Investigation of Radiopharmaceutical Potential of an Unsymmetrical Perylene diimide DMANPER Radiolabeled with 131I ​

Year 2011, Volume: 39 Issue: 3, 289 - 296, 01.08.2011

Uğur Avcıbaşı Haluk Dinçalp Nesibe Avcıbaşı

Abstract

The aim of this study was to investigate the radiopharmaceutical potential of N- 2,6-diisopropylphenyl -N’- [4- N,N-dimethylaminophenyl ]-perylene-3,4,9,10-tetra carboxylic diimide DMANPER radiolabeled with 131I using scintigraphic imaging and biodistributional techniques. Radiolabeled DMANPER 131I-DMANPER was intravenously injected into an adult male Albino rabbit via its ear vein anesthetizing with a mixture of Alfazyne and Alfamine Serva to determine dynamic and static situations of radiolabeled compound in the rabbit metabolism. Three rats were used for biodistribution studies corresponding to different time intervals. The animals were sacrificed by heart puncture under ether anesthesia within post-injection time intervals ranging from 30 to 300 min. Results were expressed as % of the injected dose per gram tissue % ID/g . TLRC analysis showed that DMANPER was successfully radioiodinated with 131I with a yield of practically 100 %. According to scintigraphy studies, 131I-DMANPER was completely accumulated in the stomach in 30 min. In the biodistributional data for 131I-DMANPER in rats, a significant amount of activity is seen in the stomach between 30-60 min. It can be concluded that 131I-DMANPER may be an alternative imaging agent like N- 2,6- diisopropylphenyl -N`- 4-pyridyl -perylene-3,4,9,10-tetracarboxylic diimide PYPER to be a potential agent for diagnosis and perhaps therapy of stomach cancer.

Keywords

Perylene dimide, iodine-131, biodistribution, stomach imaging

Radyoaktif 131I ile İşaretli Asimetrik Bir Perilen diimid’in DMANPER Radyofarmösitik Potansiyelinin İncelenmesi

Abstract

B u çalışmanın amacı sintigrafik görüntüleme ve biyodağılım teknikleri kullanılarak, 131I ile işaretlenmiş N- 2,6diizopropilfenil -N’-[4- N,N-dimetillaminofenil ]-perilen-3,4,9,10-tetra karboksilik diimid’in DMANPER radyofarmösitik potansiyelini incelemektir. Radyo işaretli DMANPER 131I-DMANPER , tavşan metabolizmasında radyoaktif olarak işaretlenmiş bileşiğin dinamik ve statik durumunu belirlemek için, Alfazin ve Alfamin karışımı ile anestezi verilmiş yetişkin bir erkek Albino tavşana kulak veni yoluyla enjekte edilmiştir. Biyodağılım çalışmalarında farklı zaman aralıkları için üç adet sıçan kullanılmıştır. Enjeksiyondan sonra 30 ile 300 dakika arasında değişen bir zaman aralığı içerisinde, hayvanların eter anestezisi ile kalplerinin durdurulmasıyla hayatlarına son verdirilmiştir. Sonuçlar, gram doku başına enjekte edilen dozun %’si olarak ifade edilmiştir % ID/g . İnce tabaka radyo-kromatografi analizleri TLRC , DMANPER’in 131I ile başarılı bir biçimde, yaklaşık % 100 verimle işaretlendiğini göstermiştir. 131I-DMANPER 30 dakikalık süre içerisinde tamamen midede birikmiştir. 131I-DMANPER için farelerde yapılan biyodağılım sonuçlarında, 30 ile 60 dakika arasında en fazla aktivite midede görülmüştür. 131I-DMANPER’in mide kanserinin teşhisi ve tedavisi için N- 2,6-diizopropilfenilN`- 4-piridil -perilen-3,4,9,10-tetrakarboksilik diimid PYPER gibi bir alternatif görüntüleme ajanı olabileceği sonucuna varılabilir

Keywords

Perilen diimid, iyot-131, biyodağılım, mide görüntülemesi

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