氟十八標記滲透性醣蛋白分子探針作為新穎正子斷層掃描藥物的研究

Abstract

The purpose of this research is to develop a novel PET imaging agent for the study of P-glycoprotein (P-gp) function. A series of fluoroalkyl-aminoanthraquinone derivatives was designed and synthesized based on the skeleton of mitoxantrone (MX) and ametantrone (AT). After pharmacological studies, compound 10 was chosen as the target compound, and compounds 5 and 8 were designed and synthesized as precursors for 18F-radiolabeling. Initially, precursor 5 was easily decomposed under basic condition, but using tetrabutylammonium bicarbonate instead of commonly used base, such as potassium carbonate and potassium oxalate, heating at 100oC for 5 minutes, and then hydrolysis with 2 N hydrochloric acid at 100oC for 5 minutes to yield enough [18F]10 for animal study with microPET. In addition to the purity of precursor, radiochemical yield (RCY) increased from 0.02% to 3.3% when the equivalent of precursor increased from 4