کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1358791 | 981363 | 2014 | 9 صفحه PDF | دانلود رایگان |
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.
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Journal: Bioorganic & Medicinal Chemistry - Volume 22, Issue 2, 15 January 2014, Pages 804–812