Automated synthesis of radiopharmaceuticals for PET: an apparatus for [1-11C]labelled aldoses

This paper describes an instrumentation system for positron emission tomography (PET). A variety of [1-11C]labelled aldoses, such as [1-11C]-D-glucose, and galactose by a modification of the Kiliani-Fischer method have been produced. The instrumentation is fully automatic and consists of a synthesis system and control system. The synthesis system has the following functions: supplying reagents; performing reactions; purifying 11C labelled aldose; and preparing an injectable solution of 11C labelled aldose. These operations are performed by the control system in a remote control room. In a preliminary, hot experiment an injectable solution of [1-11C]-D-glucose was obtained. In addition, the operator is exposed to minimal radiation. The radioactivity of [1-11C]-Dglucose was 47 MBq, and the preparation time was 49 min

Measurement of brain concentration of FK960 for development of a novel antidementia drug: A PET study in conscious rhesus monkeys

金沢大学大学院医学系研究科This study used PET to measure the time course of the brain concentration of 18F-labeled N-(4-acetyl-1-piperazinyl)-p-fluorobenzamide monohydrate (FK960), a novel antidementia drug, after oral administration to conscious rhesus monkeys. Methods: Three young-adult male rhesus monkeys were tested. FK960 (0.1 mg/kg) containing about 370 MBq of 18F-FK960 was administered orally to each monkey. Dynamic PET images were acquired for 4 h from 5 min after the administration. Arterial blood samples were withdrawn during PET scanning and were analyzed by an automatic well γ-counter and thin-layer chromatography to determine the time course of authentic 18F-FK960 activity concentration in plasma. FK960 concentrations in brain and plasma were calculated in units of mol/L using the specific activity of FK960 preparations. Results: 18F-FK960 penetrated the blood-brain barrier and underwent perfusion-dependent distribution in the entire brain. Maximal concentrations in the brain and plasma were 1.11 ± 0.30 x 10-7 mol/L (at 3.0 ± 0.6 h after administration) and 4.04 ± 1.29 x 10-7 mol/L (at 2.0 ± 1.1 h after administration), respectively. Conclusion: We succeeded in measuring the FK960 concentration in the brains of conscious monkeys and in plasma after oral administration at a dose of 0.1 mg/kg. The results suggested that this method can measure the FK960 concentration in the human brain, and a potential use of the PET technique in drug development was demonstrated