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    Wyświetlanie 1-13 z 13
    Tytuł:
    Biodistribution of doxorubicin-loaded succinoyl chitosan nanoparticles in mice injected via intravenous or intranasal routes
    Autorzy:
    Zubareva, Anastasia
    Shcherbinina, Tatyana
    Varlamov, Valery P.
    Svirshchevskaya, Elena
    Powiązania:
    https://bibliotekanauki.pl/articles/1035197.pdf
    Data publikacji:
    2014
    Wydawca:
    Sieć Badawcza Łukasiewicz - Polskie Towarzystwo Chitynowe
    Tematy:
    biodistribution
    doxorubicin
    succinoyl chitosan nanoparticles
    Opis:
    Chitosan (Chi) is an extremely promising natural biopolymer with remarkable potency for the development of drug and vaccine delivery nanosystems. Various Chi derivatives are used to form nanoparticles (NPs) with unique properties. However, the efficacy of the therapy delivered by Chi NPs depends significantly on NP biodistribution in the body. The aim of this study was the analysis of biodistribution of NPs formed by succinoyl Chi and loaded with doxorubicin (SCNPDOX). We compared the distribution of free DOX and SCNP-DOX after intravenous (i.v.) and intranasal (i.n.) delivery into tumour-bearing mice. Distribution of DOX and SCNP-DOX was comparable after i.v. injection while they differed significantly after i.n. instillation.
    Źródło:
    Progress on Chemistry and Application of Chitin and its Derivatives; 2014, 19; 145-154
    1896-5644
    Pojawia się w:
    Progress on Chemistry and Application of Chitin and its Derivatives
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Biological evaluation of [18F]-nifedipine as a novel PET tracer for L-type calcium channel imaging
    Autorzy:
    Sadeghpour, H.
    Jalilian, A. R.
    Akhlaghi, M.
    Shafiee, A.
    Mirzaii, M.
    Miri, R.
    Saddadi, F.
    Powiązania:
    https://bibliotekanauki.pl/articles/147732.pdf
    Data publikacji:
    2008
    Wydawca:
    Instytut Chemii i Techniki Jądrowej
    Tematy:
    dihydropyridines
    flourine-18
    PET
    biodistribution
    Opis:
    Due to interesting role of dihydropyridines in cardiovascular diseases and drug resistance studies and lack of a fluorine-18 labeled imaging agent for L-type calcium channel studies, this study was designed. [18F]Dimethyl 2-(fluoromethyl)-6-methyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate 2 was prepared in no-carrier-added (n.c.a.) form from a starting brominated compound in one step at 80°C in Kryptofix2.2.2/[18F]. Compound 2 was administered to normal rats via their tail veins for preliminary biodistribution studies and the ID/g% of the labeled compound was determined up to 3 h post injections. Coincidence images were obtained in rats 5 to 120 min. Radiofluorination on bromo precursor gave a fluorinated compound in 95% radiochemical purity and a 8% yield shown by RTLC and HPLC. Biodistribution studies showed that the tracer is accumulated in the heart in the first few minutes, followed by metabolism resulting in very soluble 18F-containing metabolites eliminated through the urinary tract. In coincidence images, the target organ was shown to be the heart. Lung had high accumulation possibly due to the presence of Ca2+ channels and/or hydrolyzing enzymes showing a significant myocardial uptake at 120 min. The data demonstrates a significant agreement with the reported L-type calcium channels throughout the animal body. To our knowledge, this is the first example of 18F-DHPs in the literature.
    Źródło:
    Nukleonika; 2008, 53, 4; 151-154
    0029-5922
    1508-5791
    Pojawia się w:
    Nukleonika
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Development of 62Zn bleomycin as a possible PET tracer
    Autorzy:
    Jalilian, A.
    Fateh, B.
    Ghergherehchi, M.
    Karimian, A.
    Moradkhani, S.
    Kamali-Dehghan, M.
    Tabeie, F.
    Powiązania:
    https://bibliotekanauki.pl/articles/148678.pdf
    Data publikacji:
    2005
    Wydawca:
    Instytut Chemii i Techniki Jądrowej
    Tematy:
    PET
    pharmacokinetics
    biodistribution
    62Zn
    bleomycin
    Opis:
    Abstract Bleomycin (BLM), labeled with radioisotopes, is widely used in therapy and diagnosis. In this study, BLM was labeled with 62Zn for oncologic PET studies. The complex was obtained at pH = 2 in saline at 90°C in 25 min. Radio-TLC showed an overall radiochemical yield of 95 97% (radiochemical purity > 97%). Stability of complex was checked in vitro in mice and human plasma/urine. Preliminary in vivo studies were performed to determine complex stability and distribution of 62Zn BLM in normal and fibrosarcoma-bearing mice. 62Zn BLM accumulated significantly in induced fibrosarcoma tumors in mice according to biodistribution/imaging studies. 62Zn BLM can be used in PET oncology studies due to its suitable physicochemical properties as a diagnostic complex in vitro and in vivo. Further studies should be performed for evaluation of the complex behavior in larger mammals.
    Źródło:
    Nukleonika; 2005, 50, 4; 143-148
    0029-5922
    1508-5791
    Pojawia się w:
    Nukleonika
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Development of a radiolabeled glucagon compound for imaging
    Autorzy:
    Jalilian, A. R.
    Jouiaei, M.
    Doroudi, A. R.
    Bolourinovin, F.
    Garousi, J.
    Powiązania:
    https://bibliotekanauki.pl/articles/148402.pdf
    Data publikacji:
    2010
    Wydawca:
    Instytut Chemii i Techniki Jądrowej
    Tematy:
    glucagons
    radiolabeling
    biodistribution
    Ga-67
    Opis:
    In order to develop a possible Ga-labeled glucagon (GCG) compound for imaging studies, biosynthetic glucagon (GCG) was labeled with [67Ga]-gallium chloride after conjugation with freshly prepared diethylenetriaminepentaacetic acid dianhydride (ccDTPA). After solid phase purification of the radiolabeled hormone, high performance liquid chromatography (HPLC) and instant thin-layer chromatography (ITLC) showed a radiochemical purity around 95 per cent in optimized conditions (specific activity = 296–370 GBq/mM; labeling efficiency 85 per cent). Preliminary in vivo studies (IDźg–1 per cent) in male wild-type rats showed heart:muscle, liver:muscle, lung:muscle and stomach:muscle ratios to be 5.53, 2.9, 7.56, 3.69, 3.2 (in 5 min), respectively while after 2 h liver:blood, lung:blood and spleen:blood ratios were 14.21, 16.86 and 7.8, respectively. The data suggests 5 min post injection, the tracer is accumulated in GCGR rich tissues which is in agreement with biodistribution studies and reported GCG receptors (GCGRs). The results of the present study can possibly offer a candidate for non-invasive imaging of glucagon receptor related diseased and malignancies such as glucagonoma.
    Źródło:
    Nukleonika; 2010, 55, 2; 219-224
    0029-5922
    1508-5791
    Pojawia się w:
    Nukleonika
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Molecular docking and binding interaction between psychedelic drugs and human serum albumin
    Autorzy:
    Khastar, H.
    Foroughi, K.
    Aghayan, S.S.
    Yarmohammadi, M.
    Jafarisani, M.
    Powiązania:
    https://bibliotekanauki.pl/articles/2097000.pdf
    Data publikacji:
    2020
    Wydawca:
    Polska Akademia Nauk. Czytelnia Czasopism PAN
    Tematy:
    human serum albumin
    biodistribution
    psychedelic drugs
    molecular docking
    Opis:
    Drug-plasma protein interaction is a critical concern in monitoring drug circulation and drug-drug interactions. The present study aimed to investigate the interaction of psychedelic drugs such as lysergic acid diethylamide (LSD), dimethyltryptamine (DMT), 2,5-dimethoxy-4-iodoamphetamine (DOI), psilocybin, psilocin, and mescaline with human serum albumin (HSA). The 3D structures of LSD, DMT, DOI, psilocybin, psilocin, mescaline, and albumin were obtained from the structural databases (www.rcsb.org, https://pubchem.ncbi.nlm.nih.gov/compound). The structures were then prepared for molecular docking analysis by Autodock Vina software. Ultimately, the binding energies between docked HSA and psychedelic drugs were calculated, and their interactions were predicted. It was found that the psychedelic drugs can interact with HSA in the active site and the best minimum binding energies of -7.6 kcal/mol and -6.5 kcal/mol were shown by LSD and psilocybin, respectively. Our results indicated that all psychedelic drugs tested could interact with HSA at subdomains IA and IB. The structural properties of the drugs affect their interaction sites and binding energies. It was concluded that albumin, as the most abundant protein of the serum, could act as the biodistributor of psychedelic drugs.
    Źródło:
    BioTechnologia. Journal of Biotechnology Computational Biology and Bionanotechnology; 2020, 101, 2; 109-116
    0860-7796
    Pojawia się w:
    BioTechnologia. Journal of Biotechnology Computational Biology and Bionanotechnology
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    New amino bisphosphonate compound for skeletal imaging: Comparison study with methylenediphosphonic acid (MDP) and (1-hydroxyethane-1,1-diyl) diphosphonic acid (HEDP)
    Autorzy:
    Assaad, T.
    Powiązania:
    https://bibliotekanauki.pl/articles/971536.pdf
    Data publikacji:
    2016
    Wydawca:
    Instytut Chemii i Techniki Jądrowej
    Tematy:
    aminoethylidenediphosphonic acid
    biodistribution
    bisphosphonates
    bone imaging agent
    radiolabeling
    Opis:
    A novel bisphosphonate derivative (1-aminoethane-1,1-diyl)diphosphonic acid (AEDP) has been prepared and successfully labeled with 99mTc at high labeling yields. The in vivo biodistribution of 99mTc-AEDP has been investigated and compared with two reference compounds Tc-99m methylene diphosphonate (99mTc-MDP) and Tc-99m (1-hydroxyethylidene) diphosphonate (99mTc-HEDP). The biodistribution studies have demonstrated a high uptake of the radiotracer 99mTc-AEDP in the bone and a rapid clearance from the blood (such as the two technetium-labeled bone imaging agents in current use: 99mTc-MDP and 99mTc-HEDP). Additionally, the scintigraphic images of 99mTc-AEDP in normal rats have revealed high selective skeletal uptake.
    Źródło:
    Nukleonika; 2016, 61, 1; 69-74
    0029-5922
    1508-5791
    Pojawia się w:
    Nukleonika
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Planowanie wspomagania terapii przeciwnowotworowej przez suplementację witaminą C w oparciu o nowy model jej homeostazy w komórce
    Planning the support for cancer pharmacotherapy using vitamin C supplementation based on the new model of its homeostasis in cell
    Autorzy:
    Langner, Marek
    Powiązania:
    https://bibliotekanauki.pl/articles/2159080.pdf
    Data publikacji:
    2022-12
    Wydawca:
    Wydawnictwo Naukowe Medyk sp. z o.o.
    Tematy:
    witamina C
    homeostaza
    suplementacja
    biodystrybucja
    vitamin C
    homeostasis
    supplementation
    biodistribution
    Opis:
    Witamina C jest od lat przedmiotem dyskusji i kontrowersji spowodowanych brakiem wiedzy dotyczącej mechanizmów jej działania. W rezultacie wszelkie wskazaniaodnoszące się do suplementacji witaminą C spotykały się z dużą dozą nieufności. W przedstawionym opracowaniu pokazano aktualny stan wiedzy dotyczący metabolicznej roli witaminy C oraz mechanizmy odpowiedzialne za jej homeostazę na poziomie organizmu i komórki. W oparciu o tę wiedzę zaproponowano model opisujący homeostazę witaminy C, pozwalający na wyciągnięcie praktycznych wniosków dotyczących jej suplementacji. Na potrzeby prezentowanego omówienia przyjmujemy, że witamina C to biologicznie aktywna postać askorbinianu (anion kwasu L-askorbinowego). Anion ten powstaje w wodzie w wyniku dysocjacji soli lub kwasu askorbinowego, a fizjologiczna aktywność witaminy C skorelowana jest z jej ilością w organizmie, którą ocenia się na podstawie stężenia w surowicy krwi. Przyjmuje się, że dwa stężenia witaminy C w surowicy są ważne z punktu widzenia diagnostycznego. Pierwsze stężenie to 50 μM. Jest to stężenie witaminy C w surowicy, powyżej której zapotrzebowanie organizmu na witaminę C jest zaspokojone. Drugie stężenie to 20 μM. Gdy stężenie witaminy C w surowicy krwi jest poniżej tego poziomu, to pojawia się zagrożenie wystąpienia szkorbutu.
    Vitamin C has been the subject of discussion and controversy for years due to the lack of knowledge about its mechanisms of action. As a result, all indications regarding vitamin C supplementation are met with a high degree of distrust. The presented study shows the current state of knowledge regarding the metabolic role of vitamin C and the mechanisms responsible for its homeostasis at the organism and cellular level. Based on this knowledge, a model describing vitamin C homeostasis was proposed, allowing for drawing many practical conclusions regarding its supplementation
    Źródło:
    Lek w Polsce; 2022, 378, 11; 31-40
    2353-8597
    Pojawia się w:
    Lek w Polsce
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Preparation and biodistribution of [67Ga]-insulin for SPECT purposes
    Autorzy:
    Jalilian, A. R.
    Garousi, J.
    Gholami, E.
    Akhlaghi, M.
    Bolourinovin, F.
    Rajabifar, S.
    Powiązania:
    https://bibliotekanauki.pl/articles/971522.pdf
    Data publikacji:
    2007
    Wydawca:
    Instytut Chemii i Techniki Jądrowej
    Tematy:
    radiogallium
    insulin
    radiolabeling
    biodistribution
    radiopharmaceutical
    cyclotron
    Opis:
    Human recombinant insulin was successively labeled with [67Ga]-gallium chloride after conjugation with freshly prepared cyclic DTPA-dianhydride (ccDTPA). The best results of the conjugation were obtained by the addition of 0.5 ml of an insulin pharmaceutical solution (5 mg/ml, in phosphate buffer, pH = 8) to a glass tube precoated with DTPA-dianhydride (0.01 mg) at 25°C with continuous mild stirring for 30 min. Radiothin-layer chromatography (RTLC), instant thin-layer chromatography (ITLC) and high-performance liquid chromatography (HPLC) showed overall radiochemical purity higher than 96% in optimized conditions (specific activity = 300 500 MBq/mg, labeling efficiency 77%). Preliminary in vivo studies with normal rats were performed to determine the biodistribution of the radiotracer up to 110 h. They showed a high liver uptake of the tracer which is consistent with other reported radiolabeled insulins.
    Źródło:
    Nukleonika; 2007, 52, 4; 145-151
    0029-5922
    1508-5791
    Pojawia się w:
    Nukleonika
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Preparation and quality control of lutetium-177 bleomycin as a possible therapeutic agent
    Autorzy:
    Yousefnia, H.
    Jalilian, A. R.
    Zolghadri, S.
    Bahrami-Samani, A.
    Shirvani-Arani, S.
    Ghannadi-Maragheh, M.
    Powiązania:
    https://bibliotekanauki.pl/articles/148628.pdf
    Data publikacji:
    2010
    Wydawca:
    Instytut Chemii i Techniki Jądrowej
    Tematy:
    bleomycin
    Lu-177
    biodistribution
    radiolabeling
    Opis:
    Due to interesting therapeutic properties of 177Lu and antineoblastic antibiotic, bleomycin (BLM), 177Lu-bleomycin (177Lu-BLM) was developed as a possible therapeutic compound. Lu-177 of 2.6-3 GBq/mg specific activity was obtained by irradiation of a natural Lu2O3 sample with a thermal neutron flux of 4 × 1013 nźcm-2źs-1. The product was converted into chloride form which was further used for labeling of BLM. In optimized conditions a radiochemical purity of 98% was obtained for 177Lu-BLM shown by instant thin-layer chromatography (ITLC) (specific activity, 740 GBq/mmole). Biodistribution studies of Lu-177 chloride and 177Lu-BLM were performed in wild-type rats. The accumulation of the radiolabeled compound in lungs, liver and spleen demonstrates a pattern similar to the other radiolabeled bleomycins. Lu-BLM is a possible therapeutic agent in human malignancies and the efficacy of the compound should be tested in various tumor-bearing models.
    Źródło:
    Nukleonika; 2010, 55, 3; 285-291
    0029-5922
    1508-5791
    Pojawia się w:
    Nukleonika
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Preparation, quality control and biodistribution studies of 165Dy-chitosan for radiosynovectomy
    Autorzy:
    Shirvani-Arani, S.
    Mahmoodabadi, A.
    Bahrami-Samani, A.
    Jalilian, A. R.
    Mazidi, M.
    Afarideh, H.
    Ghannadi-Maragheh, M.
    Powiązania:
    https://bibliotekanauki.pl/articles/147619.pdf
    Data publikacji:
    2011
    Wydawca:
    Instytut Chemii i Techniki Jądrowej
    Tematy:
    radiosynovectomy
    Dy-165
    chitosan
    biodistribution
    Opis:
    The preparation of 165Dy-labeled chitosan for radiosynovectomy applications is described in this paper. 165Dy (T1/2 = 2.33 h) was prepared by irradiation of natural Dy(NO3)3 at a flux of 3.4 x 1013 neutrons/cm2.s for about 6 h. The irradiation resulted in the production of 11.1 GBq (300 mCi) of 165Dy activity. Emitting gamma ray (94.7 keV) and beta particles (Emax = 1.3 MeV, 83%) 165Dy decays to 165Ho. Eight hours after bombardment, the corresponding specific activity was 703 MBq/mg (19 mCi/mg). The irradiated target was dissolved in 0.1 N HCl solution. Radionuclidic purity was ascertained by high resolution gamma spectrometry. Chitosan solution was prepared in acetic acid solution (pH 3). The chitosan solution was labeled with 165Dy to prepare 165Dy-chitosan (165Dy-Chit) complex (labeling yield, greater than 99% and specific activity small tilde 3.7 TBq/mmol). In optimized conditions (pH 3, 35 mg/4 ml chitosan acidic solution, and 370 MBq of 165Dy) Chit was stable after 48 h. Bioevaluation of the prepared 165Dy-Chit was carried out by injecting 37 MBq (1 mCi, 50.100 mi1) directly into the knee joints of wild rats. Free 165Dy cation was also injected to study the effect of complex formation on the retention of radionuclide in the administered site. To study the consequence of radioactivity leakage from the administration site, a dilute sample of the complex was injected intravenously into the rats followed by biodistribution studies. It was observed that there was no significant extra-articular leakage of the injected activity over the study period of 24 h post-injection.
    Źródło:
    Nukleonika; 2011, 56, 4; 277-282
    0029-5922
    1508-5791
    Pojawia się w:
    Nukleonika
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Radiosynthesis and biological evaluation of 123I-(±)-trans-2-hydroxy-5-((E)- -3-(iodo)allyloxy)-3-(4-phenyl-1-piperazinyl) tetralin
    Autorzy:
    Assaad, T.
    Al Rayyes, A. H.
    Powiązania:
    https://bibliotekanauki.pl/articles/147888.pdf
    Data publikacji:
    2012
    Wydawca:
    Instytut Chemii i Techniki Jądrowej
    Tematy:
    Alzheimer's disease
    brain biodistribution
    injected dose (ID)
    radioiodination
    vesamicol derivatives
    vesicular acetylcholine transporter (VAChT)
    Opis:
    This work reports both the radiolabeling and preliminary biodistribution results in the rat brains of (±)-[123I]- -II. The novel benzovesamicol derivative (±)-[123I]-II was successfully labeled with iodine-123 from its corresponding n-tributyltin, with radiochemical purity greater than 97% and radiochemical yield in the range 50–55%. (±)-[123I]-II showed a higher accumulation in striatum than in the other regions studied. To determine if (±)-[123I]-II could provide an advantage compared to reference compound [125I]-IBVM a kinetic study was carried out, at each point of the kinetic study, (±)-[123I]-II showed a lower specific binding compared to [125I]-IBVM. Time activity curves of (±)-[123I]-II confirmed that this compound is inferior to [125I]-IBVM to explore the VAChT in vivo by SPECT. Moreover, it is well known that interaction at the VAChT binding site is enantioselective, and therefore, working with enantiomerically pure compounds, could improve the compound activity.
    Źródło:
    Nukleonika; 2012, 57, 1; 75-80
    0029-5922
    1508-5791
    Pojawia się w:
    Nukleonika
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Synthesis and biodistribution of both (±)-5-[ 18F]-fluoroethoxy and (±)-5-[ 18F]-fluoropropoxy piperazine analogs of benzovesamicol as vesicular acetylcholine transporter ligands (VAChT)
    Autorzy:
    Assaad, T.
    Al Rayyes, A. H.
    Powiązania:
    https://bibliotekanauki.pl/articles/147599.pdf
    Data publikacji:
    2013
    Wydawca:
    Instytut Chemii i Techniki Jądrowej
    Tematy:
    Alzheimer's disease (AD)
    benzovisamicol derivatives
    brain biodistribution
    enantiomeric resolution
    radiofluorination
    vesicular acetylcholine transporter (VAChT)
    Opis:
    The radiosynthesis and preliminary biological evaluation in rats’ brain of two novel piperazine analogs of benzovesamicol as ligands for the vesicular acetylcholine transporter (VAChT) have been carried out. The novel benzovesamicol derivatives 5-(2-fluoroethoxy)-3-(4-phenylpiperazin-1-yl)-1,2,3,4-tetrahydronaphthalen-2-ol and 5-(3-fluoropropoxy)-3-(4-phenylpiperazin-1-yl)-1,2,3,4-tetrahydronaphthalen-2-ol [(±)-[18F]-6 and (±)-[18F]-7] were successfully labelled with fluorine-18 from their tosylate precursors, with radiochemical purities greater than 98% and with radiochemical yield in the range of 5–6%. To determine whether these compounds could have potential advantage compared to [125I]-iodo benzovesamicol (IBVM), IBVM was also labelled and used as the reference compound in all in vivo experiments. Both (±)-[18F]-6 and (±)-[18F]-7 showed lower specific binding in all brain areas explored 2 h post injection when compared to reference compound (-)-[125I] IBVM. Furthermore, defluorination indicated that (±)-[18F]-6 and (±)-[18F]-7 are not suitable as radioligands to explore the VAChT in vivo by PET. Moreover, it is well known that interaction at the VAChT binding site is enantioselective, and therefore, working with enantiomerically pure compounds, could improve the compound activity.
    Źródło:
    Nukleonika; 2013, 58, 2; 269-274
    0029-5922
    1508-5791
    Pojawia się w:
    Nukleonika
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Synthesis and in vivo evaluation of both (2R,3R)-[123I]- and (2S,3S)- -[123I]-trans-2-hydroxy-5-((E)-3-(iodo) allyloxy)-3-(4-phenyl-1-piperazinyl) tetralin as SPECT radiotracer
    Autorzy:
    Assaad, T.
    Al Rayyes, A. H.
    Powiązania:
    https://bibliotekanauki.pl/articles/148128.pdf
    Data publikacji:
    2013
    Wydawca:
    Instytut Chemii i Techniki Jądrowej
    Tematy:
    Alzheimer's disease
    benzovisamicol derivatives
    brain biodistribution
    enantiomeric resolution
    radioiodination
    vesicular acetylcholine transporter (VAChT)
    Opis:
    We report the synthesis of enantiopure benzovesamicol derivatives: (2R,3R)-[123I]-trans-2-hydroxy-5-((E)-3- -(iodo)allyloxy)-3-(4-phenyl-1-piperazinyl) tetralin and (2S,3S)-[123I]-trans-2-hydroxy-5-((E)-3-(iodo)allyloxy)-3-(4- phenyl-1-piperazinyl) tetralin; [(2R,3R)-[123I]-1 and (2S,3S)-[123I]-1]. Both compounds were obtained with radiochemical and optical purities greater than 97% and with radiochemical yields in the range of 50–60%. To determine whether these compounds could have potential advantage compared to [125I]-iodo benzovesamicol (IBVM), IBVM was also labelled and used as the reference compound in all in vivo experiments. Both (2R,3R)-[123I]-1 and (-)-[125I]-IBVM showed similar time activity curves (TACs) with the highest accumulations in the striatum region followed by the cortex, hippocampus and then cerebellum. While (2S,3S)-[123I]-1 showed an overall homogeneous brain distribution. However, time activity curves of (2R,3R)-[123I]-1 confirmed that this compound could be used to visualize the vesicular acetylcholine transporter (VAChT) in vivo, at each point of the kinetic study. Also (2R,3R)-[123I]-1 showed lower specific bindings compared to [125I]-IBVM. These results suggested that (2R,3R)-[123I]-1 is inferior in comparison with [125I]-IBVM for in vivo VAChT exploration.
    Źródło:
    Nukleonika; 2013, 58, 2; 261-267
    0029-5922
    1508-5791
    Pojawia się w:
    Nukleonika
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
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