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

  • H. Enginar
  • P. Unak
  • F. Z. Biber Müftüler
  • F. Y. Lambrecht
  • A. Yurt Kilcar
  • S. Yolcular
  • B. Seyitoğlu
  • E. I. Medine
  • I. Bulduk
Article

Abstract

In current study, ethyl-morphine (em) was synthesized from the morphine and glucuronidated via enzymatic mechanism. The conjugated glucuronide ethyl-morphine (em-glu) was radiolabeled with 131I using iodogen method. The quality control studies of radiolabeled compound (131I-em-glu) were done with Thin Layer Radio Chromatography to confirm the radiolabeling efficiency. Biodistribution studies of 131I labeled em-glu were run on healthy male Albino Wistar rats. The distribution figures demonstrated that 131I-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.

Keywords

Morphine Ethyl-morphine glucuronide (em-glu) 131I labeled ethyl-morphine-glucuronide (131I-em-glu) Biodistribution 

Notes

Acknowledgments

The authors thank for the financial supports from The Scientific and Technical Research Council of Turkey (TUBITAK, Project number 2004-104T187) and T.R Prime Ministry State Planning Organization (DPT, Project Number 2006 DPT 06).

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Copyright information

© Akadémiai Kiadó, Budapest, Hungary 2011

Authors and Affiliations

  • H. Enginar
    • 1
  • P. Unak
    • 2
  • F. Z. Biber Müftüler
    • 2
  • F. Y. Lambrecht
    • 2
  • A. Yurt Kilcar
    • 2
  • S. Yolcular
    • 2
  • B. Seyitoğlu
    • 2
  • E. I. Medine
    • 2
  • I. Bulduk
    • 3
  1. 1.Department of ChemistryAfyon Kocatepe UniversityAfyonkarahisarTurkey
  2. 2.Institute of Nuclear ScienceEge UniversityIzmirTurkey
  3. 3.Bolvadin Alkaloid FactoryAfyonkarahisarTurkey

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