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Background <p>The metabotropic glutamate receptor 4 (mGlu4) has been proposed as a target for Parkinson’s disease to measure levodopa-induced dyskinesia. [<sup>11</sup>C]PXT012253 is a PET radioligand for mGlu4 (3.4 nM), previously characterized in non-human primates. We aimed to determine the optimal method for quantification, duration for acquisition, and test-retest reliability of the binding parameters for [<sup>11</sup>C]PXT012253 in healthy volunteers.</p> Results <p>Six subjects (4 females) completed. [<sup>11</sup>C]PXT012253 displayed high uptake and rapid wash-out. Unchanged [<sup>11</sup>C]PXT012253 at 20&#xa0;min was 10–20%. <i>V</i><sub>T</sub> in subcortical regions was higher than in cortical regions. 2TC provided better fits than 1TC. <i>V</i><sub>T</sub> by Logan GA and MA1 analysis correlated with that of 2TC-CM. MA1 showed better identifiability and standard error than Logan. The test-retest metrics in pons, putamen and thalamus showed absolute variability of <i>V</i><sub>T</sub>&lt;7% and ICC &gt; 0.93 using the 2TC, Logan and MA1 graphical analyses. Time stability analysis showed that <i>V</i><sub>T</sub> values estimated using 63&#xa0;min of imaging were within 10% of the values obtained with 93&#xa0;min with all three models.</p> Conclusion <p>[<sup>11</sup>C]PXT012253 showed a high brain uptake, with rapid washout and metabolism. <i>V</i><sub>T</sub> was reliably estimated using 2TC, Logan GA and MA1. The test-retest metrics showed high repeatability, indicating [<sup>11</sup>C]PXT012253 to be a suitable PET radioligand for mGlu4.</p>

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Test-retest properties of [11C]PXT012253 as a positron emission tomography (PET) radiotracer in healthy human brain: PET imaging of mGlu4

  • 期刊论文

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  • 发表日期：

    2025年6月14日

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  • Per Stenkrona,
  • Ryosuke Arakawa,
  • Jiamei Guo,
  • Benny Bang-Andersen,
  • Sangram Nag,
  • Mohammad Mahdi Moein,
  • Zhisheng Jia,
  • Zsolt Cselenyi,
  • Christer Halldin,
  • Andrea Varrone

摘要

Background

The metabotropic glutamate receptor 4 (mGlu4) has been proposed as a target for Parkinson’s disease to measure levodopa-induced dyskinesia. [11C]PXT012253 is a PET radioligand for mGlu4 (3.4 nM), previously characterized in non-human primates. We aimed to determine the optimal method for quantification, duration for acquisition, and test-retest reliability of the binding parameters for [11C]PXT012253 in healthy volunteers.

Results

Six subjects (4 females) completed. [11C]PXT012253 displayed high uptake and rapid wash-out. Unchanged [11C]PXT012253 at 20 min was 10–20%. VT in subcortical regions was higher than in cortical regions. 2TC provided better fits than 1TC. VT by Logan GA and MA1 analysis correlated with that of 2TC-CM. MA1 showed better identifiability and standard error than Logan. The test-retest metrics in pons, putamen and thalamus showed absolute variability of VT<7% and ICC > 0.93 using the 2TC, Logan and MA1 graphical analyses. Time stability analysis showed that VT values estimated using 63 min of imaging were within 10% of the values obtained with 93 min with all three models.

Conclusion

[11C]PXT012253 showed a high brain uptake, with rapid washout and metabolism. VT was reliably estimated using 2TC, Logan GA and MA1. The test-retest metrics showed high repeatability, indicating [11C]PXT012253 to be a suitable PET radioligand for mGlu4.