Search

Prostate-specific membrane antigen (PSMA) is expressed by the majority of clinically significant prostate adenocarcinomas, and patients with target-positive disease can easily be identified by PSMA PET imaging. Promising results with PSMA-targeted radiopharmaceutical therapy have already been obtained in early-phase studies using various combinations of targeting molecules and radiolabels. Definitive evidence of the safety and efficacy of [¹⁷⁷Lu]Lu-PSMA-617 in combination with standard-of-care has been demonstrated in patients with metastatic castration-resistant prostate cancer, whose disease had progressed after or during at least one taxane regimen and at least one novel androgen-axis drug. Preliminary data suggest that ¹⁷⁷Lu-PSMA-radioligand therapy (RLT) also has high potential in additional clinical situations. Hence, the radiopharmaceuticals [¹⁷⁷Lu]Lu-PSMA-617 and [¹⁷⁷Lu]Lu-PSMA-I&T are currently being evaluated in ongoing phase 3 trials. The purpose of this guideline is to assist nuclear medicine personnel, to select patients with highest potential to benefit from ¹⁷⁷Lu-PSMA-RLT, to perform the procedure in accordance with current best practice, and to prepare for possible side effects and their clinical management. We also provide expert advice, to identify those clinical situations which may justify the off-label use of [¹⁷⁷Lu]Lu-PSMA-617 or other emerging ligands on an individual patient basis. in press

Contains fulltext : 238612.pdf (Publisher’s version ) (Closed access) Nuclear medicine plays an increasingly important role in the management neuroendocrine neoplasms (NEN). Somatostatin analogue (SSA)-based positron emission tomography/computed tomography (PET/CT) and peptide receptor radionuclide therapy (PRRT) have been used in clinical trials and approved by the European Medicines Agency (EMA) and the US Food and Drug Administration (FDA). European Association of Nuclear Medicine (EANM) Focus 3 performed a multidisciplinary Delphi process to deliver a balanced perspective on molecular imaging and radionuclide therapy in well-differentiated neuroendocrine tumours (NETs). NETs form in cells that interact with the nervous system or in glands that produce hormones. These cells, called neuroendocrine cells, can be found throughout the body, but NETs are most often found in the abdomen, especially in the gastrointestinal tract. These tumours may also be found in the lungs, pancreas and adrenal glands. In addition to being rare, NETs are also complex and may be difficult to diagnose. Most NETs are non-functioning; however, a minority present with symptoms related to hypersecretion of bioactive compounds. NETs often do not cause symptoms early in the disease process. When diagnosed, substantial number of patients are already found to have metastatic disease. Several societies' guidelines address Neuroendocrine neoplasms (NENs) management; however, many issues are still debated, due to both the difficulty in acquiring strong clinical evidence in a rare and heterogeneous disease and the different availability of diagnostic and therapeutic options across countries. EANM Focus 3 reached consensus on employing (68)gallium-labelled somatostatin analogue ([(68)Ga]Ga-DOTA-SSA)-based PET/CT with diagnostic CT or magnetic resonance imaging (MRI) for unknown primary NET detection, metastatic NET, NET staging/restaging, suspected extra-adrenal pheochromocytoma/paraganglioma and suspected paraganglioma. Consensus was reached on employing (18)fluorine-fluoro-2-deoxyglucose ([(18)F]FDG) PET/CT in neuroendocrine carcinoma, G3 NET and in G1-2 NET with mismatched lesions (CT-positive/[(68)Ga]Ga-DOTA-SSA-negative). Peptide receptor radionuclide therapy (PRRT) was recommended for second line treatment for gastrointestinal NET with [(68)Ga]Ga-DOTA-SSA uptake in all lesions, in G1/G2 NET at disease progression, and in a subset of G3 NET provided all lesions are positive at [(18)F]FDG and [(68)Ga]Ga-DOTA-SSA. PRRT rechallenge may be used for in patients with stable disease for at least 1 year after therapy completion. An international consensus is not only a prelude to a more standardised management across countries but also serves as a guide for the direction to follow when designing new research studies.

Einleitung: Der Einfluss früherer Therapien, insbesondere der Chemotherapie, auf das Gesamtüberleben (OS) von Patienten mit kastrationsresistentem Prostatakarzinom (CRPC), die mit Lu-PSMA-617 behandelt wurden, wurde kontrovers diskutiert. Daher führte WARMTH eine multizentrische Analyse[zum vollständigen Text gelangen Sie über die oben angegebene URL], 66. Kongress der Nordrhein-Westfälischen Gesellschaft für Urologie

Background and Aims: Origanum hypericifolium, Origanum minutiflorum, Origanum saccatum, and Origanum haussknechtii are some of the endemic Origanum species in Turkey. In the literature, besides the known effects of these Origanum species, no antispasmodic activity was determined. Therefore, we investigated Origanum species for possible antispasmodic effects to rationalize its traditional medicinal use. The present study aimed to investigate the antispasmodic activity of Origanum species with the organ bath. Methods: Rats were divided into 5 groups. While no treatment was given to the control group, plant extracts were given to other groups. Ileal tissues taken by rats were used for evaluating the contraction responses elicited with potassium chloride (KCl) and acetylcholine (ACh). Thereafter, the extracts of Origanum species were applied and cumulative concentrationresponse curves of these species were constructed in each experiment. Results: All treatments with Origanum species have a relaxation effect on rat ileum as compared with the control group. According to the results of the isolated organ bath study, KCl and ACh-induced ileum contraction were significantly decreased by all Origanum species. Conclusion: Origanum species that were used in the present study can prevent smooth muscle contraction of ileum, and therefore they can be used to reduce intestinal spasms.

Progesterone-loaded poly(lactic) acid fibrous polymeric patches were produced using electrospinning and pressurized gyration for infra-vaginal application to prevent preterm birth. The patches were intravaginally inserted into rats in the final week of their pregnancy, equivalent to the third trimester of human pregnancy. Maintenance tocolysis with progesterone-loaded patches was elucidated by recording the contractile response of uterine smooth muscle to noradrenaline in pregnant rats. Both progesterone-loaded patches indicated similar results from release and thermal studies, however, patches obtained by electrospinning had smaller average diameters and more uniform dispersion compared to pressurized gyration. Patches obtained by pressurized gyration had better results in production yield and tensile strength than electrospinning; thereby pressurized gyration is better suited for scaled-up production. The patches did not affect cell attachment, viability, and proliferation on Vero cells negatively. Consequently, progesterone-loaded patches are a novel and successful treatment strategy for preventing preterm birth.

In order to provide more effective treatment strategies for the rapid healing of diabetic wounds, novel therapeutic approaches need to be developed. The therapeutic potential of peroxisome proliferator-activated receptor-γ (PPAR-γ) agonist pioglitazone hydrochloride (PHR) in two different release kinetic scenarios, burst release and sustained release, were investigated and compared with in vitro and in vivo tests as potential wound healing dressings. PHR-loaded fibrous mats were successfully fabricated using polyvinyl pyrrolidone and polycaprolactone by scalable pressurized gyration. The results indicated that PHR-loaded fibrous mats expedited diabetic wound healing in type-1 diabetic rats and did not show any cytotoxic effect on NIH/3T3 (mouse embryo fibroblast) cells, albeit with different release kinetics and efficacies. The wound healing effects of fibrous mats are presented with histological and biochemical evaluations. PHR-loaded fibrous mats improved neutrophil infiltration, oedema, and inflammation and increased epidermal regeneration and fibroblast proliferation but the formation of hair follicles and completely improved oedema were observed only in the sustained release form. Thus, topical administration of PPAR-γ agonist in sustained release form has high potential for the treatment of diabetic wounds in inflammatory and proliferative phases of healing with high bioavailability and fewer systemic side effects.

Abstract Title: The inhibitory effects of Salvia triloba and Thymus praecox on acetylcholinesterase activity in diabetic ratsBackgroundDiabetes mellitus (DM) is a metabolic disease characterized by long-term complications including cerebrovascular injury and cognitive disorders. Acetylcholinesterase (AChE) which is involved in numerous pathways in the central nervous system regulates the level of acetylcholine (ACh) which plays vital functions such as memory, learning, modulation of cerebral blood flow, movement control, neurotransmission as well (1). Recent studies have shown that hypoinsulinemia and insulin resistance is the reason of the decreased level of ACh and contribute the possible biochemical link between DM and cognitive disorders including Alzheimeru2019s disease. Studies with plants have shed light on the correction of cognitive functions of diabetes mellitus with increased AChE activity. Some Salvia and Thymus species of the Lamiaceae family have antidiabetic effects (2). There is no study on antidiabetic activity of Salvia triloba and Thymus praecox.AimTo investigate the effects of Salvia triloba and Thymus praecox on brain acetylcholinesterase activities in diabetes mellitus. With the help of obtained results, further studies will be carried out for ameliorating cognitive dysfunction effectively and also supporting current treatments.MethodThe rats were divided into five groups (6 rats per group): Group-I: Normal control, Group-II: Diabetic control, Group-III: Treatment with Salvia triloba methanolic extract, (200 mg/kg/day, i.g.), Group-IV: Treatment with Thymus praecox methanolic extract, (100mg/kg/day, i.g.), Group-V: Treatment with Metformin (400 mg/kg/day, i.g.). Type 2 DM was induced experimentally in these groups of rats by the intraperitoneal administration of 55 mg/kg of STZ and 100 mg/kg nicotinamide, except control group. Treatments were carried out after induction of DM and lasted for 3 weeks except decapitation day. The AChE enzymatic assay was determined according to the method of Ellman et al. The reaction mixture (2 mL final volume) contained 100 mM K+-phosphate buffer, pH 7.5 and 1 mM 5,50-dithiobisnitrobenzoic acid (DTNB). The method is based on the formation of the yellow anion, 5, 50- dithio-bis-acid-nitrobenzoic, measured by absorbance at 412 nm during 2 min incubation at 25u00b0C. The enzyme (40u201350 mg of protein) was pre-incubated for 2 min. The reaction was initiated by adding 0.8 mM acetylthiocholine iodide (AcSCh). All samples were in triplicate readings and the enzyme activities were expressed in mmol AcSCh/h/mg of protein.ResultsThymus praecox and Salvia triloba in methanolic extract considerably decreased (pu02c20.0001) blood glucose levels compared to diabetic rats and performed this drop for 3 weeks. Thymus praecox extract reached its maximum hypoglycemic effect (141.83u00b17.31, pu02c20.0001) in 2 weeks. At the same time, Thymus praecox and Salvia triloba extract also showed strong hypoglycemic effect (164.83u00b113.30, pu02c20.0001). The diabetic group exhibited a significant increase (pu02c20.001) in AChE activity in prefrontal cortex compared to the control and the treatment groups. However Salvia triloba extract and Thymus praecox extract reverted this increase (pu02c20.001) in AChE activity induced by diabetes after 3 weeks of treatment. The metformin group decreased (%47, pu02c20.001) in AChE activity compared to diabetic groups. Salvia triloba extract (%37, pu02c20.001) and Thymus praecox extract group (%41, pu02c20.001) a considerably decrease in AChE activity compared to diabetic group. The metformin group did not show a significant difference in enzyme activity compared to the control group. However, Salvia triloba and Thymus praecox increased (pu02c20.05) in AChE activity compared to control groups.DiscussionOur study results showed that an increase in AChE activity in type 2 diabetic rat brains. This increase in AChE activity in the T2DM rat model can be linked to depletion in cholinergic actions leading to defective neurotransmission and cognitive dysfunction as a result of decreased levels of ACh in the synaptic cleft. We showed that the reestablishment of AChE activity by Salvia triloba extract and Thymus praecox extract which for the first time demonstrated antidiabetic activities can contribute to the maintenance of cholinergic signaling in diabetic rats. In the light of the results, these plants give a valuable direction for researchers on the future for diabetes-related cognitive disorders. 1. Jacobson AM., et al., Diabetes Control and Complications Trial/Epidemiology of Diabetes Interventions and Complications Study Research Group, Long-term effect of diabetes and its treatment on cognitive function. N Engl J Med. 2007;356(18):1842u20131852.2. Davids D., et al., Ethnobotanical survey of medicinal plants used to manage High Blood Pressure and Type 2 Diabetes Mellitus in Bitterfontein, Western Cape Province, South Africa, J Ethnopharmacol. 2016 Dec 24;194:755-766.

Timing of tourniquet release after extremity operations is a subject of controversy. Some surgeons maintain the tourniquet inflated while closing the wound and release it after applying a compressive bandage. Other group of surgeons release the tourniquet before wound closure and perform hemostasis, then close the wound and apply compressive bandage. The difference between these two methods was investigated on both hind limbs of 18 rabbits after standardized operations, regarding the postoperative hematoma formation. Total tourniquet time and the procedure performed were identical on both sides except for the method of tourniquet deflation. Red blood cells of all animals were labeled with Tc-99m at the end of the procedure and after one hour allowed for hematoma formation under anesthesia all animals were sacrificed by a lethal injection. Scans were obtained after sacrification and hematomas on both sides were viewed and measured for qualitative and quantitative comparison. Qualitatively more label was observed in the leg whose tourniquet was released after wound closure in 12 of 18 animals, in the other leg in 4 animals, while no difference between two sides was observed in 2 animals (K, Turnike kullanılan ekstremite ameliyatlarında turnikenin açılma zamanlaması konusunda farklı uygulama-lar vardır. Bu deneysel çalışmada, cerrahi işlemin sonunda turnikenin açılıp kanama kontrolü yapılması ve bunu takiben yaranın kapatılarak kompresif bandaj uygulanması ile önce yaranın koparılıp kompresif bandaj uygulanıp sonra turnikenin açılması arasında postoperatif hematom oluşumu açısından farklılık olup olmadı-ğı araştırılmıştır. Onsekiz adet tavşanın her iki alt ekstremitelerinde pnömatik turnike altında gerçekleştirilen aynı standard cerrahi uygulama sonrasında bir tarafta cerrahi işlemin biçiminde yara kapatılmadan önce tur-nike açılarak 2.5X büyütme altında kanama kontrolü yapılmış ve daha sonra yara kapatılarak kompresif bandaj uygulanmıştır. Diğer tarafta ise önce yara kapatılmış, kompresif bandaj uygulanmış ve sonra turnike gevşetilmistir. Tüm hayvanların eritrositleri Tc-99m ile işaretlenerek operasyon sonrasındaki 1 saatlik dönem içerisinde oluşmuş olan hematomlar, hayvanlar sakrifiye edildikten sonra sintilasyon kamerası altında saptanarak, kalitatif ve kantitatif olarak karşılaştırılmışlardır. Kalitatif değerlendirmede 18 hayvandan 12'sinde yara kapatılmadan önce turnike gevşetilerek kanama kontrolü yapılan ekstremitede oluşan hematom diğer ekstremitede oluşandan daha küçük bulunmuşlar. Dört hayvanda diğer tarafta oluşanı hematom daha küçük iken iki hayvanda ise taraflar arasındaki bulunmamıştır. İstatistiksel incelemede iki taraf arasında ters bir uyum gözlenmiştir (k

Replacement of the resected bone after wide local resection in the treatment of malignant tumors is a challenging surgical problem. Reimplantation of resected and autoclaved bone is a well known procedure for reconstruction. The use of autoclaved graft is limited because of its drawbacks such as delayed union, nonunion and infection. We investigated the effect of hyperbaric oxygen therapy (HBO) on incorporation of autoclaved bone. In 60 Wistar Rat, 5-7 mm left tibial segment was resected under anesthesia. In each animal, defect was reconstructed by reinserting the resected segment after autoclaving (121 C¡ / 20 minutes) with intramedullary Kirschner wire fixation. While half the animals had HBO therapy after operation, the other half were left at standart temperature and pressure (STP). Incorporation of the grafts were studied at 15, 45 and 90 days after surgery radiographically, scintigraphically and histopathologically. We concluded that HBO therapy improves incorporatİon of autoclaved autologous bone in the light of statistical methods., Malign kemik tümörlerinin lokal reaksiyon ile tedavi edilmeleri sırasında oluşan büyük kemik defektlerinin rekonstrüksiyonu önemli bir problemdir. Bu amaçla oroklavize otojen kemik greftleri de kullanılmaktadır. Fakat geç kaynama ve kaynamama, enfeksiyon gibi dezavantajları nedeniyle kullanımları sınırlıdır. Biz bu çalışmamada hiperbarik oksijen (HBO) uygulamasının greftin inkorporasyonunu nasıl etkilediğini araştırdık. Bu amaçla 60 adet Wistar cinsi fare 30'luk iki gruba ayrıldı. Tibia diafizinden çıkarılan 5-7 mm'lik segmentler otoklavize edilerek reimplante edildi. Deney grubuna HBO uygulanırken kontrol grubuna HBO uygulaması yapılmadı. 15, 45 ve 90 günlük takipler sonunda fareler sakrifiye edilerek radyolojik, sintigrafik ve histopatolojik olarak karşılaştırıldı. Sonuç olarak her üç parametrede HBO uygulamasının greftin kaynamasını hızlandırdığını gösterdi.

In this study the therapoetic effects of chard (Beta vulgaris L. var. cicla) aganist erectile function and cardiovascular parameters in diabetic rats were investigated. Sprague Dawley rats were divided into sham-operated or 65 mg/kg STZ diabetic groups, in which rats recieved either per oral chard extract (2 g/kg) or s.c. insulin (6U/kg/day) starting on by the 15’th day of the diabetes for 45 days. Blood pressure and intracavernosal pressure recording and echocardiographic imaging were made to evaluate erectile and cardiovascular functions. At the end of the 8’th week, the animals were decapiated and blood and tissue (heart, aort, corpus cavenosum) samples were taken. Diabetes mellitus caused a decrease in left ventricular function but had no effect on blood pressure and intracavernosal pressure. Diabetes mellitus also decreased GSH levels, increased MDA levels in the heart, aort and corpus cavernosum tissues, indicating the presence of oxidative tissue damage in peripheral target tissues. Furthermore, elevated cGMP, NO, luminol, lucigenin levels were determined in the tissue. In addition, ADMA, NO2-/NO3- and LDH levels were increased in serum samples. On the other hand, 45 days-treatment with chard extract reversed all the measured parameters, ameloriated the diabetes-induced oxidative injury in the target organs and improved cardiac functions.Anahtar Kelimeler : Diabetes mellitus, oxidative stress, chard (Beta vulgaris L.var. cicla), intracavernosal pressure, echocardiographi, rat

Objective: RNAi is a powerful tool for controlling cellular processes in the gene silencing and in the analysis of molecular mechanisms for many diseases including cancer. VEGF signaling is a potential therapeutic target for siRNA delivery in breast cancer. Although siRNA can be potential therapeutic agent for various diseases, intracellular delivery of siRNA is one of the major hurdles to turn siRNA into therapeutically active molecules. To date, numerous transfection methods or delivery systems have been developed. Among them, chitosan is potential gene carrier due to its characteristics such as biodegradability, biocompatibility, non immunogenic and toxicity. The purpose of this study was to investigate the biodistribution and tumor localization of chitosan/ VEGF siRNA complexes in breast cancer model of rat.Method: In our study, we intravenously injected FITC labeled naked siRNA-VEGF (40 µg/rat) and chitosan/FITC labeled siRNAVEGF complexes (40 µg/rat) to breast tumor-bearing rats.Results: While the biodistribution of chitosan/siVEGF complexes to the brain and heart appeared almost similar to that observed for naked siVEGF, the accumulation was slightly lower in the spleen, liver, lungs, muscle and higher in the kidney. In the breast tumor tissue, chitosan/FITC-labeled VEGF siRNA complexes were localized in the tumor 15 min post-injection but naked FITCsiVEGF did not localize in tumor tissue.Conclusion: In this preliminary study, we revealed the promising potential of chitosan as VEGF siRNA delivery system for biodistribution. Key words: siRNA, VEGF, chitosan, biodistribution, breast cancer, Amaç: RNAi kanser dahil olmak üzere birçok hastalığın moleküler mekanizmasının analizinde ve gen susturulmasında hücresel proseslerin kontrolü için önemli bir araçtır. VEGF sinyali meme kanserinde siRNA taşınmasında önemli bir hedeftir. siRNA farklı hastalıklar için potansiyel bir ajan olmasına rağmen, siRNA’nın intrasellüler taşınması, terapötik olarak aktif bir moleküle dönüşmesindeki önemli engellerden biridir. Bugüne kadar birçok transfeksiyon yöntemi ve taşıyıcı sistem geliştirilmiştir. Bunlar arasında kitozan, biyouyumlu, biyoparçalanabilir olması, toksik ve immunojenik olmaması gibi özellikleri nedeniyle önemli bir gen taşıyıcısıdır. Bu çalışmanın amacı, meme kanserinde kitozan/VEGF-siRNA komplekslerinin tümör lokalizasyonunu ve biyodağılımını araştırmaktır.Yöntem: Çalışmamızda meme tümörü taşıyan sıçanlara serbest FITC-işaretli siVEGF (40 µg/sıçan) ve kitozan/ FITC-işaretli siVEGF (40 µg/sıçan) kompleksleri intravenöz olarak enjekte edildi.Bulgular: Kitozan/siVEGF komplekslerinin beyin ve kalbe biyodağılımı, serbest siVEGF ile hemen hemen benzerken, dalak, karaciğer, akciğer ve kasta biraz daha düşük ve böbrekte ise biraz daha yüksektir. Meme tümör dokusunda, kompleksler enjeksiyon sonrası 15 dakikada tümörde lokalize iken, serbest FITC-siVEGF tümör dokusunda lokalize değildir.Sonuç: Bu ön çalışmada, biz biyodağılım için VEGF siRNA taşıyıcı sistem olarak kitozanın umut verici olduğunu gösterdik. Anahtar Kelimeler: siRNA, VEGF, kitozan, biyodağılım, meme kanseri

Recent studies have suggested that positron emission tomography (PET) imaging with Ga-68-labelled DOTA-somatostatin analogues (SST) like octreotide and octreotate is useful in diagnosing neuroendocrine tumours (NETs) and has superior value over both CT and planar and single photon emission computed tomography (SPECT) somatostatin receptor scintigraphy (SRS). The aim of the present study was to evaluate the role of Ga-68-DOTA-1-NaI3-octreotide (Ga-68-DOTANOC) in patients with SST receptor-expressing tumours and to compare the results of Ga-68-DOTA-D-Phe(1)-Tyr(3)-octreotate (Ga-68-DOTATATE) in the same patient population.

Introduction: Lack of correlation between in vitro and in vivo stability is a general problem for the development of radiopeptides especially in the case of minigastrin derivatives for therapeutic applications. In this study, we compared the influence of experimental conditions on radiopeptide stability results in vitro using a model Minigastrin (MG) analogue labelled with Lu-177. Additionally, we attempted to characterize the main serum enzymatic cleavage sites by matrix-assisted laser desorption/ionization (MALDI) time-of-flight (TOF) mass spectrometry (MS) analysis.

ÖZET Opioidler muhtelif beyin bölgelerindeki ve omurilikteki u., S ve k olarak isimlendirilen üç temel reseptörleri aracılığıyla ağrı uyarısını önlerler. Tolerans ve bağımlılık oluşturmaları onların klinik kullanımını kısıtlamaktadır. Bazı çalışmalarda tolerans ve bağımlılıkta opioid reseptörlerinin sayı ve afînitesindeki değişikliklerin etkili olduğu ileri sürülmektedir. Öte yandan son zamanlarda Nitrik Oksit (NO) 'in opioid toleransı ve bağımlılığında önemli rolü olduğu hipotezi desteklenmekte ve de akut morfin uygulamasının NO sentaz (NOS) aktivitesini stimüle ettiği ileri sürülmektedir. Son yıllarda NOS înhibitörleri (NOSİ)'nin morfine tolerans ve bağımlılık gelişimini ve de morfin yoksunluk sendromunun temel bazı belirtilerini inhibe ettiği bildirilmiştir. Bunun yanısıra, NO pekçok proteinin S-nitrozilasyonunu uyarabilir. NO tarafından proteinlerin ve reseptörlerin nitrozilasyonları onları inhibe eder. Bu bulgular NO 'nun morfine tolerans ve bağımlılık gelişiminde reseptör bağlanmasını modüle edebileceğini düşündürmektedir. Çalışmamızda, sıçanlar 4 gruba ayrıldı. 11 gün boyunca 1. gruba serum fizyolojik, 2. gruba L-Nitro Arjinin (4 mg/kg/gün) (kontrol grupları), 3. gruba Morfin (gün aşırı artan dozlarda), 4. gruba da morfin + L-Nitro Arjinin uygulandı. Sıçanların beyin ve omurilik membranlarındaki fi, 8 ve k opioid reseptörlerinin sayı ve afinitelerini tespit etmek amacıyla saturasyon deneylerinde sırasıyla [3H]-DAGO (1-30 nM), [3H]-Ile5

ÖZET EC, Tc-99m ile oda sıcaklığında kolayca bağlanabilen, renal klirensinin MAG3'den daha iyi olduğu öne sürülen, yeni bir renal farmasötiktir. Bu çalışma, EC'nin farmakokinetik özelliklerini, çeşitli böbrek hastalıklarında incelemek ve OIH ve MAG3 ile karşılaştırmak amacıyla yapıldı. Bu amaçla, 11 hastada, EC, OIH ve MAG3, sürekli infüzyon yöntemi kullanılarak incelendi. Hastalara, 100 MBq EC veya MAG3 ile birlikte 7.4 MBq OIH, intravenöz bolus verildikten sonra, 30 ml/saat gidecek şekilde 180 dk. süreyle infüzyon yapıldı. Bu süre içerisinde, karşı koldan 16 kan örneği alındı. Aynı zamanda, serbest işeme ile 5 idrar örneği alınarak biriktirildi. 20. dk. kan örneklerinden plazma protein bağlanma ve eritrosit bağlanma oranlarına bakıldı. EC, OIH ve MAG3'ün renal klirensleri, sırasıyla, 245±106, 346±134 ve 192±95 ml/dk/1.73m2 olarak bulundu. EC/OIH ve MAG3/OIH oranlan ise, sırasıyla 0.75±0.06 ve 0.55±0.12 olarak hesaplandı. Tüm vücut klirensleri EC, MAG3 ve OIH için sırasıyla, 236±118, 334±153 ve 173±106 ml/dk/1.73m2 bulundu. EC ve MAG3'ün tüm vücut klirenslerinin OIH'na oram, sırasıyla 0.76±0.13 ve 0.53±0.06 hesaplandı. ECnin dağılım volümü (15722±7646), MAG3'ün dağılun volümünden (9509±4153) belirgin olarak yüksek, OIHın dağılmı volümüne ise (17104Ü0626) yakın değerde bulundu. EC/OIH ve MAG3/OIH dağılım volüm oranlan sırasıyla 1.03±0.18 ve 0.55±0.13 idi. Her 3 radyofarmasötiğin 60. dk ekskresyon oranlan ise birbirine yakın bulundu ( EC, MAG3 ve OIH için sırasıyla, 0.54±0.21, 0.50±0.21 ve 0.57±0.17). ECnin plazma protein bağlanma oram, OIHdan belirgin yüksek bulundu (0.34±0.09 ve 0.66±0. 12). 20. dk. eritrosit bağlanma oranı ise, EC için çok düşük bulundu. Bu değer EC ve OIH için sırasıyla %3 ve %27 olarak bulundu. Az sayıda hasta üzerinde yapılan bu çalışmada ECnin farmakokinetik özellilerinin, MAG3'den daha iyi olduğu sonucuna vanldı. Bu nedenle, renal fonksiyon çalışmalannda, ve ERPF hesaplamasında, OIHna MAG3'den daha iyi bir alternatif olduğu sonucuna varıldı. 25 29