Synthesis, radiolabeling and biodistribution of a new opioid glucuronide derivative: ethyl-morphine glucuronide (em-glu)


Enginar H., Unak P. , Muftuler F. Z. B. , Lambrecht F. , Kilcar A. Y. , Yolcular S., et al.

JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY, cilt.292, ss.667-673, 2012 (SCI İndekslerine Giren Dergi) identifier identifier

  • Cilt numarası: 292 Konu: 2
  • Basım Tarihi: 2012
  • Doi Numarası: 10.1007/s10967-011-1472-5
  • Dergi Adı: JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY
  • Sayfa Sayısı: ss.667-673

Özet

In current study, ethyl-morphine (em) was synthesized from the morphine and glucuronidated via enzymatic mechanism. The conjugated glucuronide ethylmorphine (em-glu) was radiolabeled with I-131 using iodogen method. The quality control studies of radiolabeled compound (I-131-em-glu) were done with Thin Layer Radio Chromatography to confirm the radiolabeling efficiency. Biodistribution studies of I-131 labeled em-glu were run on healthy male Albino Wistar rats. The distribution figures demonstrated that I-131-em-glu was eliminated through the small intestine, large intestine and accumulated in urinary bladder both receptor blocked and unblocked biodistribution studies. A greater uptake of the radiolabeled substance was observed in the m. pons, hypothalamus and mid brain than in the other branches of the rats' brains.