F-18 labelled N,N-bis-haloethylamino-phenylsulfoxides - A new class of compounds for the imaging of hypoxic tissue

Abstract

Two N,N-bis-chloroethylamino-phenylsulfoxides have been synthesized and radiolabelled with F-18 via halogen exchange. The radiolabelling of both compounds proceeds smoothly with K[18F]F-kryptofix 2.2.2 complex at 100°C in DMSO. Decay-corrected radiochemical yields were 25-35% for [ 18F]12 (SO201) and 35-45% for [18F]11 (SO101), with an average specific activity of 1.8 Ci/μmol. Both compounds remained 80% intact in plasma over a period of 2 h. In vivo binding in a stroke model indicates that both markers are selectively retained in hypoxic tissue. Copyright © 2006 John Wiley & Sons, Ltd.