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1997 Fiscal Year Final Research Report Summary

In vitro and In vivo evaluation of Radioiodinated (-) -m-iodovesamicol : Potential radioligand for diagnosing Alzheimer's disease.

Research Project

Project/Area Number 08671010
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeSingle-year Grants
Section一般
Research Field Radiation science
Research InstitutionKANAZAWA UNIVERSITY

Principal Investigator

SHIBA Kazuhiro  Kanazawa University, Radioisotope Center, Assistant Professor, アイソトープ総合センター, 助手 (40143929)

Co-Investigator(Kenkyū-buntansha) MORI Hirofumi  Kanazawa University, Radioisotope Center, Professor, アイソトープ総合センター, 教授 (90019604)
Project Period (FY) 1996 – 1997
KeywordsIodovesamicol / Cholinergic neurons / Acetylcholine Transporter / Alzheimer's Disease
Research Abstract

The purpose of this investigation is to develop a new presynaptic cholinergic neuron mapping agent. We synthesized levorotatory isomer (-) -m-iodovesamicol ((-) mIV) radioiodinated at the meta position of the 4-phenylpiperidine moiety and evaluated the in vitro and in vivo binding affinity and specificity of [I-125] (-) -mIV for the vesamicol receptor in rat brain, furthermore, evaluated the in vivo characteristics of [I-125] (-) -mIV in the model rat of Alzheimer's disease. In vitro and In vivo binding affinity of [I-125] (-) -mIV for the vesamicol receptor (acetylcholine transporter) was very high and comparable to that of (-) -vesamicol ; the binding affinity for dopamine, serotonin, noradrenaline, acetylcholine and sigma receptors was low. These similar results were derived from saturation binding study ; Kd (18.2nM) and Bmax (660 fmol/mg of protein) of [I-125] (-) -mIV were comparable to those of (-) -vesamicol (Kd=20-30nM,Bmax=334-516fmol/mg of protein). Furthermore, double-tracer autoradiograms using [I-125] (-) -mIV and [Tc-99m] HMPAO in model rat brain of Alzheimer's disease showed a significant 11% decrease of the accumulation of [I-125] (-) -mIV in the projection cortices ipsilateral to the basalforebrain lesion in a unilateral cholinergic denervation model, which is regarded as an experimental model of Alzheimer's disease. The difference between the decrease of the accumulation of [I-125] (-) -mIV (11%) and that of [Tc-99m] HMPAO (4%) in the regions was statistically significant (P<0.01). These results suggest that radioiodinated (-) -mIV may serve as a useful radioligand for mapping presynaptic cholinergic neurons.

  • Research Products

    (6 results)

All Other

All Publications (6 results)

  • [Publications] 柴 和弘: "Radioiodinated(-)-2-[4-(3-iodophenyl) piperidino] cyclohexanol : A potential radioligand for mapping presynaptic cholinergic neurons" Nuclear Medicine Communications. 17. 485-492 (1996)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] 柴 和弘: "In vitro Characterization of Radioiodinated (-)-m-iodovesamicol in rat cerebral membranes." Life Science. 59. 1039-1045 (1996)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] 柴 和弘: "シナプス前神経機能診断用の放射線医薬品開発" Radioisotopes. 47. 97-100 (1998)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] Shiba, K.: "Radioiodinated (-) -2- [4- (3-iodophenyl) piperidino] cyclohexanol : A potential radioligand for mapping presynaptic cholinergic neurons." Nuclear Medicine Communications. 17. 485-492 (1996)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] Shiba, K.: "In vitro Characterization of radioiodinated (-) -m-iodovesamicol in rat cerebral membranes." Life Sciences. 59. 1039-1045 (1996)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] Shiba, K.: "Radiopharmaceuticals for mapping presynaptic neurons" Radioisotopes. 47. 97-100 (1997)

    • Description
      「研究成果報告書概要(欧文)」より

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Published: 1999-03-16  

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