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- Title
First Evaluation of [<sup>11</sup>C]R116301 as an In Vivo Tracer of NK1 Receptors in Man.
- Authors
Bart van Berckel; Mark Lubberink; Ronald Boellaard; William Carey; Wieb Reddingius; Albert Windhorst; Adriaan Lammertsma
- Abstract
Abstract Purpose NK1 receptors have been implicated in various neuropsychiatric and other disorders. R116301 is a selective NK1 receptor antagonist. In this pilot study, [11C]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 [11C]R116301 has potential as a radioligand for in vivo assessment of NK1 receptors in the human brain.
- Subjects
CARBON isotopes; RADIOACTIVE tracers in biology; TACHYKININ antagonists; NEUROPSYCHIATRY; POSITRON emission tomography; SUBSTANCE P antagonists; DRUG administration; BRAIN physiology
- Publication
Molecular Imaging & Biology, 2009, Vol 11, Issue 4, p241
- ISSN
1536-1632
- Publication type
Article