What question did this study set out to answer?

Evaluate the suitability of F-JNJ-64413739 as a PET ligand for quantifying P2X7 receptor expression in the brain.

September 27, 2018Open Access

18F-JNJ-64413739, a Novel PET Ligand for the P2X7 Ion Channel: Radiation Dosimetry, Kinetic Modeling, Test-Retest Variability, and Occupancy of the P2X7 Antagonist JNJ-54175446

MKMichel KooleAllen Institute for Brain Science MSMark E. SchmidtJanssen (Belgium)AHAnja HijzenJanssen (Belgium)

Key Points

Evaluate the suitability of F-JNJ-64413739 as a PET ligand for quantifying P2X7 receptor expression in the brain.
Kinetic modeling to assess radioligand behavior
Radiation dosimetry analysis
Test-retest variability evaluation
F-JNJ-64413739 demonstrates effective visualization of P2X7 receptor expression
Significant insights gained into P2X7 antagonists' target engagement
Provides guidance for optimal dose selection in therapeutic applications

Abstract

F-JNJ-64413739 is a suitable PET ligand for the quantification of P2X7R expression in the human brain. It can be used to provide insight into P2X7R expression in health and disease, to evaluate target engagement by P2X7 antagonists, and to guide dose selection.

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