Iodoethylspiperone, a new potential agent for exploration of central dopamine D2 receptors: synthesis and preliminary in vivo study.
We synthesized a new spiperone derivative: iodoethylspiperone (IES) to perform dopamine D2 receptor exploration by SPECT. IES was prepared from a precursor: tosylethylspiperone, and characterized by i.r. and 1H-NMR analyses. [125I]IES was obtained with 80% yield. In vivo biodistribution in rats showed a high and specific uptake in the striatum. The uptake ratio between the striatum and the cerebellum reached a maximum value 4 h after injection (10.05 +/- 2.81). IES labeled with 123I should be a promising new agent to investigate D2 receptors in the living human brain.
Chalon
S
S
INSERM U316, Laboratoire de Biophysique Médicale, Tours, France.
Frangin
Y
Y
Guilloteau
D
D
Caillet
M
M
Guimbal
C
C
Schmitt
M H
MH
Desplanches
G
G
Baulieu
J L
JL
Besnard
J C
JC
D000818:Animals; D001921:Brain / Q000000981:diagnostic imaging / Q000378:metabolism*; D002531:Cerebellum / Q000000981:diagnostic imaging / Q000378:metabolism; D003342:Corpus Striatum / Q000000981:diagnostic imaging / Q000378:metabolism; D007457:Iodine Radioisotopes; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D011954:Receptors, Dopamine; D017448:Receptors, Dopamine D2; D013134:Spiperone / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000493:pharmacokinetics; D014055:Tomography, Emission-Computed
D007457:Iodine Radioisotopes; D011954:Receptors, Dopamine; D017448:Receptors, Dopamine D2; C065265:iodoethylspiperone; D013134:Spiperone