Synthesis and [C-11]-radiolabelling of dechloro-epibatidine and 2PABH, twopotential radioligands for studying the central nAChRs in vivo.

Citation
Je. Spang et al., Synthesis and [C-11]-radiolabelling of dechloro-epibatidine and 2PABH, twopotential radioligands for studying the central nAChRs in vivo., J LABEL C R, 42(8), 1999, pp. 761-771
Citations number
21
Categorie Soggetti
Chemistry & Analysis","Inorganic & Nuclear Chemistry
Journal title
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS
ISSN journal
03624803 → ACNP
Volume
42
Issue
8
Year of publication
1999
Pages
761 - 771
Database
ISI
SICI code
0362-4803(199908)42:8<761:SA[ODA>2.0.ZU;2-8
Abstract
The two epibatidine (EPB) analogues dechloro-epibatidine (DC1-EPB) and 2PAB H were synthesised via a two step reaction starting from N-methoxycarbonyl- 7-azabicyclo[2.2.1]heptene. The radiochemical syntheses of [C-11]N-methylat ed derivatives was performed using the classical methylating agent [C-11]CH 3I in acetonitrile. The radiochemical yield ranged from 5 to 10 % (decay co rrected from [C-11]CH3I) and was fully sufficient for small animal experime nts. High specific activities in the range of 140 to 360 GBq/mu mol at EOS tend of synthesis) were obtained. The radiosynthesis, semipreparative HPLC, formulation and quality control were completed in an average time of 35 mi n.