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A Pipeline to Investigate the Structures and Signaling Pathways of Sphingosine 1-Phosphate Receptors

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Metabolite Study and Structural Authentication for the First-in-Human Use Sphingosine-1-phosphate Receptor 1

Lin Qiu¹, Hao Jiang¹, Kevin Cho²

¹Department of Radiology, Washington University School of Medicine, Saint Louis, Missouri 63110, United States.

ACS Chemical Neuroscience

|April 18, 2024

Summary

This summary is machine-generated.

The sphingosine-1-phosphate receptor 1 (S1PR1) radiotracer [¹¹C]CS1P1 is promising for neuroinflammation PET imaging. Its major metabolite, N-oxide [¹¹C]TZ82121, does not cross the blood-brain barrier, ensuring accurate quantitative PET data analysis.

Keywords:

N-oxide S1PR1 [11C]CS1P1 [18F]FS1P1 [18F]TZ82121 human clinical study radiometabolite radiosynthesis

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Solid Phase 11C-Methylation, Purification and Formulation for the Production of PET Tracers

Solid Phase 11C-Methylation, Purification and Formulation for the Production of PET Tracers

Published on: October 24, 2019

Area of Science:

Neuroimaging
Radiochemistry
Pharmacology

Background:

Sphingosine-1-phosphate receptor 1 (S1PR1) PET imaging shows promise for neuroinflammation in multiple sclerosis (MS).
The radiotracer [¹¹C]CS1P1 has demonstrated potential in proof-of-concept studies.
Characterizing radiometabolites that cross the blood-brain barrier is crucial for accurate quantitative modeling of neuroimaging tracers.

Purpose of the Study:

To investigate the metabolite profile of [¹¹C]CS1P1 in rats, nonhuman primates, and humans.
To identify and characterize the major lipophilic radiometabolite of [¹¹C]CS1P1.
To determine if the identified radiometabolite enters the brain and affects PET imaging accuracy.

Main Methods:

HPLC radiometabolite analysis of human plasma.
Metabolite characterization in rats using nonradioactive CS1P1, followed by LC/MS analysis.
Synthesis of mono-oxidized CS1P1 derivatives for comparison.
Radiosynthesis of [¹⁸F]TZ82121 for brain penetration studies.
Biodistribution studies in rats and PET imaging in nonhuman primates.

Main Results:

A lipophilic radiometabolite, more lipophilic than [¹¹C]CS1P1, was consistently detected in human, rat, and nonhuman primate plasma.
LC/MS analysis identified the metabolite as N-oxide 1 (TZ82121), resulting from in vivo mono-oxidation of CS1P1.
Synthesized [¹⁸F]TZ82121 did not enter the brain in rats or nonhuman primates, as confirmed by biodistribution and PET imaging.
The N-oxide metabolite [¹¹C]TZ82121 does not confound quantitative PET data analysis.

Conclusions:

The major lipophilic radiometabolite of [¹¹C]CS1P1, N-oxide [¹¹C]TZ82121, does not enter the brain.
[¹¹C]CS1P1 remains a promising S1PR1 radiotracer for CNS imaging.
The characterization of this metabolite validates the quantitative analysis of [¹¹C]CS1P1 PET imaging data.