The goal of this study was to determine the radiopharmaceutical potential of radioiodinated thebaine. Thebaine was extracted from dry capsules of opium poppy (Papaver somniferum L.), purified using high-performance liquid chromatography, and characterized with nuclear magnetic resonance and infrared spectroscopy. The purified thebaine was labeled with 131I using the iodogen method. Normal and receptor-blockage biodistribution studies were performed in male Albino Wistar rats. The results of the tissue distribution studies showed that the uptake of 131I-thebaine in the stomach, large intestine, spinal cord, and prostate was higher than in the other tissues. A greater uptake of radiolabeled thebaine in the rat brain was observed in the midbrain and hypothalamus. We concluded that (1) the labeling yield of 131I-thebaine was high, (2) a large amount of 131I-thebaine remained in the midbrain and hypothalamus, and (3) 131I-thebaine had enough stability for diagnostic scanning.

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.

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.

Apigenin (4′,5,7-trihydroxyflavone), one of the most common flavonoids, has been shown to possess a variety of biological activities including tumor growth inhibition and chemopreventation. In the present study, apigenin was labeled with 131 I using iodogen method and investigated of its bioactivity. Radiolabeling yield is 98±0.2%, as determined by radio thin layer chromatography (RTLC), electrophoresis and radio high performance liquid chromatography (RHPLC). Besides, structure analysis of synthesized cold iodoapigenin complex were assessed with LCMS/MS and 1 H-NMR. Results of in vitro study indicated a high stability (3 hours) in human serum. Biodistrubition studies are performed in male and female albino Wistar rats. Biodistribution data related to the male rats showed significant uptake in the small intestine. The female rats biodistribution results indicated that the uptake of 131 I-apigenin was high in the intestine and uterus.

This study was conducted to determine the possible radiopharmaceutical potential of morphin labeled with (131)I. Morphine was extracted from dry capsules of the opium poppy (Papaver somniferum L.), purified by high-performance liquid chromatography, and characterized with nuclear magnetic resonance and infrared spectroscopy. The purified compound was labeled with (131)I. Male Albino Wistar rats (18) were used for receptor blockage and unblockage biodistribution studies. Tissue distribution studies showed that radiolabeled morphine had higher uptake in lung, liver, small intestines, large intestines, and stomach than the other tissues. The highest uptake of radiolabeled compounds in rats' brain was found to be in the midbrain and hypothalamus. After receptor blockage with morphine, uptake of (131)I-morphine decreased in the lungs, liver, kidney, testis, prostate, spinal cord, cerebellum, hippocampus, striatum, and temporal cortex with respect to receptor unblockage studies of rats. This study concludes that the labeling yield of (131)I-morphine was high, high amount of (131)I-morphine was found in the hypothalamus, and (131)I-morphine has enough stability for diagnostic scanning.

The aim of this study was to evaluate 99mTc labeled human β-defensin-1 (HBD-1) for discrimination between bacterial infection and sterile inflammation. For this purpose, HBD-1 was radiolabeled with 99mTc and its in vivo distribution was evaluated in inflamed rats with Staphylococcus aureus (S. aureus) and sterile inflamed rats with turpentine oil. After injection into inflamed and sterile inflamed rats, 99mTc-HBD-1 was rapidly removed from the circulation via the kidneys. Binding of 99mTc-HBD-1 to inflamed muscle (T/NT = 20 at 120 min) was two times higher than binding to sterile inflamed muscle (T/NT = 10 at 120 min) of rats. It was demonstrated that 99mTc-HBD-1 can be used to detect S. aureus inflammation in rats. However, the radiolabeled antimicrobial peptide showed only poor uptake in sterile inflammation with turpentine oil in rats. As a result, 99mTc-HBD-1 can be useful for detection of bacterial inflammation.

Localizing and distinguishing the “infection” in body sites are very important and life saving processes. Scintigraphic detections may help to determine the sites of inflammation and infection. At this point, nuclear medical imaging may proceed one step further and be helpful to localize and distinguish the inflammation. The radiolabeled antibiotic 99m Tc-Cefuroxime axetil was assessed as an infection imaging agent in a rat model. In this study, 99m Tc-Cefuroxime axetil was examined in localizing the normal, sterile inflamed, and septic inflamed rat muscle tissues, and also in distinguishing each of them. The biodistribution data show that 99m Tc labeled Cefuroxime axetil was retained in infectious areas. The retention was better in septic inflamed ( S. aureus ) area than sterile inflamed area. The clearance of the labeled antibiotic from other tissues is rapid on the contrary to its clearance from the septic area. Target/non-target ratio shows a good value of 2.5 at 4-hour post injection when the activity of the other organs is cleared by urinary excretion.