R. Waterhouse, J. Gotsick, G. Kabalka
May 1, 1998
Citations
0
Influential Citations
4
Citations
Journal
Journal of Labelled Compounds and Radiopharmaceuticals
Abstract
[123I]-8-[4-[2-(5-Iodothienyl)]-4-oxobutyl]-3-methyl-1-phenyl-1,3,8-triazaspiro[4.5]-decan-4-one (1) has been synthesized as a potential ligand for dopamine D2 receptors. This new compound proved to be moderate in lipophilicity (log P=3.14) and exhibited high affinity (Ki=1.9 nM) for the dopamine D2 receptor as well as good selectivity for D2 versus serotonin 5HT2 receptors (Ki 5HT2/D2=16.7) in vitro. The corresponding radioligand, 123I-1, was synthesized from a thienyl tributylstannane precursor using oxidative iododestannylation methods. The radiochemical yield was 64–80% EOS (n=5) and the purified product was >99% radiochemically purity with a specific activity >3,500 mCi/μmol (>129,500 MBq/μmol). © 1998 John Wiley & Sons, Ltd.