First evaluation of [11C]R116301 as an in vivo tracer of NK1 receptors in man

S.P.A. Wolfensberger; B.N.M. van Berckel; A.J. Airaksinen; K. Maruyama; M. Lubberink; R. Boellaard; W.D.H. Carey; W. Reddingius; D.J. Veltman; A.D. Windhorst; J.E. Leysen; A.A. Lammertsma

doi:https://doi.org/10.1007/s11307-009-0204-5

First evaluation of [11C]R116301 as an in vivo tracer of NK1 receptors in man

S.P.A. Wolfensberger, B.N.M. van Berckel, A.J. Airaksinen, K. Maruyama, M. Lubberink, R. Boellaard, W.D.H. Carey, W. Reddingius, D.J. Veltman, A.D. Windhorst, J.E. Leysen, A.A. Lammertsma

Research output: Contribution to journal › Article › Academic › peer-review

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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

Original language	English
Pages (from-to)	241-245
Journal	Molecular Imaging and Biology
Volume	11
Issue number	4
DOIs	https://doi.org/10.1007/s11307-009-0204-5
Publication status	Published - 2009

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Wolfensberger, S. P. A., van Berckel, B. N. M., Airaksinen, A. J., Maruyama, K., Lubberink, M., Boellaard, R., Carey, W. D. H., Reddingius, W., Veltman, D. J., Windhorst, A. D., Leysen, J. E., & Lammertsma, A. A. (2009). First evaluation of [11C]R116301 as an in vivo tracer of NK1 receptors in man. Molecular Imaging and Biology, 11(4), 241-245. https://doi.org/10.1007/s11307-009-0204-5

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title = "First evaluation of [11C]R116301 as an in vivo tracer of NK1 receptors in man",

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",

author = "S.P.A. Wolfensberger and {van Berckel}, B.N.M. and A.J. Airaksinen and K. Maruyama and M. Lubberink and R. Boellaard and W.D.H. Carey and W. Reddingius and D.J. Veltman and A.D. Windhorst and J.E. Leysen and A.A. Lammertsma",

year = "2009",

doi = "https://doi.org/10.1007/s11307-009-0204-5",

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T1 - First evaluation of [11C]R116301 as an in vivo tracer of NK1 receptors in man

AU - Wolfensberger, S.P.A.

AU - van Berckel, B.N.M.

AU - Airaksinen, A.J.

AU - Maruyama, K.

AU - Lubberink, M.

AU - Boellaard, R.

AU - Carey, W.D.H.

AU - Reddingius, W.

AU - Veltman, D.J.

AU - Windhorst, A.D.

AU - Leysen, J.E.

AU - Lammertsma, A.A.

PY - 2009

Y1 - 2009

N2 - 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

AB - 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

U2 - https://doi.org/10.1007/s11307-009-0204-5

DO - https://doi.org/10.1007/s11307-009-0204-5

M3 - Article

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SN - 1536-1632

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EP - 245

JO - Molecular Imaging and Biology

JF - Molecular Imaging and Biology

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