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[18F]SP203

Development stage: Phase 1
Lead developer: National Institute of Mental Health
Modality: Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration: Intravenous

Overview

[18F]SP203 is a high-affinity and selective radioligand used for positron emission tomography (PET) imaging of metabotropic glutamate subtype 5 (mGluR5) receptors in the brain. It is a negative allosteric modulator with exceptionally high affinity (IC50 = 36 pM) and potency in a phosphoinositol hydrolysis assay (IC50 = 0.714 pM) for mGluR5. The radioligand shows high brain uptake and quantifiable specific signal, making it effective for assessing brain mGluR5 density in human subjects.

Other names: 3-[2-[2-((18F)fluoranylmethyl)-1,3-thiazol-4-yl]ethynyl]-5-fluorobenzonitrile

Targets

GRM5 (Metabotropic glutamate receptor 5)

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