An oestrogen-derivative labeled with Tc-99m and its radiopharmaceutical potential


ENGINAR H., UNAK P. , Yurt F. , BIBER F.

JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY, cilt.251, ss.473-479, 2002 (SCI İndekslerine Giren Dergi)

  • Cilt numarası: 251 Konu: 3
  • Basım Tarihi: 2002
  • Doi Numarası: 10.1023/a:1014898628890
  • Dergi Adı: JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY
  • Sayfa Sayısı: ss.473-479

Özet

An oestrogen derivative 3,17-alpha-oestradiolyl propyl 1.4,8,11-tetraazacyclotetradecanyl-1-(4-methylbenzoic acid)ester (ESTCPTA) that is 3,17-alpha-oestradiolyl propinol coupled to 1-(4-methylbenzoic acid) 1,4,8,1 1-tetraazacyclotetradecane (CPTA) was synthesized in five steps. The product was purified by recrystallization in ethyl alcohol, and analysed by NMR and IR spectroscopy. ESTCPTA was labeled with Tc-99m and radio thin layer chromatography (RTLC) and radio-paper electrophoresis were used to determine the radiochemical yields. Specific activity was approximately 23.7 GBq/mmol and the labeling yield was over 95%. The biodistribution studies were performed on female Albino Wistar rats. The rats were sacricified by ether narcotization at certain time intervals and the activity of the organs was counted by a gamma counter. The activity per gram tissue was calculated and time activity curves were generated.