In vitro and In vivo Assessment of Suitable Reference Region and Kinetic Modelling for the mGluR1 Radioligand [¹¹C]ITDM in Mice.

ABSTRACT:

Purpose

This study aimed at investigating binding specificity, suitability of reference region-based kinetic modelling, and pharmacokinetics of the metabotropic glutamate receptor 1 (mGluR1) radioligand [¹¹C]ITDM in mice.

Procedures

We performed in vivo blocking as well as displacement of [¹¹C]ITDM during positron emission tomography (PET) imaging using the specific mGluR1 antagonist YM-202074. Additionally, we assessed in vitro blocking of [³H]ITDM at two different doses of YM-202074. As an alternative to reference region models, we validated the use of a noninvasive image-derived input function (IDIF) compared to an arterial input function measured with an invasive arteriovenous (AV) shunt using a population-based curve for radiometabolite

SUBMITTER: Bertoglio D 

PROVIDER: S-EPMC7343737 | biostudies-literature | 2020 Aug

REPOSITORIES: biostudies-literature