Comparison of in vivo D-2 dopamine receptor binding of IBZM and NMSP in rat brain.
In vivo biodistribution of S- and R-isomers of [125I]IBZM in rats showed a significant initial brain uptake (3.20 and 2.67% dose/organ at 2 min, respectively). The wash-out from the brain was slower for the S-isomer. The striatum to cerebellum ratio for [125I]S-IBZM decreased with an increasing dose of cold carrier or spiperone, suggesting that the brain uptake is stereospecific and saturable, and may be related to the binding of D-2 dopamine receptors. In a dual isotope digital autoradiography study [125I]IBZM and [3H]NMSP(N-methylspiperone) show comparable regional cerebral distribution in rats.
Kung
H F
HF
Department of Nuclear Medicine, SUNY, Buffalo.
Billings
J J
JJ
Guo
Y Z
YZ
Mach
R H
RH
D000818:Animals; D001549:Benzamides / Q000493:pharmacokinetics*; D001921:Brain / Q000000981:diagnostic imaging / Q000378:metabolism*; D007457:Iodine Radioisotopes; D008297:Male; D011759:Pyrrolidines / Q000493:pharmacokinetics*; D051381:Rats; D011954:Receptors, Dopamine / Q000378:metabolism*; D017448:Receptors, Dopamine D2; D013134:Spiperone / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D014055:Tomography, Emission-Computed; D014316:Tritium
D001549:Benzamides; D007457:Iodine Radioisotopes; D011759:Pyrrolidines; D011954:Receptors, Dopamine; D017448:Receptors, Dopamine D2; D014316:Tritium; D013134:Spiperone; C055743:3-iodo-2-hydroxy-6-methoxy-N-((1-ethyl-2-pyrrolidinyl)methyl)benzamide; C039167:3-N-methylspiperone