An investigation on radiopharmaceutical potantial of I-131 labeled sertraline

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Date
2000-10
Journal Title
Journal ISSN
Volume Title
Publisher
Turkish Atomic Energy Authority
Abstract
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.
Description
I. Avrasya Nükleer Bilimler ve Uygulamaları Konferansı : 23-27 Ekim 2000. İzmir, Türkiye.
Keywords
Radiopharmaceutical, Radyofarmasötik, Sertraline, Sertralin, I-131
Citation
Yurt, F., Ünak, P., Biber, F. Z. (2000). An investigation on radiopharmaceutical potantial of I-131 labeled sertraline. I. Eurasia Conference on Nuclear Science and Its Application, Presentations, Vol 1, (s. 404-409). 23-27 October 2000. İzmir, Turkey.