446873-84-3Relevant articles and documents
Synthesis and biological evaluation of both enantiomers of [ 18F]flubatine, promising radiotracers with fast kinetics for the imaging of α4β2-nicotinic acetylcholine receptors
Smits, René,Fischer, Steffen,Hiller, Achim,Deuther-Conrad, Winnie,Wenzel, Barbara,Patt, Marianne,Cumming, Paul,Steinbach, J?rg,Sabri, Osama,Brust, Peter,Hoepping, Alexander
, p. 804 - 812 (2014)
Both enantiomers of the epibatidine analogue flubatine display high affinity towards the α4β2 nicotinic acetylcholine receptor (nAChR) in vitro, accompanied by negligible interactions with diverse off-target proteins. Extended single dose toxicity studies in rodent indicated a NOEL (No Observed Effect Level) of 6.2 μg/kg for (-)-flubatine and 1.55 μg/kg for (+)-flubatine. We developed syntheses for both flubatine enantiomers and their corresponding precursors for radiolabeling. The newly synthesized trimethylammonium precursors allowed for highly efficient 18F- radiolabelling in radiochemical yields >60% and specific activities >750 GBq/μmol, thus making the radioligands practical for clinical investigation.