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Imidazolium salts and derivatives have antitumor efficacy and toxic effects in different micro-organisms. In this study, an imidazolium bromide salt (NMI) was synthesized, and its antitumor potential was investigated by in vitro studies. Radiolabeling of synthesized NMI was carried out by iodogen method using 131 I radionuclide. The yield of radiolabeling was determined as 98.5 ± 0.1%. After that, cytotoxicity and intracellular uptake studies were evaluated in various cell lines. The cytotoxicity of NMI was determined as 35, 20, 10, and 1 μm for HEK-293, PC-3, CaCo-2, and MCF-7 cells, respectively. In addition, the intracellular uptake of 131 I-NMI was investigated in the cell lines, and the uptake was significantly found as 4 hr for MCF-7 and 6 hr for PC-3. In future studies, antitumor efficacy of 131 I-NMI on tumor-bearing animal model might be studied in light of these results.

Topoisomerase I inhibitor topotecan (TPT) is the only single-agent therapy certified for the remedy of repetitive small cell lung cancer (SCLC). In this study, TPT was labeled with I-131 via iodogen method and its quality control was determined using thin layer radiochromatography and paper electrophoresis methods. Intracellular uptake study was carried out with human lung adenocarcinoma cell line (A-549) and human lung fibroblast cell line (WI-38). The interaction of I-131-TPT with healthy DNA and cancer DNA was also investigated using single-use sensor technology combined with electrochemical impedance spectroscopy (EIS). The change at the charge transfer resistance (R-ct) obtained before/after interaction was evaluated. Similar to the results of intracellular uptake study, it was found that I-131-TPT could more interact with the cancer DNA than healthy DNA according to the impedimetric results. I-131-TPT is promising in terms of a new nuclear imaging agent for lung cancer. (C) 2016 Elsevier B.V. All rights reserved.

Photodynamic therapy (PDT) is a medical treatment for the removal of target tissues involving the delivery of a photosensitizer agent followed by irradiation with visible light. In the present study, symmetric Zn(II) Pc 1 and asymmetrically substituted Zn(II) Pc 2 were synthesized and examined multifunctional agents for tumor nuclear imaging and PDT potential. The Zn(II) Pc 1 and Zn(II) Pc 2 were radiolabeled with 131 I with high efficiency (93.4 ± 1.6% and 91.4 ± 1.6%, respectively). The results of the biodistribution study showed that radiolabeled Zn(II) Pc 1 had high uptake on lung, large intestine, ovary and pancreas. However, the uptake of radiolabeled Zn(II) Pc 2 was statically significant in pancreas and intestine. In PDT studies, EMT6/P (mouse mammary cell) and HeLa (cervical adenocarcinoma cell) with Zn(II) Pc 1 and Zn(II) Pc 2 were exposed to red light at the doses of 10–30 J/cm 2 . Although PDT activity of Zn(II) Pc 2 in HeLa cell line was determined, Zn(II) Pc 1 showed no phototoxic effect in both cell lines. In conclusion, radiolabeled Zn(II) Pc 1 might be a promising imaging agent for the lung, the ovary pancreas, and the colon tumors. However, radiolabeled Zn(II) Pc 2 might be a promising nuclear imaging agent for the colon and the pancreas tumors and promising PDT agent for cervical tumors.

A near IR absorbing phthalocyanine bearing four binaphtyl group has been synthesized in order to investigate its cytotoxicity and intracellular uptake of sensitizer on MCF-7 (human breast cancer), MDAH (ovarian cancer), HeLa (human epitheloid cervix carcinoma), EMT-6 (mouse breast cancer) and WI-38 (human fibroblast lung) cell lines. ZnPc showed four time higher intracellular uptake in carcinoma cells (MCF-7) than normal (WI-38) cell lines. With the aim of studying in detail the biodistribution feature and tumor nuclear imaging capacity, ZnPc was also labeled with I-131. The efficiency of radiolabeled compound was 95±4.6%. In addition, ZnPc reveals to be very efficient singlet oxygen generators (ΦΔ=0.612 in DMSO) and promising PS for PDT application. In vitro fluorescence imaging study with MCF-7 cells showed that ZnPc localized in cytoplasm of the cells. This results showed that synthesized ZnPc is promising candidate for dual fluorescence/nuclear imaging breast cancer and shows potential PS for PDT application.

Novel octylthio-containing asymmetrically substituted Zn(II) phthalocyanine (Zn(II)Pc1) and a symmetric derivative (Zn(II)Pc2) have been prepared to investigate the biological potential and ability to photosensitize singlet oxygen for photodynamic therapy applications. In this study, the singlet oxygen generation potential and in vitro photodynamic activities of these compounds have been tested. Both ZnPcs reveal to be very efficient singlet oxygen generators and promising PSs for PDT applications. In vitro PDT activities of the compounds were evaluated in EMT-6 murine mammary carcinoma and HeLa human cervix carcinoma cell lines. Moreover, Zn(II)Pc1 displayed the phototoxic effects in the mammary cancer cell line (6.25 μm concentration at 30 J/cm(2) light dose and 12.5 μm concentration at 20 J/cm(2) light dose), while Zn(II)Pc2 did not show any phototoxic effects both in two cell lines. Zn(II)Pcs were radiolabeled with (131) I in high yields. Biodistribution studies revealed that the radiolabeled Zn(II)Pc1 showed significant uptake in l. intestine, pancreas, brain, and ovary, while Zn(II)Pc2 has significant uptake in ovary and pancreas in normal rats. Hence, these Pcs derivatives could be promising candidate for tumor nuclear imaging.

In this study, the biological potential of a nickel chlorophyll derivative (Ni-PH-A) as a multimodal agent for tumor imaging and photodynamic therapy (PDT) was investigated. Optimum conditions of labeling with I-131 were investigated and determined as pH 10 and 1 mg amount of iodogen. Biodistribution results of I-131 labeled Ni-PH-A in female rats indicated that radiolabeled Ni-PH-A maximum uptake in the liver, spleen and ovary was observed at 30 min. Intercellular uptake and PDT efficacy of Ni-PH-A were better in MDAH-2774 (human ovarian endometrioid adenocarcinoma) than in MCF-7 (human breast adenocarcinoma) cells. Ni-PH-A might be a promising multimodal agent for lung, ovary and liver tumor imaging and PDT.

Gümüşün antimikrobiyal etkisini ve titanyum nitrürün mekanik ve kimyasal özelliklerini birleştirmek için, ortopedik implant malzemesi olarak kullanılan Ti6Al4V alaşımının yüzeyine N2 plazmasında plazma daldırma iyon implantasyonu ve biriktirme (PIII&D) yöntemi ile gümüş biriktirilmiştir. Kaplamalar, PIII&D prosesinin farklı negatif darbeli yüksek gerilim ve magnetron sıçratma gerilimi değerleri kullanılarak elde edilmiştir. Kaplamaların yüzey morfolojileri atomik kuvvet mikroskobu (AFM) ve kesit morfolojileri ise alan emisyonlu taramalı elektron mikroskobu (FE-SEM) kullanılarak tespit edilmiştir. Kaplamaların fazları ve kimyasal kompozisyonları sırasıyla X-ışını difraksiyonu (XRD) ve X-ışını fotoelektron spektroskopisi (XPS) kullanılarak tespit edilmiştir. Buna ek olarak, numunelerin yüzeyinden içeri Ag iyonlarının nüfuziyetini belirlemek için XPS derinlik profili (depth profile) analizi yapılmıştır. In-vitro biyouyumluluk deneylerinde numunelerin yüzeylerine 99mTc radyoizotopu ile işaretlenmiş E.coli (Escherichia coli) mikroorganizmasının adezyonu araştırılmıştır. Çalışmada, 8 kV'luk negatif darbeli gerilimin kullanıldığı deneylerle elde edilen kaplamalarda gümüşün dominant olduğu; bunun yanında, negatif darbeli yüksek gerilimin artmasıyla yüzeyde gümüş miktarının azaldığı gözlemlenmiştir.

Gümüşün antimikrobiyal etkisini ve titanyum nitrürün mekanik ve kimyasal özelliklerini birleştirmek için, ortopedik implant malzemesi olarak kullanılan Ti6Al4V alaşımının yüzeyine N2 plazmasında plazma daldırma iyon implantasyonu ve biriktirme (PIII&D) yöntemi ile gümüş biriktirilmiştir. Kaplamalar, PIII&D prosesinin farklı negatif darbeli yüksek gerilim ve magnetron sıçratma gerilimi değerleri kullanılarak elde edilmiştir. Kaplamaların yüzey morfolojileri atomik kuvvet mikroskobu (AFM) ve kesit morfolojileri ise alan emisyonlu taramalı elektron mikroskobu (FE-SEM) kullanılarak tespit edilmiştir. Kaplamaların fazları ve kimyasal kompozisyonları sırasıyla X-ışını difraksiyonu (XRD) ve X-ışını fotoelektron spektroskopisi (XPS) kullanılarak tespit edilmiştir. Buna ek olarak, numunelerin yüzeyinden içeri Ag+ iyonlarının nüfuziyetini belirlemek için XPS derinlik profili (depth profile) analizi yapılmıştır. In vitro anti-bakteriyel etkinlik deneylerinde numunelerin yüzeylerine 99mTc radyoizotopu ile işaretlenmiş E. coli (Escherichia coli) mikroorganizmasının adezyonu araştırılmıştır. Çalışmada, 8 kV'luk negatif darbeli gerilimin kullanıldığı deneylerle elde edilen kaplamalarda gümüşün dominant olduğu; bunun yanında, negatif darbeli yüksek gerilimin artmasıyla yüzeyde gümüş miktarının azaldığı gözlemlenmiştir., In order to combine the antimicrobial effect of silver with mechanical and chemical properties of titaniumnitrate, Ag was deposited on the surface of Ti6Al4V (orthopedic implant material) in N2 plasma by using plasma immersion ion implantation and deposition (PIII&D) method. The coatings were formed by usingvaried negative pulsed high voltage and magnetron sputtering voltage values of PIII&D process. Surfacemorphologies of coatings were determined with atomic force microscopy (AFM), while cross-section morphologies were determined with field emission scanning electron microscopy (FE-SEM). The phases and chemical compositions of coatings were investigated by using X-ray diffraction (XRD) and X-ray photoelectron spectroscopy (XPS), respectively. XPS depth profile analysis were done to reveal thepenetration of Ag+ ions into the surface of specimen. In in vitro anti-bacterial effectiveness experiments,the adhesion of E. coli (Escherichia coli) microorganism, which were marked with 99mTc radioisotope, on surfaces of specimens was investigated. It was consequently determined that Ag was dominant in thecoatings obtained by applying 8 kV negative pulsed high voltage, while Ag decreased on the surfacedepending on the increase in the voltage.

WOS: 000316936600007, PubMed ID: 23164988, Introduction: Bacterial translocation occurs when intestinal mucosa and the intestinal wall lose their barrier properties against bacteria such as in the case of intestinal obstruction. Enteral nutrition with immunonutrients strengthens the immune system and thickens the intestinal barrier thus preventing bacterial translocation. Aim: The purpose of this study is to investigate the effect of uracil which is an immunonutrient on bacterial translocation using rats with intestinal obstruction as a model. Methods: Wistar albino rats were divided into three groups. The control group was fed with standard chow diet, while the other two groups were fed with uracil-supplemented chow diet. The rats were fed with these diets for seven days. And the end of the feeding period all groups were submitted intestinal obstruction and injected with Tc-99m labeled Escherichia coli into the rats' terminal ileum under anesthetic. The rats were sacrificed 24 h later. Their blood, mesenteric lymph nodes (MLN), liver, spleen, lung and ileum were removed to determine level of radioactivity. Results: When compared with the control group it was determined that uracil supplementation reduced the level of bacterial translocation. Conclusion: Uracil may be used in the prevention of bacterial translocation in cases of intestinal obstruction because it strengthens the intestinal barrier and the immune system. However, more studies are needed to clearly explain the mechanism behind uracil's beneficial role here. Crown Copyright (C) 2012 Published by Elsevier Ltd on behalf of Surgical Associates Ltd. All rights reserved.

This study aims to investigate effects of adenine on bacterial translocation (BT) using Tc-99m-labeled E. coli in an intestinal obstruction rat model. In the study twenty-one rats were used. The rats were divided into three groups according to different feeding patterns. The control group (CG) was fed with a standard chow diet for 7 days. Group A1 and group A2 were fed with adenine supplemented chow diet for 7 days. At the end of the feeding period, after all groups was submitted intestinal obstruction. Tc-99m-E. coli was injected into the rats' terminal ileum under anesthetic. The rats were sacrificed under aseptic conditions at 24th h after the surgery. The uptake of Tc-99m-E. coli was determined in organs such as the liver, mesenteric lymph nodes, spleen and ileum. Group A1 and group A2 results show that the uptake of Tc-99m-E. coli decreased in the blood and organs comparing to the CG. As a result, it was observed that adenine reduced the level of BT when compared with CG. The beneficial effect of adenine on BT in intestinal obstruction was observed. However, further studies are needed to more clearly assess how this benefit can be achieved.

Despite the progress in the diagnosis and management of early stage disease, the management of advanced prostate cancer remains an important problem. Prostate tissue expresses folate receptor (FR) which binds both folic acid and folate-linked drugs or imaging agents. Doxorubicin is the best known and most widely used member of the anthracycline antibiotic group of anticancer agents. The aim of this work is to develop a multifunctional nanoconjugate, (99m)Tc-folate-PEG-doxorubicin, in order to investigate its radiopharmaceutical potential as a prostate cancer imaging and real-time drug location imaging agent. Through this aim, biodistribution studies of (99m)Tc-folate-PEG-doxorubicin and control groups ((99m)Tc-doxorubicin and (99m)Tc-PEG-doxorubicin) in male rats were carried out. Obtained data showed that uptake of (99m)Tc-folate-PEG-doxorubicin in prostate was significantly higher than that of the control groups due to the affinity of folate ligand to folate receptor. As a consequence, it was indicated that (99m)Tc-FOL-PEG-DOX radiolabeled conjugate which has a great target/non-target organ ratio, is specific for target organ and has a high radiopharmaceutical potential as a prostate cancer and real-time drug location imaging agent.

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.

Folate conjugates exhibit high affinity for folate receptor (FR) positive cells and tissues, such as those in tumors, making them attractive candidates and of interest in diagnostic tumor imaging. The aim of study was to synthesize a novel radiopharmaceutical based folate conjugate, (99m)Tc-citro-folate, and to evaluate its efficiency as a targeted agent for imaging tumors that over express FR. TLC, HPLC (1)H NMR and LC-MS/MS methods were used to check and confirm the synthesized citro-folate. Citro-folate was labeled with Tc-99m with high labeling efficiency (97±1.0%). Biodistribution of the radiolabeled conjugate (99m)Tc-citro-folate was investigated in vivo using two groups of rats: FR saturated and unsaturated. These experiments showed high uptake of (99m)Tc-citro-folate in FR rich tissues and demonstrated its sensitivity and specificity in imaging ovary and uterus. Based on the demonstrated good radiolabeling and biodistribution properties, the compound (99m)Tc-citro-folate may potentially be used as a radiopharmaceutical agent for imaging the FR-positive tumors.

One of the fields of research in nuclear medicine is the development of new radiopharmaceuticals for imaging infection and inflammation in humans. For this development, several antimicrobial peptides, antibiotics, antibiotic peptide and chemotactic peptides, etc., have been radiolabeled with different radionuclides (⁶⁷Ga, ⁹⁹(m)Tc, ¹¹¹In, ¹⁸F, ¹³¹I, etc.) and their imaging potentials studied. Actually, it is very important to distinguish between infection and inflammation. In this respect, radiolabeled antibiotics have advantages because many of the properties of the ideal infection-specific agent through antibiotics localizes in infection site. In this review, only ⁹⁹(m)Tc-labeled antibiotics are evaluated and discussed.

Raloxifene is a selective estrogen receptor modulator that produces both estrogen agonistic effects on bone and lipid metabolism and estrogen-antagonistic effects on uterine endometrium and breast tissue. In the present study, raloxifene was labeled with I-131 by iodogen method and investigated for its radiopharmaceutical potential. Radiolabeling yield is 91±0.7%, as determined by radio thin layer chromatography (RTLC). Results of in vitro study indicated 131 I-raloxifene has high stability (4 h) in serum. Biodistribution study was carried out with Albino wistar female rats. The result has shown that the radioiodinated raloxifene has higher uptake in uterus than breast and ovarian.

Codeine which was extracted from dry capsules of the opium poppy (Papaver somniferum) was purified by HPLC (High Performance Liquid Chromatography) and characterized by NMR (Nuclear Magnetic Resonance) and IR (Infrared) spectroscopy techniques. The purified compound was labeled with 131I and biodistribution studies were performed in rats. Radioiodinated codeine distributed uniformly in the cerebellum, m.pons, striatum and hypothalamus while the other branch of brain and Stomach, urinary bladder, and small intestine uptakes were significantly higher than other tissues.

Multiple-drug therapy is common in current clinical practice. Because of this, people have been ready to embrace simplistic approaches to cold treatment, such as vitamin C and zinc. Ascorbic acid (vitamin C) is mostly administrated together with cough–cold drugs. The aim of this study was to investigate the effect of cough–cold drugs on the uptake of ascorbic acid using 99mTc-ascorbic acid (99mTc-AA) in male albino Wistar rats. Ascorbic acid was labeled with Tc-99m and the distribution of 99mTc-AA was investigated. The uptake of 99mTc-AA was evaluated when administrated alone (group I), with chlorpheniramine maleate (CPR) (group II), with phenylpropanolamine hydrochloride (PPA) (group III), and with acetaminophen (APAP) (group IV). In some organs (apart from kidneys, intestinal system, and stomach) the uptake of 99mTc-AA was not significantly affected by the administration of 99mTc with CPR or 99mTc with APAP at 120 min. On the other hand, there was significant difference in the uptake of 99mTc-AA between groups I and III. The administration of 99mTc-AA with PPA in rats caused an increase of the uptake of 99mTc-AA at 120 min in the investigated organs compared to the administration of 99mTc-AA alone. The present data show that vitamin C might be more effective for the treatment of common cold when coadministered with PPA compared to with CPR, with APAP, or alone.

Bombesin-like peptides are related to several human cancer receptors, including small cell lung, prostate, breast, colon, and pancreatic cancers. Litorin, an amphibian bombesin peptide derivative, is found to stimulate the contraction of smooth muscle, to stimulate gastrin, gastric acid, and pancreatic secretion, and to suppress the nutriment in in vivo experiments. In the present study, litorin was labeled with 99mTc by the stannous chloride procedure. Labeling yield is 95 +/- 1.4%, as determined by radio thin layer chromatography (RTLC) and radio high performance chromatography (RHPLC). Results of in vitro studies demonstrated a high stability in serum and cysteine solutions. In vivo biodistribution was investigated with normal male Albino Wistar rats. Biodistribution data showed fast clearance, low intestinal accumulation, and significant uptake in bombesin/gastrin releasing peptide (BN/GRP) receptor rich tissues such as the pancreas (23.56 +/- 0.01 %ID/g 30 min pi). It can be blocked partially by previous administration of 'cold' litorin. The results showed specificity of the uptake. As 99mTc-litorin displays good radiolabeling and biodistribution, it is a potentially useful radiopharmaceutical for detection of bombesin receptor-expressing cancers.

Background and Objective: Pancreatic cancer is very common and difficult to diagnose in early stage. Imaging systems for diagnosing cancer have many disadvantages. However, combining different imaging modalities offers synergistic advantages. Optical imaging is the most multidirectional and widely used imaging modality in both clinical practice and research. Methods: In present study, Zinc(II) phthalocyanine [Zn(II)Pc] was synthesized, labeled with iodine- 131 and in vitro study was carried out. The intracellular uptake studies of radiolabeled Zn(II)Pc were performed in WI-38 [ATCC CCL-75™, tissue: human fibroblast lung] and MIA PaCa-2 [ATCC CRL-1420™, tissue: human epithelial pancreas carcinoma] cell lines. Results: The intracellular uptake efficiency of radiolabeled Zn(II)Pc in MIA PaCa-2 cells was determined two times higher than WI-38 cells. Also, fluorescence imaging (FI) efficiency of synthesized Zn(II)Pc was investigated in MIA PaCa-2 cells and significant uptake was observed. Conclusion: Zn(II)Pc might be used as a new agent for dual fluorescence/nuclear imaging for pancreatic cancer.

Photodynamic therapy (PDT) is based on exposing a light-sensitive material that has been localized in target tissues with visible light. In the current study, symmetric Zn(II) octaoctadodecylphthalocyanine (1) and the asymmetrically substituted hydroxyhexyloxy derivative (2) were examined as a multifunctional agent for tumour nuclear imaging and for PDT potential. Zn(II)Pc 1 and Zn(II)Pc 2 were radiolabelled with (131) I using an iodogen method with high efficiency (93.5 ± 3.5% and 93.0 ± 2.8%, respectively) under the optimum conditions. Biodistribution study results showed that radiolabelled Zn(II)Pc 1 had a high uptake in the large intestine and unchanging uptake in the ovary. However, radiolabelled Zn(II)Pc 2 uptake was statically significant in the large intestine, pancreas, ovary and lung. For the PDT studies, EMT6/P (mouse mammary cell line) and HeLa (cervical adenocarcinoma cell line) with Zn(II)Pc 1 and Zn(II)Pc 2 were exposed to red light (650 nm) at 10-30 J/cm(2) . Zn(II)Pc 1 and Zn(II)Pc 2 had a good PDT efficacy in the EMT6/P cell line. In conclusion, radiolabelled Zn(II)Pc 1 might be a promising imaging agent for pancreas, ovary and colon tumours. However, the radiolabelled Zn(II)Pc 2 might be a promising nuclear imaging and PDT agent for colon, lung, pancreas and ovary tumours.

Crude extract of S. officinalis L. was found to have suspending agent, hemolytic, antitumor, antioxidant and antimicrobial activities. Its major components benzofurans and benzofuran glycosides have antifungal, anticancer, antibacterial and anticomplement activities and display acetylcholinesterase-cyclooxygenase inhibitory and cytotoxic properties. Recently, it has been reported that egonolgentiobioside is a valuable target for structural modification and warrants further investigation for its potential as a novel pharmaceutical tool for the prevention of estrogen deficiency induced diseases. The aim of the current study is to perform in vivo biological evaluation of a glycosides extract, which was isolated from the fruits endocarp of Styrax officinalis L, identified as egonolgentiobioside and homoegonolgentiobioside and labeled with 131I. The radiolabeled glycosides extract was labeled with 131I with high yield. The labeled obtained radiolabeled compound was found to be quite stable and lipophilic. In order to determine its tissue distribution, an in vivo study was performed using healthy female Albino Wistar rats injected by 131I-glycosides. The biodistribution results showed that clearance of the radiolabeled compound is through the hepatobiliary pathway. The experimental study indicated that the radiolabeled glycosides extract accumulated in the large intestine. Therefore, the potential of 131I-glycosides might be evaluated in colon cancer cell lines and this might be a promising of tumor-imaging agent.

In recent years, the photodynamic therapy studies have gained considerable attention as an alternative method to surgery, chemotherapy and radiotherapy which is commonly used to fight cancer. In this study, biological potentials of a benzyloxy bearing zinc(II) pheophorbide-a (Zn-PH-A) were investigated via in vivo and in vitro experiments. Zn-PH-A was labeled with (131)I with high efficiency (95.3 ± 2.7%) and its biodistribution studies were investigated on female Albino Wistar rats. The radiolabeled photosensitizer had been intravenously injected into the tail vein, and then the animals were sacrificed at 30, 60 and 120 min post injection. The percent of radioactivity per gram of organs (%ID/g) was determined. The radiolabeled Zn-PH-A showed high uptake in ovary. In addition, photodynamic therapy studies of the photosensitizer were conducted in EMT6, murine mammary carcinoma and HeLa, human cervix carcinoma cell lines. For the photodynamic therapy studies, the cells with Zn-PH-A were exposed to red light (650 nm) at the doses of 10-30 J/cm(2). The results showed that Zn-PH-A has stronger PDT effect in EMT6 than HeLa cell. Our present work demonstrates (131)I-labeled photosensitizer as a bifunctional agent (PDT and nuclear imaging) which could be improved in future by using EMT6 growing tumor in nude mice.

Summary Objective This study was designed to evaluate iodine deficiency status in children 6–12 years in the west coast (Aegean Region) of Turkey after 5 years of mandatory iodine prophylaxis. A total of 2300 children from 72 populations (rural and urban area) were evaluated with urinary iodine excretion and thyroid volume. Design Cross-sectional, observational study designed and performed according to surveillance methods for iodine deficiency disease (IDD) prevalence recommended by WHO/UNICEF/ICCIDD. Subjects The study population consisted of 2300 school children age ranging from 6 to 12 years. The children were selected by multiple stage randomization from 91 primary schools of 76 zones (91 clusters). Information about the use of iodized salt was obtained from the families. Measurements Data on the following were collected: birth date, sex, weight, height, thyroid size by palpation and ultrasonography; and urinary iodine by isotope dilution analysis method. Thyroid volumes above 97th percentile according to the WHO/ICCIDD by age and body surface area (BSA) were accepted as goitre. Results Iodized salt consumption was 51·7%. The prevalence of goitre determined by palpation was 12·1% and by ultrasound based on BSA and age were 9·8% and 5·5%, respectively. Median urinary iodine was 53 (2–142) µg/l. Conclusion Mild to severe degree of iodine deficiency was detected in the west coast of Turkey.

The aim of this study is to synthesize novel 131I labeled estrone derivatives that may have therapeutical potentials on Estrogen Receptor rich tumors. Two radiolabeled estrone derivatives, [131I]2-iodo-3-methoxy-estra-1,3,5-trien-17-one and [131I]4-iodo-3-methoxy-estra-1,3,5-trien-17-one were synthesized. Ether amino estrone derivatives were obtained from estrone in three steps by means of diazonium compounds. Tissue distribution studies exhibited receptor-mediated uptake in target organs in female Albino Wistar rats. Maximum uptakes for 2-iodo[131I]-3-methoxy-estrone are in stomach, pancreas, intestines and uterus. A similar biodistribution profile was obtained for 4-iodo[131I]-3-methoxy-estrone. However 2-iodo-3-methoxy-estra-1,3,5-trien-17-one has higher uptake in stomach, kidneys, pancreas, and intestines than 4-iodo-derivative.

Famotidine, a gastrointestinal drug was labeled with 99mTc and its radiopharmaceutical potential was observed on male Albino Wistar rats. Labeling yield was over 95%. Average specific activity and n-octanol/water partition coefficient (lipophilicity) were approximately 74 MBq/mg-0.66 GBq/mg and 3.4, respectively. Biodistribution studies were performed on Albino Wistar rats. The activity per gram tissue was calculated and time-activity curves were generated. The majority of the activity was observed in stomach, small intestines and kidneys. Liver and kidneys showed lower uptake compared to other H2-receptor rich tissues. Results show that 99mTc-famotidine is H2receptor specific.

Tissue distribution of the 99mTc labeled derivative of the estrogen compound 3,17-alpha-estradiolyl propyl 1,4,8,11-tetraazacyclotetradecanyl-l-(4-methylbenzoic acid) ester (ESTCPTA), which has an 3,17-alpha-estradiolyl propinol coupled to l-(4-methylbenzoic acid)1,4,8,11-tetraazacyclotetradecane (CPTA), was compared to 99mTc-MIBI (methoxyisobutyl isonitrile) in female Albino Wistar rats. Tissues of interest included lung, liver, heart, kidneys, spleen, stomach, intestines, pancreas, muscle, blood, breast, ovary, fat, and uterus. 99mTc-ESTCPTA uptake by the uterus and ovary, as ER-rich tissues, was highly selective. Maximum uptakes for 99mTc-MIBI and 99mTc-ESTCPTA are 90 min in breast, ovary and uterus. The pancreas also showed significant receptor saturated and unsaturated ratios for 99mTc-ESTCPTA. Results are sufficiently encouraging to generate further evaluation of these and related compounds as possible estrogen receptor based tumor imaging and therapeutic agents in estrogen-rich tissues.

The biological potential of a synthetic copper chlorophyll derivative was investigated via in vivo and in vitro experiments. The Cu-chlorophyll derivative photosensitizer (Cu-PH-A) was labeled with 131I with high efficiency (92.9 ± 4.2%) using the iodogen method. Cell culture studies were performed with the MCF-7 and MDAH-2774 cell lines after radiolabeling. The photosensitizing activity of Cu-PH-A was more effective in MDAH-2774 cells than in MCF-7 cells at a concentration of 50 μM. When the biodistribution in female Albino Wistar rats was examined, uptake of the radiolabeled photosensitizer was maximal in the liver and ovaries after 60 min. It is concluded that radiolabeled Cu-chlorophyll derivative photosensitizer has high uptake in ovaries in normal rats. In addition, the intercellular uptake and PDT efficacy of the Cu-PH-A in MDAH-2774 were good compared with MCF-7 cells. This photosensitizer could be useful for both ovary tumour imaging and PDT.

The aim of the present study was to demonstrate the possible transplacental transmission of I-131 labeled recombinant human erythropoietin (I-131-rh-EPO) in pregnant rats and its distribution through maternal and fetal organs. Six Wistar Albino Rats in their pregnancy of 18 days were used I-131 labeled recombinant human erythropoietin (specific activity = 2.4 mu Ci/IU) was injected into the tail vein of rats. After 30 minutes labeled erythropoietin infusion maternal stomach, kidney, lung, liver, brain and heart as well as fetus were removed. Then, the same organs were removed from each fetus. Measuring weight of maternal and fetal organs as well as placenta were followed by radioactivity count via Cd(Te) detector. I-131 labeled recombinant human erythropoietin was found to be able to pass rat placenta and its distribution order in fetal organs was similar to those of maternal organs. Besides, as measurements were performed closer to cornu uteri, uptakes were decreasing in every fetus and its corresponding placenta.

15th International Symposium on Radiopharmaceutical Chemistry -- AUG 10-14, 2003 -- Sydney, AUSTRALIA, WOS: 000234790900001, PubMed ID: 16394539, The aim of this study was to label ascorbic acid with Te-99m and to investigate its radiopharmaceutical potential in rats. Ascorbic acid was labeled with Tc-99m using the stannous chloride method. The radiochemical purity of [Tc-99m]ascorbic acid (Tc-99m-AA) was determined by RTLC, paper electrophoresis, and RHPLC methods. The labeling yield was found to be 93 +/- 5.0%. The maximum labeling yield of Tc-99m-AA was determined at pH 5 and 25 degrees C. The biodistribution studies related to Tc-99m-AA were done in male albino Wistar rats. Tc-99m-AA, which has a specific activity of 13.02 GBq/mmol, was administered into the tail vein of the rats. The rats were sacrificed at 15, 30, 60, and 120 min after the injection by heart puncture under ether anaesthesia. The organs were weighed after removal. Their activities were counted using a Cd(Te) detector equipped with a RAD 501 count system. The %ID/g (% of injected dose per gram of tissue weight) in each organ and in blood was calculated. Maximum uptake of Tc-99m-AA was observed in prostate and kidneys at the 60th min. Tc-99m-AA may be a promising radio-pharmaceutical for the imaging of prostate and kidneys.

We aimed to assess the ability of (131)I-Pentamidine scintigraphy to detect the lesions of Leishmania tropica infection. An experimental model of cutaneous leishmaniasis was developed. The presence of cutaneous leishmaniasis was confirmed. Pentamidine was radioiodinated with (131)I. The radiolabeled pentamidine was validated by the requisite quality control tests to check its radiolabeling efficiency, in vitro stability. (131)I-Pentamidine (activity: 18.5 MBq/100 µl) was injected intracardiacally into infected hamsters. Static whole body images of the hamsters were acquired under the gamma camera at 5 and 30 min, 2, 6 and 24 h following the administration. On the scintigrams, anatomically adjusted regions of interest (ROIs) were drawn over the right feet (target) and left feet (not-target) and various organs. Accumulation of (131)I-Pentamidine at sites of infection is expressed as the target to non-target (T/NT) ratio. The results T/NT ratio decreased with time. In concluding the (131)I-Pentamidine has poor sensitivity in detection of L. tropica infection.

Radiopharmaceuticals are localized in (malignant) tumor tissues by different mechanisms. One of these mechanisms, gelatinase enzyme activity, is associated with poor prognosis in cancer patients and potential targets for tumor imaging. There are some gelatinases to be associated with metastatic potential for tumor imaging to possibly predict metastases. In this study, a cyclic decapeptide conjugate, DTPA-CLP (DTPA-Cys-Leu-Pro-Gly-His-Trp-Gly-Phe-Pro-Ser-Cys), was selected as a peptide conjugate because of its selective inhibitory activity toward gelatinases. Peptide-conjugated DTPA-CLP was labeled with (99m) Tc with a radiolabeling efficiency of 97.0 ± 2.8%. After determining optimization conditions for radiolabeling, a biodistribution study of radiolabeled peptide in albino Wistar rats was performed. According to biodistribution data, (99m) Tc-DTPA-CLP showed high uptake in the lung, liver, uterus, and spleen. These results show that (99m) Tc-DTPA-CLP may be used for the imaging of gelatinase activity in metastatic tumors.

In malignant tissues, MMP-9 (gelatinase B, 92 kDa type IV collagenase) and MMP-2 (gelatinase A, 72 kDa type IV collagenase) are the most prevalent matrix metalloproteinases related to the tumor aggressiveness and metastatic potential. Since elevated levels of gelatinases are associated with poor prognosis in cancer patients, these enzymes are potential targets for tumor imaging to possibly predict metastases. In the present study, a cyclic decapeptide, CLP (Cys–Leu–Pro–Gly–His–Trp–Gly–Phe–Pro–Ser–Cys), was selected as a basic peptide because of its selective inhibitory activity toward gelatinases. The peptide was labelled with 99mTc with a radiolabelling efficiency of 94.6±4.1%. After determining the appropriate conditions for radiolabelling, a biodistribution study of radiolabelled peptide in Albino Wistar rats was done. According to biodistribution data, 99mTc-CLP showed high uptake in the lung, liver, uterus and spleen. The amount of normal tissue MMPs enzymes is known to be lower than a tumor tissue. In this connection, our findings show that matrix metalloproteinases inhibitory peptide which is CLP is labeled with 99mTc with high yield and radiolabeled peptide might be might be utilized for the imaging of gelatinase activity due to overexpression of MMP-2 and MMP-9 in tumor tissue.

We aimed to assess the ability of (131)I-Pyrimethamine scintigraphy to detect the lesions of Toxoplasma gondii infection. An experimental model of toxoplasmosis was developed. The presence of toxoplasmosis was confirmed 60 days after implantation. Pyrimethamine was radioiodinated with I-131. The radioligand was validated by the requisite quality control tests to check its radiolabeling efficiency, in vitro stability and radiochemical purity etc. (131)I-Pyrimethamine (specific activity: 7.08 MBq/µmol) was injected intravenously into the tail vein of the control and infected rats. Static whole body images of the rats were acquired under the gamma camera at 5 min, 45 min, 2 h, 6 h, and 24 h following the intravenous administration of the radioactivity (3.7 MBq/rat). Then the scintigraphic data were analyzed both visually and semiquantitatively. Regions of interest (ROIs) were drawn over the organs (thyroid, stomach, liver, bladder, and soft tissues) to calculate the ratios of the radiotracer in infected vs. control rats. The mean ratio of radiotracer in infected/control rats in the liver and diaphragm was over 1 at 45 min which persisted till 24 h. In conclusion, (131)I-Pyrimethamine may be useful agent for diagnosis toxoplasmosis especially involving liver and diaphragm, needs further preclinical validation before being extended for use in clinical applications.

Epigallocatechin gallate (EGCG), is the most abundant and widely studied catechin in green tea (Camellia sinensis Theaceae). The inhibitory effects of EGCG and green tea extract on carcinogenesis in various organs in rodents have now been demonstrated over the past decade. The aim of study was to label EGCG with I-131, to determinate its structure and to evaluate its biodistribution in Wistar rats. Radiolabeling was carried out by direct electrophilic iodination method (iodogen) and yield was determined by radio thin layer chromatography (RTLC). Radiolabelling yield is determined as 89 ± 1.0%. Besides, determination of structure of iodinated molecule, serum stability, and partition coefficient experiments was performed. The structure analysis of synthesized cold 127I-EGCG complex was assessed with LC–MS–MS and 1H-NMR. 1H-NMR and LC–MS–MS results of iodinated EGCG (127I-EGCG) show that oxidize iodine reacts electrophilic with aromatic ring. Serum stability results showed that in vitro stability of 131I-EGCG was quite high. It is observed that labeling percentage decreased 83 ± 2% at 24th, Partition coefficient results show that the partition coefficient of EGCG was calculated as theoretical partition coefficient = 2.04 ± 0.42 and the experimental partition coefficient of 131I-EGCG was found as 1.46 ± 0.2. The biodistribution data shown that the maximum uptake of the radioiodinated EGCG was seen in lung and pancreas at 30 min. The blocking assay results indicated that the uptake of 131I-EGCG in lung was not significantly change (0.25, 0.23, and 0.22%ID/g at 30, 60, and 150 min, respectively). Biodistribution data showed no significant uptake in a specific organ of the rat. Hence radiolabeled EGCG is seen in some organs (lung, liver, pancreas, kidney, etc.).

This study aims to prepare (99m)Technetium Pheophorbide-a ((99m)Tc-PH-A) complex and evaluate its efficiency as an infection imaging agent. First, PH-A was obtained from Spirulina maxima algae, and the product compound was confirmed using (1)H NMR and MS (ESI) methods. The PH-A was then labeled with (99m)Tc using the tin chloride method and its biological efficacy as a potential radiotracer for Staphylococcus aureus (S. aureus) infection was evaluated in bacterially infected and sterile inflamed rats. The radiochemical stability of the (99m)Tc-PH-A in human serum was determined by thin-layer radiochromatography (TLRC). The radiochemical purity was 87±3.2% and remained constant at more than 80±0.1% even in serum for 120 min after radiolabeling. These experiments indicated that the ratio of (99m)Tc-PH-A uptake in bacterially infected muscle, as compared to normal muscle, [target/non-target (T/NT)=5.6 at 1h] was over four times higher than that in sterile inflamed muscle (T/NT=1.29 at 1h). Disappearance of activity from the kidney and liver indicated that the urinary and hepatobiliary systems were the normal routes of excretion of the complex. (99m)Technetium Pheophorbide prepared with high yield is able to localize well in the bacterially infected muscle of the rats and (99m)Tc-PH-A may be developed as a radiopharmaceutical agent to distinguish infection from inflammation by nuclear imaging.

In this study, we reported on the synthesis and biological evaluation of radiolabeled fluorescent dye conjugated bovine serum albumin nanoparticles within the size range 190–210 nm. The bovine serum albumin nanoparticles (BSANPs) were prepared using a desolvation method, and chemical cross-linking was performed using gluteraldehyde. Furthermore, pheophorbide-a (PH-A) was loaded on the BSANPs. The results obtained from dynamic light scattering and electron microscopy have proved that nanoparticles are highly monodisperse and near-spherical shaped. The photo-physical properties of the PH-A-BSANPs were obtained using the spectrophotometric techniques. According to the results, PH-A and BSANPs show high non-covalent interaction. PH-A loaded nanoparticles were labeled with 99m Tc and the radio-labeling efficiency was determined as 90 ± 1.2%. Biodistribution studies of 99m Tc labeled PH-A-BSANPs and PH-A were carried out using female Albino Wistar rats, and 99m Tc-PH-A-BSANPs showed a significantly higher uptake in the breast and uterus than 99m Tc-PH-A. Cell culture study was carried out in MCF-7 cell line (human breast adenocarcinoma cell line). According to the cell culture studies, 99m Tc-PH-A-BSANPs showed a higher uptake than 99m Tc-PH-A. Moreover, PH-A-BSANPs demonstrated good photo-physical properties and BSANPs increased the uptake of PH-A on to the MCF-7 cell line. These results confirm that 99m Tc labeled PH-A-BSANPs could be utilized for radioimaging.

The aim of the present study was to prepare (99m)Tc-folate-glucaric acid and investigate the radiopharmaceutical potential for tumors imaging that over express folate receptor. Folate-glucaric acid was synthesized and the synthesized folate conjugate was confirmed with (1)H NMR and LC-MS/MS methods. Folate-glucaric acid was labeled with (99m)Tc, and its radiolabelling efficiency was found as 96 ± 2.0%. Biodistribution study of (99m)Tc-folate-glucaric acid was carried out in vivo using two groups of female Albino Wistar rats: folate receptor (FR) saturated and unsaturated. Biodistribution study showed that (99m)Tc-folate-glucaric acid indicated high uptake in folate receptor rich tissues such as breast, ovary and uterus. Therefore, (99m)Tc-folate-glucaric acid shows good radiolabeling and biodistribution in FR organs, the radiolabeled conjugate is a reason potentially useful radiopharmaceutical for detection of FR-positive tumors.

Radiopharmaceuticals are useful to evaluate effectiveness of cancer treatments as well as diagnosis of diseases. (99m)Tc-Glucoheptonate has high sensitivity for imaging lung cancer tissues. In this study, the potential use of (99m)Tc-glucoheptonate for monitoring apoptosis related to chemotherapeutic agents is investigated in vitro using A549 lung cancer cell line. A decrease in (99m)Tc-glucoheptonate uptake ratio was observed depending on the level of apoptosis. (99m)Tc-glucoheptonate is found to be useful for the detection of apoptosis following treatment in A549 lung tumor cells.

The aim of this study was to localize the biodistribution of Technetium-99m (Tc-99m) Mebendazole in experimentally Trichinella spiralis (T. spiralis)-infected rats. Localizing and distinguishing the "T. spiralis" in body sites are very important and life saving processes. Scintigraphic detections may help to determine the sites of trichinellosis infection. Twelve healthy female Wistar rats were infected via oral administration of infected muscle containing 750 to 1000 larvae. In this study, the antibiotic was labeled with Tc-99m, and Tc-99m-Mebendazole was assessed as an infection imaging agent in a rat model. Tc-99m-mebendazole was examined for localizing the normal, and inflamed with trichinellosis in rat muscle tissues after administrated Tc-99m-mebendazole via intravenous (IV) or oral gastric catheter, and also for differentiating them from each other. Tc-99m labeled mebendazole was retained in infectious areas. It was established that Tc-99m-mebendazole which was administrated via IV route has high organ restrain level. It was observed that Tc-99m-mebendazole uptake was high in tongue and diaphragm muscles of T. spiralis-infected rats after administration of radiolabeled mebendazole via either oral or IV routes. This study may be viewed as a basement of future studies on diagnosis of T. spiralis infection.

Two 99mTc-DTPA attached estrone derivatives were synthesized and their radiopharmaceutical potential was determined using female albino Wistar rats.Two novel radiolabeled estrone derivatives, 99mTc-2,2',2"2"'-(2,2'-(2-(3-methoxy-13-methyl-17-oxo-7, 8, 9, 11, 12, 13, 14, 15, 16, 7-decahydro-6H- cyclopenta[a]phenanthren-2-ylamino)-2- oxoethylazanediyl) bis(ethane-2,1-diyl)) bis(azanetriyl) tetraacetic acid (99mTc-2-DTPA-3-methoxy estrone) and 9mTc-2,2',2",2'"-(2,2'- (2-(3-methoxy-13-methyl-17-oxo- 7,8,9,11,12,13,14,15,16,17-decahydro- 6H-cyclopenta[a]phenanthren-4-ylamino)-2-oxoethylazanediyl) bis(ethane-2,1-diyl))bis(azanetriyl)tetraacetic acid (99mTc-4-DTPA-3-methoxy estrone) were synthesized starting from estrone (3-hydroxy-13-methyl-7,8, 9,11,12,13,15,16-octahydro-6H-cyclopenta[a]phenanthren-17(14H)-one) and DTPA anhydride (2-(bis(2-(2,6-dioxomorpholino)ethyl)amino)acetic acid) as potential estrogen receptor imaging agents. The products were crystallized in ethyl alcohol (95%), purified by high performance liquid chromatography (HPLC) and characterized by nuclear magnetic resonance (NMR) and infrared spectroscopy (IR). The effect of the radiolabeled compounds on the biological behaviour of the molecules was evaluated through biodistribution studies in female albino Wistar rats. The rats were sacrificed at various time intervals, their organs were removed, and the activities of organs were counted using a gamma counter equipped with a Cd(Te) solid state detector.Organ uptake was calculated as activity/gram tissue and time versus activity curves were generated. The tissue distribution studies exhibited a receptor-mediated uptake in the target organs of the rats for each compound. Both 99mTc-2-DTPA-3-methoxy estrone and 99mTc-4-DTPA-3-methoxy estrone were stable in vitro and were mainly excreted through the hepatobiliary pathway. The biological data showed that the 99mTc-2-DTPA-3-methoxy estrone had higher uptake in the target tissues than the 99mTc-4-DTPA-3-methoxy estrone. The favourable in vitro/in vivo stability and biodistribution profiles suggest that these radioligands are good candidates for further exploration of their potential clinical applications.

In general, lead is used as shielding material for protection against radiation. In spite of its high density, lead is toxic and lead aprons are very heavy for personal shielding. Thus, there is a need for nontoxic, light, and environmental friendly radiation-shielding materials. Polymers cannot be effective against gamma radiation on their own. High-density metal wolfram carbide could be useful against gamma radiation, and boron carbide could also be useful for neutron shielding. In this study, high-density polyethylene, boron carbide, and wolfram carbide can be mixed in certain amounts and composite discs can be obtained in this way. According to results, a new shielding material is efficient for gamma radiation.

New [Ru(L1)(dcbpy)(NCS) 2 ] complex was synthesized in a one-pot reaction starting from [RuCl 2 ( p -cymene)] 2 , where the ligands (dcbpy=4,4′-dicarboxy-2,2′-bipyridine, L1=dipyrido[3,2- a :2′,3′- c ]phenazine-11-ylcarbonyl)-sodium) are introduced sequentially. The resulting complex was characterized by IR, NMR, and elemental analysis. The complex was labeled with I-131. Biodistribution study of the complex was carried out using 131 I-labeled [Ru(L1)(dcbpy)(NCS) 2 ] complex. The biodistribution study performed with albino Wistar male rats has shown that the complex has high uptake in the lung, small intestine, fat, and spleen.

To investigate the microbial adherence to the surfaces of a nonprecious metal alloy after plasma nitriding.The plasma-nitriding process was performed to the surfaces of metals prepared from a nickel-chromium alloy. The microorganisms were labeled with technetium-99m. After the labeling procedure, 60 metal disks were treated with a microorganism for each use.The results revealed that the amount of adherence of all microorganisms on surfaces was changed by plasma-nitriding process; adherence decreased substantially (P.05) and the differences in plasma nitriding time were not significant (P.05)With the plasma-nitriding process, the surface properties of nonprecious metal alloys can be changed, leading to decreased microbial adherence.

Objective We aimed to evaluate whether Ca +2 utilization of intestinal flora (IF) has an effect on urinary excretion of Ca +2 (UCaE) levels. Materials and Methods Fecal samples (0.1 g/mL) of children who underwent UCaE examination in the past year were implanted in broths. Labeled 45 Ca (5 μL) was added to the samples and incubated. From these samples, a 200-μL quantity was filtrated with a 0.45-micrometer membrane and was rinsed in 200 μL pure water. 45 Ca activity in the membrane was measured and defined as percent activity per bacteria ( 45 Ca act %/CFU). Levels of aerobic and anaerobic 45 Ca act %/CFU and their correlations with UCaE were compared between hypercalciuric (Group I) and normocalciuric (Group II) patients. Results Levels of 45 Ca %/CFU were similar between groups ( P > .05). Aerobic and anaerobic 45 Ca act %/CFU levels were not significantly correlated to UCaE, either in normocalciuric ( P = .079, r=−0.503; P = .260, r=−0.420, stray mart respectively) or in hypercalciuric children ( P = .509, r=0.223; P = .623, r=−0.257, respectively). Conclusion Similar 45 Ca act %/CFU levels in the 2 groups imply that calcium utilization of IF does not have a distinct effect on UCaE.

WOS: 000235852700021, PubMed ID: 16462075, The aim of the present study was to label acetaminophen (APAP) with I-131 and to determine its radiopharmaceutical potential in rats. Acetaminophen was labeled with I-131 using the iodogen method. The radiochemical purity of I-131-APAP was determined by RTLC and paper electrophoresis. The labeling yield was 94 +/- 4%. The biodistribution studies of the labeled compound (specific activity; 56.60 GBq/mmol) were performed in male Albino Wistar rats. The uptake of I-131-APAP in some organs were determined at different time after injection to the rats. The radioactivity in each organ was counted and the percentage of injected activity per gram of tissue weight (%ID/g) for each organ and blood was calculated. I-131-APAP uptake in the lung, liver, kidneys, pancreas, blood, stomach and some brain region, were observed. Thus, I-131-APAP may be radiopharmaceutical for the imaging of the brain.