Synthesis, radiolabeling and biodistribution of morphine glucuronide (mor-glu)

The aim of this study was to synthesize a glu- curonide conjugated morphine derivative which could be labeled with 131 I, as a radiopharmaceutical, and to inves- tigate its radiopharmaceutical potential using biodistribu- tion 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) spec- troscopy and liquid chromatography mass spectroscopy (LC-MS/MS). Normal and receptor blockage biodistribu- tion studies were performed in male Albino Wistar rats. The results of the tissue distribution studies showed that 131 I labeled morphine glucuronide ( 131 I-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.