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2-Iodophenol

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Akira Odani – One of the best experts on this subject based on the ideXlab platform.

  • Development and evaluation of a novel radioiodinated vesamicol analog as a sigma receptor imaging agent
    EJNMMI research, 2012
    Co-Authors: Kazuma Ogawa, Kazuhiro Shiba, Hiroya Kanbara, Yoji Kitamura, Takashi Kozaka, Tatsuto Kiwada, Akira Odani
    Abstract:

    Background Sigma receptors are highly expressed in human tumors and should be appropriate targets for developing tumor imaging agents. Previously, we synthesized a vesamicol analog, (+)-2-[4-(4-iodophenyl)piperidino]cyclohexanol ((+)-p IV), with a high affinity for sigma receptors and prepared radioiodinated (+)-p IV. As a result, (+)-[125I]p IV showed high tumor uptake in biodistribution experiments. However, the accumulation of radioactivity in normal tissues, such as the liver, was high. We supposed that some parts of the accumulation of (+)-p IV in the liver should be because of its high lipophilicity, and prepared and evaluated a more hydrophilic radiolabeled vesamicol analog, (+)-4-[1-(2-hydroxycyclohexyl)piperidine-4-yl]-2-Iodophenol ((+)-IV-OH).

  • Development and evaluation of a novel radioiodinated vesamicol analog as a sigma receptor imaging agent
    EJNMMI Research, 2012
    Co-Authors: Kazuma Ogawa, Kazuhiro Shiba, Hiroya Kanbara, Yoji Kitamura, Takashi Kozaka, Tatsuto Kiwada, Akira Odani
    Abstract:

    Background Sigma receptors are highly expressed in human tumors and should be appropriate targets for developing tumor imaging agents. Previously, we synthesized a vesamicol analog, (+)-2-[4-(4-iodophenyl)piperidino]cyclohexanol ((+)- p IV), with a high affinity for sigma receptors and prepared radioiodinated (+)- p IV. As a result, (+)-[^125I] p IV showed high tumor uptake in biodistribution experiments. However, the accumulation of radioactivity in normal tissues, such as the liver, was high. We supposed that some parts of the accumulation of (+)- p IV in the liver should be because of its high lipophilicity, and prepared and evaluated a more hydrophilic radiolabeled vesamicol analog, (+)-4-[1-(2-hydroxycyclohexyl)piperidine-4-yl]-2-Iodophenol ((+)-IV-OH). Methods (+)-[^125I]IV-OH was prepared by the chloramine T method from the precursor. The partition coefficient of (+)-[^125I]IV-OH was measured. Biodistribution experiments were performed by intravenous administration of a mixed solution of (+)-[^125I]IV-OH and (+)-[^131I] p IV into DU-145 tumor-bearing mice. Blocking studies were performed by intravenous injection of (+)-[^125I]IV-OH mixed with an excess amount of ligand into DU-145 tumor-bearing mice. Results The hydrophilicity of (+)-[^125I]IV-OH was much higher than that of (+)-[^125I] p IV. In biodistribution experiments, (+)-[^125I]IV-OH and (+)-[^131I] p IV showed high uptake in tumor tissues at 10-min post-injection. Although (+)-[^131I] p IV tended to be retained in most tissues, (+)-[^125I]IV-OH was cleared from most tissues. In the liver, the radioactivity level of (+)-[^125I]IV-OH was significantly lower at all time points compared to those of (+)-[^131I] p IV. In the blocking studies, co-injection of an excess amount of sigma ligands resulted in significant decreases of tumor/blood uptake ratios after injection of (+)-[^125I]IV-OH. Conclusions The results indicate that radioiodinated (+)-IV-OH holds a potential as a sigma receptor imaging agent.

Kazuma Ogawa – One of the best experts on this subject based on the ideXlab platform.

  • Development and evaluation of a novel radioiodinated vesamicol analog as a sigma receptor imaging agent
    EJNMMI research, 2012
    Co-Authors: Kazuma Ogawa, Kazuhiro Shiba, Hiroya Kanbara, Yoji Kitamura, Takashi Kozaka, Tatsuto Kiwada, Akira Odani
    Abstract:

    Background Sigma receptors are highly expressed in human tumors and should be appropriate targets for developing tumor imaging agents. Previously, we synthesized a vesamicol analog, (+)-2-[4-(4-iodophenyl)piperidino]cyclohexanol ((+)-p IV), with a high affinity for sigma receptors and prepared radioiodinated (+)-p IV. As a result, (+)-[125I]p IV showed high tumor uptake in biodistribution experiments. However, the accumulation of radioactivity in normal tissues, such as the liver, was high. We supposed that some parts of the accumulation of (+)-p IV in the liver should be because of its high lipophilicity, and prepared and evaluated a more hydrophilic radiolabeled vesamicol analog, (+)-4-[1-(2-hydroxycyclohexyl)piperidine-4-yl]-2-Iodophenol ((+)-IV-OH).

  • Development and evaluation of a novel radioiodinated vesamicol analog as a sigma receptor imaging agent
    EJNMMI Research, 2012
    Co-Authors: Kazuma Ogawa, Kazuhiro Shiba, Hiroya Kanbara, Yoji Kitamura, Takashi Kozaka, Tatsuto Kiwada, Akira Odani
    Abstract:

    Background Sigma receptors are highly expressed in human tumors and should be appropriate targets for developing tumor imaging agents. Previously, we synthesized a vesamicol analog, (+)-2-[4-(4-iodophenyl)piperidino]cyclohexanol ((+)- p IV), with a high affinity for sigma receptors and prepared radioiodinated (+)- p IV. As a result, (+)-[^125I] p IV showed high tumor uptake in biodistribution experiments. However, the accumulation of radioactivity in normal tissues, such as the liver, was high. We supposed that some parts of the accumulation of (+)- p IV in the liver should be because of its high lipophilicity, and prepared and evaluated a more hydrophilic radiolabeled vesamicol analog, (+)-4-[1-(2-hydroxycyclohexyl)piperidine-4-yl]-2-Iodophenol ((+)-IV-OH). Methods (+)-[^125I]IV-OH was prepared by the chloramine T method from the precursor. The partition coefficient of (+)-[^125I]IV-OH was measured. Biodistribution experiments were performed by intravenous administration of a mixed solution of (+)-[^125I]IV-OH and (+)-[^131I] p IV into DU-145 tumor-bearing mice. Blocking studies were performed by intravenous injection of (+)-[^125I]IV-OH mixed with an excess amount of ligand into DU-145 tumor-bearing mice. Results The hydrophilicity of (+)-[^125I]IV-OH was much higher than that of (+)-[^125I] p IV. In biodistribution experiments, (+)-[^125I]IV-OH and (+)-[^131I] p IV showed high uptake in tumor tissues at 10-min post-injection. Although (+)-[^131I] p IV tended to be retained in most tissues, (+)-[^125I]IV-OH was cleared from most tissues. In the liver, the radioactivity level of (+)-[^125I]IV-OH was significantly lower at all time points compared to those of (+)-[^131I] p IV. In the blocking studies, co-injection of an excess amount of sigma ligands resulted in significant decreases of tumor/blood uptake ratios after injection of (+)-[^125I]IV-OH. Conclusions The results indicate that radioiodinated (+)-IV-OH holds a potential as a sigma receptor imaging agent.

Frédéric Lamaty – One of the best experts on this subject based on the ideXlab platform.

  • Efficient synthetic approach to heterocycles possessing the 3,3-disubstituted-2,3-dihydrobenzofuran skeleton via diverse palladium-catalyzed tandem reactions
    Tetrahedron, 2007
    Co-Authors: Magali Szlosek-pinaud, Philippe Diaz, Jean Martinez, Frédéric Lamaty
    Abstract:

    Abstract Various palladium-catalyzed cascade reactions of O -alkylated 2-Iodophenol were explored in order to synthesize novel dihydrobenzofurans. An efficient tandem cyclization/anion capture reaction was developed to yield 3,3-disubstituted-2,3-dihydrobenzofurans. A small library of these compounds was prepared with a parallel organic synthesizer. A multi-component version of this reaction involving 2-Iodophenol, an alkylating agent and a nucleophile, provided the same products. The methoxycarbonyl-substituted heterocyclic ring was hydrolyzed to a free acid, which could be used for further transformations.

  • Palladium-catalyzed cascade allylation/carbopalladation/cross coupling: a novel three-component reaction for the synthesis of 3,3-disubstituted-2,3-dihydrobenzofurans
    Tetrahedron Letters, 2003
    Co-Authors: Magali Szlosek-pinaud, Philippe Diaz, Jean Martinez, Frédéric Lamaty
    Abstract:

    A novel one-pot palladium-catalyzed cascade between 2-Iodophenol, methyl bromomethylacrylate and an arylboronic acid provides an efficient access to heterocycles possessing the 3,3-disubstituted-2,3-dihydrobenzofuran skeleton via allylation/carbopalladation/Suzuki cross-coupling.