Noninvasive quantification of metabotropic glutamate receptortype 1 with [11C]ITDM:a small-animal PET study

Because of its role in multiple central nervous system
(CNS) pathways, metabotropic glutamate receptor type 1
(mGluR1) is a crucial target in the development of
pharmaceuticals for CNS disorders. N-[4-[6-
(isopropylamino)-pyrimidin-4-yl]-1,3-thiazol-2-yl]-Nmethyl-
4-[11C]-methylbenzamide ([11C]ITDM) was
recently developed as a positron emission tomography
(PET) ligand for mGluR1. To devise a method for
measurement of the binding potential (BPND) of
[11C]ITDM to mGluR1, reference tissue methods aimed at
replacing measurement of the arterial input function are　desirable. In this study, we evaluated a noninvasive
quantification method of mGluR1 with [11C]ITDM,
demonstrating its accuracy using Huntington disease
model R6/2 mice. The BPND measurements based on the
Logan reference (Logan Ref) method have closely
approximated that based on the arterial input method. We
performed PET analysis with Logan Ref to assess its
accuracy in quantifying the decline of mGluR1 expression
in R6/2 mice. Significant decreases in BPND values in R6/2
mice were detected in cerebellum, thalamus, striatum,
and cingulate cortex. We compared autoradiographs of
R6/2 mouse brain sections with immunohistochemical
images, and found a close correlation between changes in
radioactive signal intensity and degree of mGluR1
expression. In conclusion, [11C]ITDM-PET is a promising
tool for in vivo quantification of mGluR1 expression.

書誌情報

Journal of Cerebral Blood Flow & Metabolism

巻 34, 号 1, p. 1-7, 発行日 2014-01

出版者

Nature Publishing Group

ISSN

収録物識別子タイプ

ISSN

収録物識別子

0271-678X

DOI

識別子タイプ

DOI

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2023-05-15 23:41:10.126006

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