Preliminary tests of the radiopharmaceutical potential of N-(2,6-diisopropylphenyl)-N'-(4-pyridyl)-perylene-3,4,9,10-tetracarboxylic diimide radiolabeled with I-131


AVCIBAŞI U., DİNÇALP H., Uenak T., Yildirim Y. , Avcibasi N. , DUMAN Y., et al.

JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY, cilt.273, ss.669-675, 2007 (SCI İndekslerine Giren Dergi)

  • Cilt numarası: 273 Konu: 3
  • Basım Tarihi: 2007
  • Doi Numarası: 10.1007/s10967-007-0929-z
  • Dergi Adı: JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY
  • Sayfa Sayısı: ss.669-675

Özet

Perylene diimide derivatives are one of the G-quadruplex DNA interactive agents which are thought to be useful in application of cancer treatment Starting from this consideration, N-(2,6-diisopropylphenyl)-N'-(4-pyridyl)-perylene-3,4,9,10-tetracarboxylic diimide (PYPER) was synthesized, radioiodinated with I-131, and its radiopharmaceutical potentials were tested on a male Albino rabbit and male Albino Wistar rats. This compound was successfully radioiodinated with I-131 with a radioiodination yield of about 100%. Scintigraphic imaging with the radiiodinated compound (I-131-PYPER) was performed on a rabbit. Static images were obtained from posterior projection using a Diacan gamma camera at several time intervals. The scintigrams clearly showed that the radioiodinated compound was not quickly cleared from the metabolism, accumulating in the stomach over about 30 minutes. The clearance time of this compound was considerably longer than 5 hours. The results obtained in this study agreed with that of the biodistribution studies and indicated that I-131-PYPER might be used as a scintigraphic agent for examining stomach diseases.