Fluspidine

Fluspidine is a fluorine-18 (¹⁸F) labeled radiotracer used in positron emission tomography (PET) scans to image σ₁ (sigma-1) receptors in the brain and other tissues. Sigma-1 receptors are proteins involved in many neurological and psychiatric processes. They have been linked to pain modulation, psychosis, Alzheimer's disease, and depression.^[1]

Chemical properties

Fluspidine is a small organic compound with a spirocyclic structure. A 2-fluoroethyl group on the molecule carries the fluorine-18. The compound exists as two mirror image enantiomers, called (R)-fluspidine and (S)-fluspidine. These enantiomers have slightly different properties: (R)-fluspidine has about 4-fold higher affinity for the σ₁ receptor than (S)-fluspidine, but (S)-fluspidine is metabolically more stable in the body.^[2]

References

↑ "[¹⁸FFluspidine-A PET Tracer for Imaging of σ₁ Receptors in the Central Nervous System"]. Pharmaceuticals 17 (2): 166. January 2024. doi:10.3390/ph17020166. PMID 38399380.
↑ "Distinctive in vivo kinetics of the new σ1 receptor ligands (R)-(+)- and (S)-(-)-18F-fluspidine in porcine brain". Journal of Nuclear Medicine 55 (10): 1730–1736. October 2014. doi:10.2967/jnumed.114.137562. PMID 25071097.

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[1] "[¹⁸FFluspidine-A PET Tracer for Imaging of σ₁ Receptors in the Central Nervous System"]. Pharmaceuticals 17 (2): 166. January 2024. doi:10.3390/ph17020166. PMID 38399380.

[2] "Distinctive in vivo kinetics of the new σ1 receptor ligands (R)-(+)- and (S)-(-)-18F-fluspidine in porcine brain". Journal of Nuclear Medicine 55 (10): 1730–1736. October 2014. doi:10.2967/jnumed.114.137562. PMID 25071097.

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Fluspidine

Topic: Medicine

Chemical properties

References