Synthesis,radiolabeling and biodistribution of morphine glucuronide (mor-glu) |
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| Authors: | H Enginar P Unak F Z Biber Müftüler F Y Lambrecht E I Medine S Yolcular A Yurt Kilcar B Seyito?lu I Bulduk |
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| Institution: | (1) Department of Chemistry, Afyon Kocatepe University, Afyonkarahisar, Turkey;(2) Institute of Nuclear Science, Ege University, Izmir, Turkey;(3) Bolvadin Alkaloid Factory, Afyonkarahisar, Turkey; |
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| Abstract: | The aim of this study was to synthesize a glucuronide conjugated morphine derivative which could be labeled with 131I, as a radiopharmaceutical, and to investigate its radiopharmaceutical potential using biodistribution studies in male Albino
Wistar rats. Morphine was extracted from dry capsules of the opium poppy (Papaver somniferum L.). It was conjugated with UDP-glucuronic acid by using UDP-glucuronyl transferase (UDPGT) enzyme rich microsomes, purified
by high performance liquid chromatography (HPLC) and characterized by nuclear magnetic resonance (NMR), infrared (IR) spectroscopy
and liquid chromatography mass spectroscopy (LC-MS/MS). Normal and receptor blockage biodistribution studies were performed
in male Albino Wistar rats. The results of the tissue distribution studies showed that 131I labeled morphine glucuronide (131I-mor-glu) uptake in the small intestine, large intestine and urinary bladder was higher than in the other tissues of the
rats in the blocked receptor and unblocked receptor. A greater uptake of the radio labeled substance was observed in the hypothalamus
and mid brain than in the other branches of the rats’ brains. |
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