The development of PET radioligands for imaging the translocator protein (18 kDa): What have we learned?

The translocator protein (TSPO; 18 kDa), formerly known as the peripheral benzodiazepine receptor (PBR), is minimally expressed in the healthy brain. On the other hand, increased levels of TSPO have been noted in brain disorders for which an immune response is elicited. This increase in TSPO express...

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Veröffentlicht in:Journal of labelled compounds & radiopharmaceuticals 2010-06, Vol.53 (7), p.501-510
Hauptverfasser: Luus, Christopher, Hanani, Raphy, Reynolds, Aaron, Kassiou, Michael
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creator Luus, Christopher
Hanani, Raphy
Reynolds, Aaron
Kassiou, Michael
description The translocator protein (TSPO; 18 kDa), formerly known as the peripheral benzodiazepine receptor (PBR), is minimally expressed in the healthy brain. On the other hand, increased levels of TSPO have been noted in brain disorders for which an immune response is elicited. This increase in TSPO expression has been reported to coincide with the process of microglial activation making the measurement of TSPO density a useful indicator of active brain disease. To this end several new classes of TSPO positron emission tomography radioligands have been developed and evaluated. However, the incomplete pharmacological characterization of the TSPO and its ligands as well as differences in pathophysiology, pharmacology and molecular nature across species and tissue types means that caution must be exercised when comparing data obtained with various TSPO radioligands. A re‐evaluation of our interpretation of imaging data, which better correlates with our current understanding of TSPO pharmacology in disease, requires consideration. Copyright © 2010 John Wiley & Sons, Ltd. Although several new classes of translocator protein (TSPO) (18 kDa) PET radioligands have been developed and evaluated our current understanding of the pharmacology and molecular nature of the TSPO is not completely understood. In this regard, a re‐evaluation of our interpretation of imaging data which better correlates with our current understanding of TSPO pharmacology in disease requires consideration. Copyright © 2010 John Wiley & Sons, Ltd.
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Although several new classes of translocator protein (TSPO) (18 kDa) PET radioligands have been developed and evaluated our current understanding of the pharmacology and molecular nature of the TSPO is not completely understood. In this regard, a re‐evaluation of our interpretation of imaging data which better correlates with our current understanding of TSPO pharmacology in disease requires consideration. Copyright © 2010 John Wiley &amp; Sons, Ltd.</description><identifier>ISSN: 0362-4803</identifier><identifier>EISSN: 1099-1344</identifier><identifier>DOI: 10.1002/jlcr.1752</identifier><language>eng</language><publisher>Chichester, UK: John Wiley &amp; Sons, Ltd</publisher><subject>Biological and medical sciences ; Carbon-11 ; Contrast media. Radiopharmaceuticals ; Fluorine-18 ; Medical sciences ; PBR ; PET ; Pharmacology. 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Although several new classes of translocator protein (TSPO) (18 kDa) PET radioligands have been developed and evaluated our current understanding of the pharmacology and molecular nature of the TSPO is not completely understood. In this regard, a re‐evaluation of our interpretation of imaging data which better correlates with our current understanding of TSPO pharmacology in disease requires consideration. Copyright © 2010 John Wiley &amp; Sons, Ltd.</description><subject>Biological and medical sciences</subject><subject>Carbon-11</subject><subject>Contrast media. Radiopharmaceuticals</subject><subject>Fluorine-18</subject><subject>Medical sciences</subject><subject>PBR</subject><subject>PET</subject><subject>Pharmacology. 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Drug treatments</topic><topic>translocator protein (TSPO)</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Luus, Christopher</creatorcontrib><creatorcontrib>Hanani, Raphy</creatorcontrib><creatorcontrib>Reynolds, Aaron</creatorcontrib><creatorcontrib>Kassiou, Michael</creatorcontrib><collection>Istex</collection><collection>Pascal-Francis</collection><collection>CrossRef</collection><jtitle>Journal of labelled compounds &amp; radiopharmaceuticals</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Luus, Christopher</au><au>Hanani, Raphy</au><au>Reynolds, Aaron</au><au>Kassiou, Michael</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>The development of PET radioligands for imaging the translocator protein (18 kDa): What have we learned?</atitle><jtitle>Journal of labelled compounds &amp; radiopharmaceuticals</jtitle><addtitle>J Label Compd Radiopharm</addtitle><date>2010-06-15</date><risdate>2010</risdate><volume>53</volume><issue>7</issue><spage>501</spage><epage>510</epage><pages>501-510</pages><issn>0362-4803</issn><eissn>1099-1344</eissn><abstract>The translocator protein (TSPO; 18 kDa), formerly known as the peripheral benzodiazepine receptor (PBR), is minimally expressed in the healthy brain. 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Although several new classes of translocator protein (TSPO) (18 kDa) PET radioligands have been developed and evaluated our current understanding of the pharmacology and molecular nature of the TSPO is not completely understood. In this regard, a re‐evaluation of our interpretation of imaging data which better correlates with our current understanding of TSPO pharmacology in disease requires consideration. Copyright © 2010 John Wiley &amp; Sons, Ltd.</abstract><cop>Chichester, UK</cop><pub>John Wiley &amp; Sons, Ltd</pub><doi>10.1002/jlcr.1752</doi><tpages>10</tpages></addata></record>
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subjects Biological and medical sciences
Carbon-11
Contrast media. Radiopharmaceuticals
Fluorine-18
Medical sciences
PBR
PET
Pharmacology. Drug treatments
translocator protein (TSPO)
title The development of PET radioligands for imaging the translocator protein (18 kDa): What have we learned?
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