A simple and fast method for the preparation of n.c.a. 2-[18F]F-A85380 for human use

J Schmaljohann; D Gündisch; M Minnerop; A Joe; J Bucerius; C Dittmar; F Jessen; S Guhlke; U Wüllner

doi:10.1016/j.apradiso.2005.05.040

A simple and fast method for the preparation of n.c.a. 2-[18F]F-A85380 for human use

Appl Radiat Isot. 2005 Oct;63(4):433-5. doi: 10.1016/j.apradiso.2005.05.040.

Authors

J Schmaljohann¹, D Gündisch, M Minnerop, A Joe, J Bucerius, C Dittmar, F Jessen, S Guhlke, U Wüllner

Affiliation

¹ Department of Nuclear Medicine, University of Bonn, Germany. joern.schmaljohann@ukb.uni-bonn.de

PMID: 16024252
DOI: 10.1016/j.apradiso.2005.05.040

Abstract

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.

MeSH terms

Azetidines / chemical synthesis*
Brain / diagnostic imaging
Brain / metabolism
Humans
Hydrogen-Ion Concentration
Positron-Emission Tomography
Pyridines / chemical synthesis*
Radiopharmaceuticals / chemical synthesis*
Receptors, Nicotinic / metabolism

Substances

2-fluoro-3-(2-azetidinylmethoxy)pyridine
Azetidines
Pyridines
Radiopharmaceuticals
Receptors, Nicotinic
nicotinic receptor alpha4beta2