A simple and fast method for the preparation of n.c.a. 2-[18F]F-A85380 for human use.
2-[18F]F-A85380 is the first subtype selective PET-radiotracer to visualize the distribution of alpha4beta2 nicotinic acetylcholine receptors in human brain in vivo. We investigated a fast and safe automated production of 2-[18F]F-A85380 by purification of the BOC-protected intermediate product with a combination of solid phase extraction cartridges. After deprotection, adjustment of the pH and sterile filtration n.c.a. 2-[18F]F-A85380 was applicable for the use in human studies with a high specific activity and an overall radiochemical yield of 55% in 35 minutes.
Schmaljohann
J
J
Department of Nuclear Medicine, University of Bonn, Germany. joern.schmaljohann@ukb.uni-bonn.de
Gündisch
D
D
Minnerop
M
M
Joe
A
A
Bucerius
J
J
Dittmar
C
C
Jessen
F
F
Guhlke
S
S
Wüllner
U
U
D001384:Azetidines / Q000138:chemical synthesis*; D001921:Brain / Q000000981:diagnostic imaging / Q000378:metabolism; D006801:Humans; D006863:Hydrogen-Ion Concentration; D049268:Positron-Emission Tomography; D011725:Pyridines / Q000138:chemical synthesis*; D019275:Radiopharmaceuticals / Q000138:chemical synthesis*; D011978:Receptors, Nicotinic / Q000378:metabolism
C119803:2-fluoro-3-(2-azetidinylmethoxy)pyridine; D001384:Azetidines; D011725:Pyridines; D019275:Radiopharmaceuticals; D011978:Receptors, Nicotinic; C403531:nicotinic receptor alpha4beta2