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Synthesis and radiolabelling of 2β‐carbomethoxy‐3β‐(3′‐iodo‐4′‐isopropylphenyl) nortropane as a radioligand for the exploration of the serotonin transporter by SPET
Author(s) -
Helfenbein J.,
Emond P.,
Sandell J.,
Halldin C.,
Pereyre S.,
Frangin Y.,
Garreau L.,
Besnard J.C.,
Guilloteau D.,
Chalon S.
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(199904)42:4<337::aid-jlcr194>3.0.co;2-b
Subject(s) - chemistry , radiosynthesis , radioligand , ex vivo , tropane , radiochemistry , serotonin transporter , in vivo , serotonin , peracetic acid , stereochemistry , biochemistry , in vitro , receptor , microbiology and biotechnology , biology , hydrogen peroxide
In order to develop a potential tool for SPET examination of the serotonin transporter (5‐HTT) in the human brain, we report the synthesis and radiolabelling of 2β‐carbomethoxy‐3β‐(3′‐iodo‐4′‐isopropylphenyl) nortropane (LBT‐44). We also report ex vivo autoradiography performed in the rat brain. The radiosynthesis of [ 125 I]LBT‐44 was accomplished by iododestannylation of a trimethyltin precursor using [ 125 I]sodium iodide and peracetic acid or choramine‐T as oxidant. After purification by reverse phase HPLC, [ 125 I]LBT‐44 was obtained in a radiochemical yield higher than 75% and a radiochemical purity greater than 95%. Ex vivo autoradiographic studies revealed a marked accumulation of [ 125 I]LBT‐44 in brain areas rich in 5‐HTT whereas no accumulation was observed in the striatum, which is rich in dopamine transporters. These results are in favour of specific binding of [ 125 I]LBT‐44 to 5‐HTT that is required for SPET exploration in human. Copyright © 1999 John Wiley & Sons, Ltd.