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[11C]metoclopramide is a Carbon-11 labeled radiopharmaceutical developed as a positron emission tomography (PET) tracer to evaluate the functional activity of the efflux transporter P-glycoprotein (P-gp) at the blood-brain barrier. While the parent compound, metoclopramide, is a well-established dopamine D2 and D3 receptor antagonist used clinically as an antiemetic and prokinetic agent, its use as a radiotracer leverages its status as a P-gp substrate. Developed and extensively studied by researchers at the Medical University of Vienna, [11C]metoclopramide is primarily used in clinical research to investigate the role of P-gp dysfunction in neurodegenerative diseases, particularly Alzheimer's disease, where impaired efflux of amyloid-beta is a key pathological feature. By quantifying the brain uptake of the tracer, clinicians can assess the integrity of the blood-brain barrier's clearance mechanisms.
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