Medical Radiological Scientific Center

Obninsk, Russia

Medical Radiological Scientific Center

Obninsk, Russia
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Plotnikova E.D.,Moscow State University | Nurieva E.V.,Moscow State University | Onufriev M.V.,Russian Academy of Sciences | Gulyaeva N.V.,Russian Academy of Sciences | And 4 more authors.
Russian Journal of Organic Chemistry | Year: 2013

iNOS-Inhibitor activity of 3-imino-2,4-diazabicyclo[3.3.1]nonan-1-ol hydrochloride was predicted basing on molecular modeling and was confirmed by experiments in vitro. The results of the study by XRD analysis of the molecular and crystal structure of this compound are reported. © 2013 Pleiades Publishing, Ltd.


Petriev V.M.,Medical Radiological Scientific Center | Siruk O.V.,Medical Radiological Scientific Center | Bryukhanova A.A.,Medical Radiological Scientific Center | Smoryzanova O.A.,Medical Radiological Scientific Center | Skvortsov V.G.,Medical Radiological Scientific Center
Pharmaceutical Chemistry Journal | Year: 2014

Studies of the pharmacokinetics of 188Re-human serum albumin microspheres (MSA) of diameter 10 – 20 μm in intact mice showed that the maximum accumulation of activity (about 70%) 5 min at after intravenous administration was in the lungs. Elimination of activity from the lungs over the period 5 min to 3 h was about 7%. Over a period of 72 h, the quantity of 188Re-MSA in the lungs decreased approximately twofold. Prolonged retention of 188Re-MSA in the lungs could be explained in terms of the high stability of the chemical bond between 188Re and MSA. This was confirmed in control experiments of the pharmacokinetics of free 188Re as Na188ReO4. Results on the pharmacokinetic characteristics of 188Re-MSA provided evidence that this material may be useful for the radionuclide therapy of tumors in different locations after intravascular administration. © 2014, Springer Science+Business Media New York.


Petriev V.M.,Medical Radiological Scientific Center | Tishchenko V.K.,Medical Radiological Scientific Center | Siruk O.V.,Medical Radiological Scientific Center | Smoryzanova O.A.,Medical Radiological Scientific Center | Skvortsov V.G.,Medical Radiological Scientific Center
Pharmaceutical Chemistry Journal | Year: 2014

The pharmacokinetic properties of a bone-seeking radiopharmaceutical based on pentaphosphonic acid labeled with technetium-99m (99mTc-PPA) were investigated. The experiments were performed in healthy rats and in rats with a femoral bone-fracture (BF) model. The radiopharmaceutical was injected into a tail vein 14 days after the fracture. 99mTc-PPA showed good stability in vivo because it accumulated in the thyroid less than unlabeled 99mTc. The maximum accumulation of 99mTc-PPA was found in bones tissue, where it reached 1.48 ± 0.19% of injected dose per gram of tissue at 1 h after injection. The drug exhibited rapid blood clearance, showed minimum uptake into soft organs and tissues, and was excreted mainly via renal pathways. The presence of femoral BF significantly changed the biodistribution of99mTc-PPA in soft organs and tissues. The 99mTc-PPA content in BF was 1.9-2.5 times higher than in healthy femur and 2-3 times higher than in skeleton. The concentration of 99mTc-PPA in other soft organs and tissues of rats with bone lesion was lower than in organs and tissues of healthy rats. The maximum BF-to-blood and BF-to-muscle ratios were 184.8 ± 14.1 and 415.4 + 59.5, respectively, 3 h after injection. The results showed that 99mTc-PPA had favorable properties for diagnosing bone-tissue metastases. © 2014 Springer Science+Business Media New York.


Petriev V.M.,Medical Radiological Scientific Center | Podgorodnichenko V.K.,Medical Radiological Scientific Center | Smoryzanova O.A.,Medical Radiological Scientific Center | Skvortsov V.G.,Medical Radiological Scientific Center
Pharmaceutical Chemistry Journal | Year: 2013

The pharmacokinetics of 225Ac-labeled hydroxyethylenediphosphoric acid monopotassium salt (225Ac-KHEDP) and 225AcCl3 were studied in intact mice after intravenous administration. The results obtained here showed that in contrast to free 225Ac, 225Ac-KHEDP was rapidly eliminated from the body. Asmall proportion of 225Ac is probably cleaved from KHEDP and is taken up by the liver and bone tissue, with kinetics similar to those of 225Ac. The accumulation of 225Ac-KHEDP in most soft organs and tissues was statistically significantly lower than that of unbound 225Ac. The tropism of 225AcCl3 for bone tissue was greater than that of 225Ac-KHEDP. The high level of activity in bones persisted throughout the study period (10 days). © 2013 Springer Science+Business Media New York.


Tishchenko V.K.,Medical Radiological Scientific Center | Petriev V.M.,Medical Radiological Scientific Center | Skvortsov V.G.,Medical Radiological Scientific Center
Pharmaceutical Chemistry Journal | Year: 2015

This review presents results on the pharmacokinetic characteristics of osteotropic radiopharmaceuticals (RP) based on polyaminophosphonic acids labeled with various radionuclides. The greatest number of studies cited in the scientific literature address ethylenediaminetetramethylenephosphonic (EDTMP), propylenediaminetetramethylenephosphonic (PDTMP), diethylenetriaminepentakis(methylphosphonic) (PPA), triethylenetetraminohexamethylenephosphonic (TTHMP), 1,4,7,10-tetraazacyclododecan-1,4,7,10-tetramethylenephosphonic (DOTMP) and other acids. RP based on these have high stability in vitro and in vivo, with selective accumulation in bone tissue, and are excreted mainly via the kidneys. This review also presents data on a wide spectrum of radionuclides used to label the various phosphonic acids. These include radionuclides used in radionuclide diagnosis (99mTc, 68Ga) and radionuclide therapy - γ emitters: 153Sm, 188Re, 177Lu, 170Tm, 166Ho, and others, and α emitters: 227Th, 228Ac, and 212Bi. © 2015, Springer Science+Business Media New York.


Osipov A.N.,RAS Semenov Institute of Chemical Physics | Ryabchenko N.I.,Medical Radiological Scientific Center | Ivannik B.P.,Medical Radiological Scientific Center | Ryabchenko V.I.,Medical Radiological Scientific Center
Biophysics | Year: 2011

The effect of combined action of cadmium chloride at a dose of 0.5 mg/kg of body weight and γ-radiation of 1 Gy on induction of DNA damage in thymocytes and the total number of cells in the thymus of mice was studied. We found that injection of CdCl2 0.5 h prior to irradiation decreased the number of single-strand DNA breaks and the number of alkali-labile sites in thymocytes 48 h after irradiation as compared to the γ-radiation effect only. This effect was associated with a strong decrease in the total number of thymocytes in this organ as compared to the action of cadmium ions and γ radiation separately. This masked the general genotoxic effect of combined treatment and created an illusion of a radioprotective effect of cadmium ions. Injection of cadmium chloride into mice 24 h prior to irradiation was followed by an additive increase in the number of the single-strand DNA breaks and the number of alkali-labile sites in thymocytes as compared to the respective controls such as the separate effects of cadmium ions and irradiation. We revealed a simultaneous decrease in the part of DNA tightly bound to proteins, i. e., DNA-protein cross-links as compared to the effect of γ-radiation only. We did not observe any statistically significant changes in the total number of thymocytes as compared to the separate effects of cadmium ions and irradiation. Thus, our data show that exposure of murine thymocytes to combined action of cadmium ions and γ-radiation at the doses and with the methods of treatment used induced additive effects but not antagonistic effects or protection against radiation. © 2011 Pleiades Publishing, Ltd.


Kryshtal G.V.,RAS N. D. Zelinsky Institute of Organic Chemistry | Zhdankina G.M.,RAS N. D. Zelinsky Institute of Organic Chemistry | Konoplyannikov A.G.,Medical Radiological Scientific Center | Tartakovsky V.A.,RAS N. D. Zelinsky Institute of Organic Chemistry | And 5 more authors.
Russian Chemical Bulletin | Year: 2012

Novel synthetic approaches towards analogs of methaprogerol, the efficient wound healing drug, were developed. Several hitherto unknown compounds obtained exhibited in vivo activity similar to methaprogerol. 2-(3-Dimethylaminopropyl)- 5-methylhex-4-enoic acid enhanced the efficacy of the treatment of diseases of various etiologies and different organ injuries by transplantation of mesenchymal stem cells (MSC) and MSC-derived cardiomyoblasts. © 2012 Springer Science+Business Media New York.


Orlova M.A.,Moscow State University | Trofimova T.P.,Moscow State University | Filimonova M.V.,Medical Radiological Scientific Center | Proshin A.N.,Russian Academy of Sciences | Zaitsev D.A.,Moscow State University
Russian Chemical Bulletin | Year: 2013

The effector activity of thiazine and thiourea derivatives towards various forms of NO-synthase (NOS) in vitro and ex vivo was compared with their cytotoxic effect on human lymphocytes and leukemic cells. A thiazine derivative was revealed that exhibits a selective effect only on malignant cells and is an inhibitor of inducible and neuronal NOS. © 2013 Springer Science+Business Media New York.


Lychagin A.A.,Medical Radiological Scientific Center
Biomedical Engineering | Year: 2014

Portable neutron generators developed at the All-Russian Scientific Research Institute of Automatics (Moscow) and their potential applications for radiobiological experiments and therapy are considered. Experience in the use of such generators at the Medical Radiological Scientific Center, Ministry of Health of Russian Federation, is reviewed. © 2014 Springer Science+Business Media New York.


Skoropad V.Yu.,Medical Radiological Scientific Center | Berdov B.A.,Medical Radiological Scientific Center | Rukhadze G.O.,Medical Radiological Scientific Center
Voprosy Onkologii | Year: 2012

There were analyzed patterns of polyneoplasia development in radically operated gastric cancer patients. The second tumors were revealed in 99 of 1255 patients (7,9%) as soon as patients with early gastric cancer manifested primary-multiple malignant tumors almost two times more (15,4%). Among second tumors there were predominantly tumors of the colon, urinogenital system, head and neck and also lymphoproliferative diseases. Along with tumors prior to the diagnosis "gastric cancer" there were met mostly lymphoproliferative diseases and breast cancer; of synchronous - cancer of the colon and bladder; among exposed after treatment of gastric cancer - cancer of the colon, pancreas, and skin. Radical surgery because of the second tumor was provided to 77,6% patients, palliative surgery - to 12,6%. In the treatment of second tumors there were most commonly used surgical technique - in 40 (39%) patients, radiotherapy ± chemotherapy - in 27 (26%), the combined method (surgery+radiotherapy/ chemotherapy) - in 22 (21%). Second tumors (both synchronous and metachronous) were the main cause of death of patients. Thus, the occurrence of a second tumor in patients with gastric cancer is constantly increasing the frequency of the event, with the possibility of early detection and curative treatment of synchronous and especially metachronous tumors determine the prognosis in this group of patients. Primary tumor multiplicity is not a contraindication both to a radical, including combined, and palliative treatment of each of the tumors.

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