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Synthesis of [ 11 C]LU 29‐066, a 5‐HT 2 receptor antagonist
Author(s) -
Amokhtari Mostafa,
Andersen Kim,
Ibazizène Meziane,
Gourand Fabienne,
Dauphin François,
Barré Louisa
Publication year - 1999
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/(sici)1099-1344(199905)42:5<437::aid-jlcr202>3.0.co;2-i
Subject(s) - chemistry , radioligand , phosgene , antagonist , radiochemistry , high performance liquid chromatography , receptor antagonist , receptor , nuclear chemistry , chromatography , organic chemistry , biochemistry
Lu 29‐066 (1‐(2{4‐[2,5‐dimethyl‐3‐(4‐fluorophenyl)‐1 H ‐indol‐1‐yl]piperidin‐1‐yl}ethyl)‐2‐imidazolidinone), a selective antagonist of serotoninergic 5‐HT 2 receptors, was labelled with carbon‐11. The synthesis of the non‐radioactive precursor and its reaction with [ 11 C]phosgene affording [ 11 C]Lu 29‐066 are described. Approximately 1.5 to 2.2 GBq (40–60 mCi) of the radioligand were obtained with a specific activity ranging from 11 to 18.5 GBq/μmol (300–500 mCi/μmol) and analytical HPLC showed a radiochemical purity over 99%. Copyright © 1999 John Wiley & Sons, Ltd.