M. Schou, V. Pike, J. Sóvágó
Dec 31, 2006
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Journal
NeuroImage
Abstract
Introduction: (R)-1-(10,11-Dihydro-dibenzo[b,f]azepin-5-yl)-3-methylamino-propan-2-ol ((R)-OHDMI) and (S,S)-1-cyclopentyl-2-(5-fluoro2-methoxy-phenyl)-1-morpholin-2-yl-ethanol ((S,S)-CFMME) were synthesized and found to be potent inhibitors of norepinephrine reuptake (inhibitory constants (K is) were 8.29 and 10.8 nM for (R)-OHDMI and (S,S)-CFMME, respectively, as compared with (S,S)-2-(a-(2methoxyphenoxy)benzyl)morpholine (S,S)-MeNER) which has a Ki of 7.93 nM). Here, we have explored the labeling of these ligands with carbon-11 for evaluation as candidate radioligands for imaging central norepinephrine transporters (NET).