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Improved Visualization and Specific Binding for Metabotropic Glutamate Receptor Subtype 1 (mGluR1) Using [11C]ITMM with Ultra-High Specific Activity in Small-Animal PET.

Metabotropic glutamate receptor subtype 1 (mGluR1) is a crucial target in the development of new medications to treat central nervous system (CNS) disorders. Recently, we developed N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-4-[.sup.11 C]methoxy-N-methyl-benzamide ([.sup.11 C]ITMM) as... Full description

Journal Title: PloS one 2015, Vol.10(6), p.e0130006
Main Author: Yamasaki, Tomoteru
Other Authors: Fujinaga, Masayuki , Yui, Joji , Wakizaka, Hidekatsu , Ohya, Tomoyuki , Nengaki, Nobuki , Ogawa, Masanao , Ikoma, Yoko , Hatori, Akiko , Xie, Lin , Kawamura, Kazunori , Zhang, Ming-Rong
Format: Electronic Article Electronic Article
Language: English
Subjects:
ID: E-ISSN: 1932-6203 ; DOI: 10.1371/journal.pone.0130006
Link: http://search.proquest.com/docview/1689622405/?pq-origsite=primo
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title: Improved Visualization and Specific Binding for Metabotropic Glutamate Receptor Subtype 1 (mGluR1) Using [11C]ITMM with Ultra-High Specific Activity in Small-Animal PET.
format: Article
creator:
  • Yamasaki, Tomoteru
  • Fujinaga, Masayuki
  • Yui, Joji
  • Wakizaka, Hidekatsu
  • Ohya, Tomoyuki
  • Nengaki, Nobuki
  • Ogawa, Masanao
  • Ikoma, Yoko
  • Hatori, Akiko
  • Xie, Lin
  • Kawamura, Kazunori
  • Zhang, Ming-Rong
subjects:
  • Animals–Pharmacokinetics
  • Benzamides–Diagnostic Imaging
  • Brain–Metabolism
  • Carbon Radioisotopes–Pharmacokinetics
  • Image Processing, Computer-Assisted–Methods
  • Male–Pharmacokinetics
  • Positron-Emission Tomography–Metabolism
  • Radiopharmaceuticals–Pharmacokinetics
  • Rats–Pharmacokinetics
  • Rats, Sprague-Dawley–Pharmacokinetics
  • Receptors, Metabotropic Glutamate–Pharmacokinetics
  • Thiazoles–Pharmacokinetics
  • Tissue Distribution–Pharmacokinetics
  • Benzamides
  • Carbon Radioisotopes
  • N-(4-(6-(Isopropylamino)Pyrimidin-4-Yl)-1,3-Thiazol-2-Yl)-4-Methoxy-N-Methylbenzamide
  • Radiopharmaceuticals
  • Receptors, Metabotropic Glutamate
  • Thiazoles
  • Metabotropic Glutamate Receptor Type 1
ispartof: PloS one, 2015, Vol.10(6), p.e0130006
description: Metabotropic glutamate receptor subtype 1 (mGluR1) is a crucial target in the development of new medications to treat central nervous system (CNS) disorders. Recently, we developed N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-4-[.sup.11 C]methoxy-N-methyl-benzamide ([.sup.11 C]ITMM) as a useful positron emission tomography (PET) probe for mGluR1 in clinical studies. Here, we aimed to improve visualization and threshold of specific binding for mGluR1 using [.sup.11 C]ITMM with ultra-high specific activity (SA) of > 3,500 GBq/[mu]mol in rat brains. A two-tissue compartment model indicated large differences between the two SAs in the constants k.sub.3 and k.sub.4, representing binding ability for mGluR1, while constants K.sub.1 and k.sub.2 showed no differences. The total distribution volume (V.sub.T) values of conventional and ultra-high SA were 9.1 and 11.2 in the thalamus, 7.7 and 9.7 in the striatum, and 6.4 and 8.5 mL/cm.sup.3 in the substantia nigra, respectively. The specific binding of [.sup.11 C]ITMM with ultra-high SA was significantly higher than the conventional SA, especially in the basal ganglia. Parametric PET images scaled with V.sub.T of the ultra-high SA clearly identified regional differences in the rat brain. In conclusion, PET studies using [.sup.11 C]ITMM with ultra-high SA could sufficiently improve visualization and specific binding for mGluR1, which could help further understanding for mGluR1 functions in CNS disorders.
language: eng
source:
identifier: E-ISSN: 1932-6203 ; DOI: 10.1371/journal.pone.0130006
fulltext: fulltext
issn:
  • 19326203
  • 1932-6203
url: Link


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titleImproved Visualization and Specific Binding for Metabotropic Glutamate Receptor Subtype 1 (mGluR1) Using [11C]ITMM with Ultra-High Specific Activity in Small-Animal PET.
creatorYamasaki, Tomoteru ; Fujinaga, Masayuki ; Yui, Joji ; Wakizaka, Hidekatsu ; Ohya, Tomoyuki ; Nengaki, Nobuki ; Ogawa, Masanao ; Ikoma, Yoko ; Hatori, Akiko ; Xie, Lin ; Kawamura, Kazunori ; Zhang, Ming-Rong
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identifierE-ISSN: 1932-6203 ; DOI: 10.1371/journal.pone.0130006
subjectAnimals–Pharmacokinetics ; Benzamides–Diagnostic Imaging ; Brain–Metabolism ; Carbon Radioisotopes–Pharmacokinetics ; Image Processing, Computer-Assisted–Methods ; Male–Pharmacokinetics ; Positron-Emission Tomography–Metabolism ; Radiopharmaceuticals–Pharmacokinetics ; Rats–Pharmacokinetics ; Rats, Sprague-Dawley–Pharmacokinetics ; Receptors, Metabotropic Glutamate–Pharmacokinetics ; Thiazoles–Pharmacokinetics ; Tissue Distribution–Pharmacokinetics ; Benzamides ; Carbon Radioisotopes ; N-(4-(6-(Isopropylamino)Pyrimidin-4-Yl)-1,3-Thiazol-2-Yl)-4-Methoxy-N-Methylbenzamide ; Radiopharmaceuticals ; Receptors, Metabotropic Glutamate ; Thiazoles ; Metabotropic Glutamate Receptor Type 1
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descriptionMetabotropic glutamate receptor subtype 1 (mGluR1) is a crucial target in the development of new medications to treat central nervous system (CNS) disorders. Recently, we developed N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-4-[.sup.11 C]methoxy-N-methyl-benzamide ([.sup.11 C]ITMM) as a useful positron emission tomography (PET) probe for mGluR1 in clinical studies. Here, we aimed to improve visualization and threshold of specific binding for mGluR1 using [.sup.11 C]ITMM with ultra-high specific activity (SA) of > 3,500 GBq/[mu]mol in rat brains. A two-tissue compartment model indicated large differences between the two SAs in the constants k.sub.3 and k.sub.4, representing binding ability for mGluR1, while constants K.sub.1 and k.sub.2 showed no differences. The total distribution volume (V.sub.T) values of conventional and ultra-high SA were 9.1 and 11.2 in the thalamus, 7.7 and 9.7 in the striatum, and 6.4 and 8.5 mL/cm.sup.3 in the substantia nigra, respectively. The specific binding of [.sup.11 C]ITMM with ultra-high SA was significantly higher than the conventional SA, especially in the basal ganglia. Parametric PET images scaled with V.sub.T of the ultra-high SA clearly identified regional differences in the rat brain. In conclusion, PET studies using [.sup.11 C]ITMM with ultra-high SA could sufficiently improve visualization and specific binding for mGluR1, which could help further understanding for mGluR1 functions in CNS disorders.
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titleImproved Visualization and Specific Binding for Metabotropic Glutamate Receptor Subtype 1 (mGluR1) Using [11C]ITMM with Ultra-High Specific Activity in Small-Animal PET.
authorYamasaki, Tomoteru ; Fujinaga, Masayuki ; Yui, Joji ; Wakizaka, Hidekatsu ; Ohya, Tomoyuki ; Nengaki, Nobuki ; Ogawa, Masanao ; Ikoma, Yoko ; Hatori, Akiko ; Xie, Lin ; Kawamura, Kazunori ; Zhang, Ming-Rong
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