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(R)-[11C]PK11195
- Development stage
- Phase 1
- Lead developer
- ABX
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Positron Emitters → Radiopharmaceuticals, Small Molecules
- Administration
- Intravenous
01
Overview
(R)-[11C]PK11195 is a radiolabeled small molecule used as a positron emission tomography (PET) imaging agent to detect neuroinflammation in the brain. It acts as an antagonist of the translocator protein 18 kDa (TSPO), formerly known as the peripheral benzodiazepine receptor, which is upregulated in activated microglia and other immune cells during neuroinflammatory processes. The compound enables noninvasive visualization and quantification of microglial activation, making it useful for studying various neurological disorders such as multiple sclerosis, Alzheimer's disease, Parkinson's disease, HIV-associated dementia, hepatic encephalopathy, and mitochondrial diseases. Developed over thirty years ago, it remains a prototypical TSPO PET tracer despite newer alternatives with improved signal-to-noise ratios being developed. Its mechanism involves binding to TSPO on the outer mitochondrial membrane in glial cells within inflamed or diseased brain regions[2][4][5][7].
- Other names
- PK11195PK-11195PK 111951-(2-chlorophenyl)-N-methyl-N-(1-methylpropyl)-3-isoquinolinecarboxamide
02
Targets
TSPO (Translocator Protein (18 kDa))
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