AI Article Synopsis
- The study investigates the potential of [(11)C]R116301 as a PET ligand to visualize NK1 receptors in the human brain, which are linked to neuropsychiatric disorders.
- Two dynamic PET scans were conducted on three healthy volunteers, measuring the NK1 receptor signal before and after administering aprepitant, a blocking agent.
- Results showed that aprepitant successfully blocked NK1 receptor signals, indicating that [(11)C]R116301 may be a useful tool for studying these receptors in vivo.
Article Abstract
Purpose: NK1 receptors have been implicated in various neuropsychiatric and other disorders. R116301 is a selective NK1 receptor antagonist. In this pilot study, [(11)C]R116301 was evaluated as a potential positron emission tomography (PET) ligand for the NK1 receptor.
Procedures: Two dynamic PET studies were performed in three normal volunteers before and after a blocking dose of aprepitant. Data were analyzed using striatum to cerebellum standardized uptake value (SUV) ratios.
Results: Baseline SUV ratios at 60-90 min after injection ranged from 1.22 to 1.70. Following aprepitant administration, this specific signal was completely blocked. Aprepitant administration did not significantly affect uptake in cerebellum, confirming the absence of NK1 receptors in cerebellum.
Conclusion: These preliminary results indicate that [(11)C]R116301 has potential as a radioligand for in vivo assessment of NK1 receptors in the human brain.
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Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2693769 | PMC |
| http://dx.doi.org/10.1007/s11307-009-0204-5 | DOI Listing |
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