A1 Vertaisarvioitu alkuperäisartikkeli tieteellisessä lehdessä
First Evaluation of [C-11]R116301 as an In Vivo Tracer of NK1 Receptors in Man
Tekijät: Wolfensberger Saskia PA, van Berckel Bart NM, Airaksinen Anu J, Maruyama Kaoru, Lubberink Mark, Boellaard Ronald, Carey William DH, Reddingius Wieb, Veltman Dick J, Windhorst Albert D, Leysen Josee E, Lammertsma Adriaan A
Kustantaja: SPRINGER
Julkaisuvuosi: 2009
Journal: Molecular Imaging and Biology
Tietokannassa oleva lehden nimi: MOLECULAR IMAGING AND BIOLOGY
Lehden akronyymi: MOL IMAGING BIOL
Vuosikerta: 11
Numero: 4
Aloitussivu: 241
Lopetussivu: 245
Sivujen määrä: 5
ISSN: 1536-1632
eISSN: 1860-2002
DOI: https://doi.org/10.1007/s11307-009-0204-5
Tiivistelmä
NK1 receptors have been implicated in various neuropsychiatric and other disorders. R116301 is a selective NK1 receptor antagonist. In this pilot study, [C-11]R116301 was evaluated as a potential positron emission tomography (PET) ligand for the NK1 receptor.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.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.These preliminary results indicate that [C-11]R116301 has potential as a radioligand for in vivo assessment of NK1 receptors in the human brain.
NK1 receptors have been implicated in various neuropsychiatric and other disorders. R116301 is a selective NK1 receptor antagonist. In this pilot study, [C-11]R116301 was evaluated as a potential positron emission tomography (PET) ligand for the NK1 receptor.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.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.These preliminary results indicate that [C-11]R116301 has potential as a radioligand for in vivo assessment of NK1 receptors in the human brain.
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