Dataset Information

First-in-human evaluation of [¹¹C]PS13, a novel PET radioligand, to quantify cyclooxygenase-1 in the brain.

ABSTRACT:

Purpose

This study assessed whether the newly developed PET radioligand [¹¹C]PS13, which has shown excellent in vivo selectivity in previous animal studies, could be used to quantify constitutive levels of cyclooxygenase-1 (COX-1) in healthy human brain.

Methods

Brain test-retest scans with concurrent arterial blood samples were obtained in 10 healthy individuals. The one- and unconstrained two-tissue compartment models, as well as the Logan graphical analysis were compared, and test-retest reliability and time-stability of total distribution volume (V_T) were assessed. Correlation analyses were conducted between brain regional V_T and COX-1 transcript levels provided in the Allen Human Brain Atlas.

Results

In the brain, [¹¹C]PS13 showed highest uptake in the hippocampus and occipital cortex. The pericentral cortex also showed relatively higher uptake compared with adjacent neocortices. The two-tissue compartment model showed the best fit in all the brain regions, and the results from the Logan graphical analysis were consistent with those from the two-tissue compartment model. V_T values showed excellent test-retest variability (range 6.0-8.5%) and good reliability (intraclass correlation coefficient range 0.74-0.87). V_T values also showed excellent time-stability in all brain regions, confirming that there was no radiometabolite accumulation and that shorter scans were still able to reliably measure V_T. Significant correlation was observed between V_T and COX-1 transcript levels (r = 0.82, P = 0.007), indicating that [¹¹C]PS13 binding reflects actual COX-1 density in the human brain.

Conclusions

These results from the first-in-human evaluation of the ability of [¹¹C]PS13 to image COX-1 in the brain justifies extending the study to disease populations with neuroinflammation.

Clinical trial registration

NCT03324646 at https://clinicaltrials.gov/ . Registered October 30, 2017. Retrospectively registered.

SUBMITTER: Kim MJ

PROVIDER: S-EPMC8261645 | biostudies-literature | 2020 Dec

REPOSITORIES: biostudies-literature

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Publications

First-in-human evaluation of [<sup>11</sup>C]PS13, a novel PET radioligand, to quantify cyclooxygenase-1 in the brain.

Kim Min-Jeong MJ Lee Jae-Hoon JH Juarez Anaya Fernanda F Hong Jinsoo J Miller William W Telu Sanjay S Singh Prachi P Cortes Michelle Y MY Henry Katharine K Tye George L GL Frankland Michael P MP Montero Santamaria Jose A JA Liow Jeih-San JS Zoghbi Sami S SS Fujita Masahiro M Pike Victor W VW Innis Robert B RB

European journal of nuclear medicine and molecular imaging 20200512 13

<h4>Purpose</h4>This study assessed whether the newly developed PET radioligand [<sup>11</sup>C]PS13, which has shown excellent in vivo selectivity in previous animal studies, could be used to quantify constitutive levels of cyclooxygenase-1 (COX-1) in healthy human brain.<h4>Methods</h4>Brain test-retest scans with concurrent arterial blood samples were obtained in 10 healthy individuals. The one- and unconstrained two-tissue compartment models, as well as the Logan graphical analysis were comp ...[more]

PMID: 32399622

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Dataset Information

First-in-human evaluation of [¹¹C]PS13, a novel PET radioligand, to quantify cyclooxygenase-1 in the brain.

Purpose

Methods

Results

Conclusions

Clinical trial registration

Publications

First-in-human evaluation of [<sup>11</sup>C]PS13, a novel PET radioligand, to quantify cyclooxygenase-1 in the brain.

Similar Datasets

OmicsDI is part of the ELIXIR infrastructure

Tweets

Dataset Information

First-in-human evaluation of [11C]PS13, a novel PET radioligand, to quantify cyclooxygenase-1 in the brain.

Purpose

Methods

Results

Conclusions

Clinical trial registration

Publications

First-in-human evaluation of [&lt;sup&gt;11&lt;/sup&gt;C]PS13, a novel PET radioligand, to quantify cyclooxygenase-1 in the brain.

Similar Datasets

OmicsDI is part of the ELIXIR infrastructure

Tweets

First-in-human evaluation of [¹¹C]PS13, a novel PET radioligand, to quantify cyclooxygenase-1 in the brain.

First-in-human evaluation of [<sup>11</sup>C]PS13, a novel PET radioligand, to quantify cyclooxygenase-1 in the brain.