Imperial College London
Alternate

Dr David R Owen MD PhD

Faculty of Medicine, Department of Brain Sciences

Reader in Molecular Pharmacology and Experimental Medicine
 
 
 
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Contact

 

+44 (0)20 3313 6195d.owen Website

 
 
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Location

 

G20AICTEM buildingHammersmith Campus

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Summary

 

Publications

Citation

BibTex format

@article{Kobayashi:2017:10.1177/0271678X17699223,
author = {Kobayashi, M and Jiang, T and Telu, S and Zoghbi, SS and Gunn, RN and Rabiner, EA and Owen, DR and Guo, Q and Pike, VW and Innis, RB and Fujita, M},
doi = {10.1177/0271678X17699223},
journal = {Journal of Cerebral Blood Flow and Metabolism},
pages = {393--403},
title = {(11)C-DPA-713 has much greater specific binding to translocator protein 18 kDa (TSPO) in human brain than (11)C-( R)-PK11195},
url = {http://dx.doi.org/10.1177/0271678X17699223},
volume = {38},
year = {2017}
}
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RIS format (EndNote, RefMan)

TY  - JOUR
AB  - Positron emission tomography (PET) radioligands for translocator protein 18 kDa (TSPO) are widely used to measure neuroinflammation, but controversy exists whether second-generation radioligands are superior to the prototypical agent (11)C-( R)-PK11195 in human imaging. This study sought to quantitatively measure the "signal to background" ratio (assessed as binding potential ( BPND)) of (11)C-( R)-PK11195 compared to one of the most promising second-generation radioligands, (11)C-DPA-713. Healthy subjects had dynamic PET scans and arterial blood measurements of radioligand after injection of either (11)C-( R)-PK11195 (16 subjects) or (11)C-DPA-713 (22 subjects). To measure the amount of specific binding, a subset of these subjects was scanned after administration of the TSPO blocking drug XBD173 (30-90 mg PO). (11)C-DPA-713 showed a significant sensitivity to genotype in brain, whereas (11)C-( R)-PK11195 did not. Lassen occupancy plot analysis revealed that the specific binding of (11)C-DPA-713 was much greater than that of (11)C-( R)-PK11195. The BPND in high-affinity binders was about 10-fold higher for (11)C-DPA-713 (7.3) than for (11)C-( R)-PK11195 (0.75). Although the high specific binding of (11)C-DPA-713 suggests it is an ideal ligand to measure TSPO, we also found that its distribution volume increased over time, consistent with the accumulation of radiometabolites in brain.
AU  - Kobayashi,M
AU  - Jiang,T
AU  - Telu,S
AU  - Zoghbi,SS
AU  - Gunn,RN
AU  - Rabiner,EA
AU  - Owen,DR
AU  - Guo,Q
AU  - Pike,VW
AU  - Innis,RB
AU  - Fujita,M
DO  - 10.1177/0271678X17699223
EP  - 403
PY  - 2017///
SN  - 1559-7016
SP  - 393
TI  - (11)C-DPA-713 has much greater specific binding to translocator protein 18 kDa (TSPO) in human brain than (11)C-( R)-PK11195
T2  - Journal of Cerebral Blood Flow and Metabolism
UR  - http://dx.doi.org/10.1177/0271678X17699223
UR  - http://hdl.handle.net/10044/1/51601
VL  - 38
ER  -
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