for imaging the hepatic asialoglycoprotein receptor

摘要: Abstract Asialoglycoprotein receptors (ASGP-R) are well known to exist on the mammalian liver, situate surface of hepatocyte membrane. Quantitative imaging asialoglycoprotein could estimate function liver. 99m Tc labeled galactosyl-neoglycoalbumin (NGA) and diethylenetriaminepentaacetic acid galactosyl human serum albumin (GSA) have been developed for SPECT clinical used in Japan. In this study, we NGA with 18 F get a novel PET tracer [ F]FNGA evaluated its hepatic-targeting efficacy pharmacokinetics. Methods : was by conjugation N -succinimidyl-4- F-fluorobenzoate ([ F]SFB) under slightly basic condition. The vivo metabolic stability determined. Ex biodistribution blocking experiment investigated normal mice. MicroPET images were acquired rat without block at 5 min 15 min after injection radiotracer (3.7 MBq/rat), respectively. Results Starting − Kryptofix 2.2.2./K 2 CO 3 solution, total reaction time is about 150 min. Typical decay-corrected radiochemical yield 8–10%. After rapid purified HiTrap desalting column, purity more than 99% determined radio-HPLC. metabolized produce F]FB-Lys urine 30 min. mice showed that liver accumulated 79.18 ± 7.17% 13.85 ± 3.10% injected dose per gram 5 30 min injection, addition, hepatic uptake blocked pre-injecting free as agent (18.55 ± 2.63%ID/g pi), indicating specific binding ASGP receptor. study obtained quality post-injection. Conclusion receptor synthesized high yield. promising biological properties afford potential applications assessment future. It may provide quantitative information better resolution which particularly help surgery.