Synthesis and radiolabelling of 2β-carbomethoxy-3β-(3′-iodo-4′-isopropylphenyl) nortropane as a radioligand for the exploration of the serotonin transporter by SPET.

被引：0
|
作者：
Helfenbein, J
Emond, P
Sandell, J
Halldin, C
Pereyre, S
Frangin, Y
Garreau, L
Besnard, JC
Guilloteau, D
Chalon, S
机构：
[1] Fac Pharmaceut Sci, Lab Biophys Med & Pharmaceut, INSERM, U316, F-37200 Tours, France
[2] Karolinska Hosp, Karolinska Inst, Dept Clin Neurosci, Psychiat Sect, S-17176 Stockholm, Sweden
来源：
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS | 1999年 / 42卷 / 04期
关键词：
cocaine derivatives; radioiodination; serotonin transporter;
D O I：
10.1002/(SICI)1099-1344(199904)42:4<337::AID-JLCR194>3.0.CO;2-B
中图分类号：
Q5 [生物化学];
学科分类号：
071010 ; 081704 ;
摘要：
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 2 beta-carbomethoxy-3 beta-(3'-iodo-4'-isopropylphenyl) nortropane (LBT-44). We also report ex vivo autoradiography performed in the rat brain. The radiosynthesis of [I-125]LBT-44 was accomplished by iododestannylation of a trimethyltin precursor using [I-125]sodium iodide and peracetic acid or choramine-T as oxidant. After purification by reverse phase HPLC, [I-125]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 [[I-125]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 [I-125]LBT-44 to 5-HTT that is required for SPET exploration in human.
引用
收藏
页码：337 / 347
页数：11
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