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Hoigebazar, Lathika,Jeong, Jae Min,Lee, Ji-Youn,Shetty, Dinesh,Yang, Bo Yeun,Lee, Yun-Sang,Lee, Dong Soo,Chung, June-Key,Lee, Myung Chul American ChemicalSociety 2012 Journal of medicinal chemistry Vol.55 No.7
<P>Hypoxia imaging is important for diagnosis of ischemicdiseases, and thus various <SUP>18</SUP>F-labeled radiopharmaceuticalshave been developed. However, <SUP>18</SUP>F-labeling requires multistepprocedures including azeotropic distillation, which is complicatedand difficult to automate. Recently, <SUP>18</SUP>F-labeling methodusing Al–F complex in aqueous solution was devised that offereda straightforward <SUP>18</SUP>F-labeling procedure. We synthesizednitroimidazole derivatives conjugated with 1,4,7-triazacyclononane-1,4-diaceticacid (NODA) that can be labeled with <SUP>18</SUP>F using Al–Fcomplex and examined their radiochemistries, in vitro and in vivobiological properties, and animal PET imaging characteristics. Wefound that the synthesized derivatives have excellent <SUP>18</SUP>F-labeling efficiencies, high stabilities, specific uptakes in culturedhypoxic tumor cells, and high tumor to nontumor ratios in xenograftedmice. Furthermore, the derivatives were labeled with <SUP>18</SUP>F in a straightforward manner within 15 min at high labeling efficienciesand radiochemical purities. In conclusion, <SUP>18</SUP>F-labeledNODA–nitroimidazole conjugates were developed and proved tobe promising hypoxia PET agents.</P><P><B>Graphic Abstract</B> <IMG SRC='http://pubs.acs.org/appl/literatum/publisher/achs/journals/content/jmcmar/2012/jmcmar.2012.55.issue-7/jm201611a/production/images/medium/jm-2011-01611a_0009.gif'></P><P><A href='http://pubs.acs.org/doi/suppl/10.1021/jm201611a'>ACS Electronic Supporting Info</A></P>
Lee, Young Kyoung,Jeong, Jae Min,Hoigebazar, Lathika,Yang, Bo Yeun,Lee, Yun-Sang,Lee, Byung Chul,Youn, Hyewon,Lee, Dong Soo,Chung, June-Key,Lee, Myung Chul Society of Nuclear Medicine 2012 The Journal of nuclear medicine Vol.53 No.9
<P>The attachment of specific ligands to the surfaces of nanoparticles is important for medical and biologic imaging. However, covalent modification of nanoparticles has inherent problems in reproducibility because of many factors such as temperature, pH, concentration, and reaction time. Thus, we developed a method for modifying nanoparticles by encapsulation with specific ligand-conjugated amphiphiles.</P>
Shetty, Dinesh,Choi, Soo Young,Jeong, Jae Min,Lee, Ji Youn,Hoigebazar, Lathika,Lee, Yun-Sang,Lee, Dong Soo,Chung, June-Key,Lee, Myung Chul,Chung, Young Keun Royal Society of Chemistry 2011 Chemical communications Vol.47 No.34
<P>A single crystal structure of an aluminium-fluoride complex of a model compound (NODA-benzyl) was studied to understand the co-ordination chemistry. Series of ligands with an extra carboxylic acid linker for biomolecule conjugation were studied for improved <SUP>18</SUP>F-labeling applications.</P> <P>Graphic Abstract</P><P>A study on the crystal structure of an aluminium-fluoride complex allowed us to develop NODA ligands for <SUP>18</SUP>F-labeling with an excellent yield. <IMG SRC='http://pubs.rsc.org/services/images/RSCpubs.ePlatform.Service.FreeContent.ImageService.svc/ImageService/image/GA?id=c1cc13151f'> </P>
Shetty, Dinesh,Choi, Soo Young,Jeong, Jae Min,Hoigebazar, Lathika,Lee, Yun‐,Sang,Lee, Dong Soo,Chung, June‐,Key,Lee, Myung Chul,Chung, Young Keun WILEY‐VCH Verlag 2010 European journal of inorganic chemistry Vol.2010 No.34
<P><B>Abstract</B></P><P>Two monoamide derivatives of 1,4,7‐triazacyclononane‐1,4,7‐triacetic acid (NOTA) conjugated with methylamine (<B>4</B>) or benzylamine (<B>5</B>) were synthesized by treating di‐<I>tert</I>‐butyl 1,4,7‐triazacyclononane‐1,4‐diacetate (<B>1</B>) with 2‐chloro‐<I>N</I>‐benzyl‐ or ‐<I>N</I>‐methylacetamide, followed by an acid cleavage reaction. Complexes of <B>4</B> and <B>5</B> chelated to Ga<SUP>3+</SUP> to give Ga‐<B>4</B> and Ga‐<B>5</B>, respectively, in reaction solutions at different pH values (3 and 5). Complexes Ga‐<B>4</B> and Ga‐<B>5</B> were characterized by single‐crystal X‐ray diffraction and multinuclear NMR spectroscopy. In the solid state, these complexes were isostructural, and the coordination spheres of the metal ions exhibited distorted octahedral geometries. In the case of the Ga‐<B>4</B> complex, which was formed at both pH values, the metal ion is coordinated to the amide nitrogen atom of the modified pendent arm of <B>4</B>. However, in the case of Ga‐<B>5</B>, the metal ion is coordinated to a nitrogen or an oxygen atom of the amide linkage when the pH of the reaction soultion was 5 or 3, respectively. No significant difference was found between the <SUP>1</SUP>H NMR spectra of the complexes formed at pH = 3 and 5. However, <SUP>71</SUP>Ga NMR spectra showed a broad resonance signal and a narrow singlet for the complex synthesized at the lower pH, but only a single narrow singlet for the complex prepared at neutral pH. Variable‐temperature <SUP>1</SUP>H NMR spectra showed that complexes Ga‐<B>4</B> and Ga‐<B>5</B> are rigid in solution. The stability of these complexes in the physiological pH range and at high temperature suggests that NOTA can be used as a bifunctional chelating agent to label biomolecules with radioactive gallium by direct conjugation of the complex to target molecules. This finding could open up a wide range of applications for NOTA‐type bifunctional chelating agents by eliminating the multi‐step synthesis routes required to introduce extra linker groups to the labelling agent.</P>
Compartmental Modeling and Simplified Quantification of [11C]sertraline Distribution in Human Brain
Ji Who Kim,이동수,이재성,Su Jin Kim,Lathika Hoigebazar,Kwang-Hee Shin,Kyung-Sang Yu,Wonsik Ahn,정재민 대한약학회 2012 Archives of Pharmacal Research Vol.35 No.9
Sertraline hydrochloride (Zoloft®, Pfizer) is an antidepressant drug of the selective serotonin reuptake inhibitor (SSRI). The aims of this study were evaluating its in vivo distribution and kinetic models in human brain. Also, this study was to determine optimal scan duration of dynamic positron emission tomography (PET) for accurate [11C]sertraline kinetic parameters and the feasibility of semi-quantitative approach for assessing distribution volume ratio (DVR). [11C]sertraline dynamic PET and magnetic resonance imaging (MRI) scans were performed in 5 healthy males. Blood sampling were collected for the input function. Tissue time-activity curves (TAC) were obtained in 7 brain regions using MRI. Goodness-of-fit for TAC using simple tissue compartment model (2C2P) and 3-compartment models with irreversible (3C3P) and reversible (3C4P) were compared. Total distribution volume (DV) for each region of interest (ROI) and DVR were calculated. Also, ratio between the standard uptake value (SUV) of each ROI and that of cerebellum (SUVr) was computed and correlated with the DVR. Akaike information criteria analysis showed that the 2C2P was the most suitable model. Average values of K1 (mL/min/g) and k2 (1/min) were 0.54 and 0.012 in putamen. PET scan time longer than 50 min was required for the accurate estimation of DV. SUVr in 50-90 min was well correlated with DVR.