Synthesis and biodistribution of both (±)-5-[ 18F]-fluoroethoxy and (±)-5-[ 18F]-fluoropropoxy piperazine analogs of benzovesamicol as vesicular acetylcholine transporter ligands (VAChT)
Synthesis and biodistribution of both (±)-5-[ 18F]-fluoroethoxy and (±)-5-[ 18F]-fluoropropoxy piperazine analogs of benzovesamicol as vesicular acetylcholine transporter ligands (VAChT)
The radiosynthesis and preliminary biological evaluation in rats’ brain of two novel piperazine analogs
of benzovesamicol as ligands for the vesicular acetylcholine transporter (VAChT) have been carried out. The novel
benzovesamicol derivatives 5-(2-fluoroethoxy)-3-(4-phenylpiperazin-1-yl)-1,2,3,4-tetrahydronaphthalen-2-ol and
5-(3-fluoropropoxy)-3-(4-phenylpiperazin-1-yl)-1,2,3,4-tetrahydronaphthalen-2-ol [(±)-[18F]-6 and (±)-[18F]-7] were
successfully labelled with fluorine-18 from their tosylate precursors, with radiochemical purities greater than 98% and
with radiochemical yield in the range of 5–6%. To determine whether these compounds could have potential advantage
compared to [125I]-iodo benzovesamicol (IBVM), IBVM was also labelled and used as the reference compound
in all in vivo experiments. Both (±)-[18F]-6 and (±)-[18F]-7 showed lower specific binding in all brain areas explored
2 h post injection when compared to reference compound (-)-[125I] IBVM. Furthermore, defluorination indicated that
(±)-[18F]-6 and (±)-[18F]-7 are not suitable as radioligands to explore the VAChT in vivo by PET. Moreover, it is well
known that interaction at the VAChT binding site is enantioselective, and therefore, working with enantiomerically
pure compounds, could improve the compound activity.
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