(Turkish Atomic Energy Authority, 2000-10) Yurt, Fatma; Ünak, Perihan; Biber, F. Zümrüt; 10811; Bölüm Yok
Sertraline [(IS- cis)- 4-( 3, 4-dichlorophenyl)-l,2,3,4 -tetrahydro - N-methyl-l-naphalenamine
hydrochloride] is an antidepressant drug. It is presumed to be linked to its inhibition of central
nervous system (CNS) neuronal uptake of serotonin (5-HT) receptors. Serotonin 5-HT1A
receptors are prominently expressed in the CNS that binding sites are present various brain
regions.
The aim of this study is to label with 1-131 and investigate of its radiopharmaceutical potential.
Sertraline was labeled with 1-131 by using iodogen method. Quality Controls were fixed by
Radio-TLC and Electrophoresis Methods. Labeling yield was 85-90% and spesific activity was
approximately 1.75 Ci/mmol. The purification of radioiodinated Sertraline was performed by
Sep Pak C-18 plus and determined radiochemical purity over 99%. Biodistribution studies were
carried out by male Albino Wistar rats. 1-131 labeled Sertraline was administered by
intravenous injection into tail vein of the rats. The rats were sacrificed by ether narcotization at
certain time intervals and the organs were removed. The whole brain was excised quickly and
dissected into their regions. Their activities were counted by Cd(Te) detector equipped with
RAD 501 Single Channel Analyzer Instrument. The percentage injected radioactivity per gram
of tissue was calculated, and these data versus time curves were generated for organs and brain
regions.
Obtained results showed that 1-131 labeled Sertraline may be a promising radiopharmaceutical
for investigation of serotonin 5-HT receptor functions of brain.