PET studies of 18F-memantine in healthy volunteers
Previous studies in mice and PET investigations in a Rhesus monkey showed that the regional uptake of 18F-memantine could be blocked by pharmacological doses of memantine and (+)-MK-801. In the present study, the binding characteristics of 18F-memantine was examined in five healthy volunteers. In hu...
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Veröffentlicht in: | Nuclear medicine and biology 2002-02, Vol.29 (2), p.227-231 |
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creator | AMETAMEY, S. M BRUEHLMEIER, M SCHUBIGER, P. A KNEIFEL, S KOKIC, M HONER, M ARIGONI, M BUCK, A BURGER, C SAMNICK, S QUACK, G |
description | Previous studies in mice and PET investigations in a Rhesus monkey showed that the regional uptake of 18F-memantine could be blocked by pharmacological doses of memantine and (+)-MK-801. In the present study, the binding characteristics of 18F-memantine was examined in five healthy volunteers. In humans, 18F-memantine was homogeneously distributed in gray matter i.e. cortex and basal ganglia regions, as well as the cerebellum. No radioactive metabolites were detected in plasma during the time-frame of the PET studies. The uptake of 18F-memantine in receptor-rich regions such as striatum and frontal cortex could be well described by a 1-tissue compartment model. The DV" values of all gray matter regions were similar and ranged from 15 to 20 ml/ml. The white matter showed lower DV" values of 15 +/- 1.4 ml/ml. These results suggest that 18F-memantine distribution in human brain does not reflect the regional NMDA receptor concentration, and therefore, this radioligand is not suitable for the PET imaging of the NMDA receptors. |
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M ; BRUEHLMEIER, M ; SCHUBIGER, P. A ; KNEIFEL, S ; KOKIC, M ; HONER, M ; ARIGONI, M ; BUCK, A ; BURGER, C ; SAMNICK, S ; QUACK, G</creator><creatorcontrib>AMETAMEY, S. M ; BRUEHLMEIER, M ; SCHUBIGER, P. A ; KNEIFEL, S ; KOKIC, M ; HONER, M ; ARIGONI, M ; BUCK, A ; BURGER, C ; SAMNICK, S ; QUACK, G</creatorcontrib><description>Previous studies in mice and PET investigations in a Rhesus monkey showed that the regional uptake of 18F-memantine could be blocked by pharmacological doses of memantine and (+)-MK-801. In the present study, the binding characteristics of 18F-memantine was examined in five healthy volunteers. In humans, 18F-memantine was homogeneously distributed in gray matter i.e. cortex and basal ganglia regions, as well as the cerebellum. No radioactive metabolites were detected in plasma during the time-frame of the PET studies. The uptake of 18F-memantine in receptor-rich regions such as striatum and frontal cortex could be well described by a 1-tissue compartment model. The DV" values of all gray matter regions were similar and ranged from 15 to 20 ml/ml. The white matter showed lower DV" values of 15 +/- 1.4 ml/ml. These results suggest that 18F-memantine distribution in human brain does not reflect the regional NMDA receptor concentration, and therefore, this radioligand is not suitable for the PET imaging of the NMDA receptors.</description><identifier>ISSN: 0969-8051</identifier><identifier>EISSN: 1872-9614</identifier><identifier>PMID: 11823128</identifier><language>eng</language><publisher>Amsterdam: Elsevier</publisher><subject>Adult ; Biological and medical sciences ; Brain - diagnostic imaging ; Brain - metabolism ; Humans ; Investigative techniques, diagnostic techniques (general aspects) ; Male ; Medical sciences ; Memantine - analogs & derivatives ; Memantine - blood ; Memantine - pharmacokinetics ; Nervous system ; Radioligand Assay ; Radionuclide investigations ; Radiopharmaceuticals - blood ; Radiopharmaceuticals - pharmacokinetics ; Receptors, N-Methyl-D-Aspartate - analysis ; Receptors, N-Methyl-D-Aspartate - metabolism ; Reference Values ; Tomography, Emission-Computed</subject><ispartof>Nuclear medicine and biology, 2002-02, Vol.29 (2), p.227-231</ispartof><rights>2002 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=13480254$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/11823128$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>AMETAMEY, S. 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In humans, 18F-memantine was homogeneously distributed in gray matter i.e. cortex and basal ganglia regions, as well as the cerebellum. No radioactive metabolites were detected in plasma during the time-frame of the PET studies. The uptake of 18F-memantine in receptor-rich regions such as striatum and frontal cortex could be well described by a 1-tissue compartment model. The DV" values of all gray matter regions were similar and ranged from 15 to 20 ml/ml. The white matter showed lower DV" values of 15 +/- 1.4 ml/ml. These results suggest that 18F-memantine distribution in human brain does not reflect the regional NMDA receptor concentration, and therefore, this radioligand is not suitable for the PET imaging of the NMDA receptors.</description><subject>Adult</subject><subject>Biological and medical sciences</subject><subject>Brain - diagnostic imaging</subject><subject>Brain - metabolism</subject><subject>Humans</subject><subject>Investigative techniques, diagnostic techniques (general aspects)</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Memantine - analogs & derivatives</subject><subject>Memantine - blood</subject><subject>Memantine - pharmacokinetics</subject><subject>Nervous system</subject><subject>Radioligand Assay</subject><subject>Radionuclide investigations</subject><subject>Radiopharmaceuticals - blood</subject><subject>Radiopharmaceuticals - pharmacokinetics</subject><subject>Receptors, N-Methyl-D-Aspartate - analysis</subject><subject>Receptors, N-Methyl-D-Aspartate - metabolism</subject><subject>Reference Values</subject><subject>Tomography, Emission-Computed</subject><issn>0969-8051</issn><issn>1872-9614</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2002</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpFz81Kw0AUBeBBFFurryDZ6C4wd2YyubOU0lqhoIvuw83kDo3kp2YSoW9vwIqrA4ePA-dKLAFzlToL5lospbMuRZnBQtzF-CklWAPyViwAUGlQuBTqY3NI4jhVNcekDwngNm25pW6sO07qLjkyNePxnHz3zdSNzEO8FzeBmsgPl1yJw3ZzWO_S_fvr2_pln57QYIroiCrygFgZCNpLaV1mVW6NL4PTmZe5rJgchry0nsn7uddQOm80hFKvxPPv7GnovyaOY9HW0XPTUMf9FIscjJp_4AwfL3AqW66K01C3NJyLv5MzeLoAip6aMFDn6_jvtEGpMqN_AOInWqc</recordid><startdate>200202</startdate><enddate>200202</enddate><creator>AMETAMEY, S. 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M</creatorcontrib><creatorcontrib>BRUEHLMEIER, M</creatorcontrib><creatorcontrib>SCHUBIGER, P. A</creatorcontrib><creatorcontrib>KNEIFEL, S</creatorcontrib><creatorcontrib>KOKIC, M</creatorcontrib><creatorcontrib>HONER, M</creatorcontrib><creatorcontrib>ARIGONI, M</creatorcontrib><creatorcontrib>BUCK, A</creatorcontrib><creatorcontrib>BURGER, C</creatorcontrib><creatorcontrib>SAMNICK, S</creatorcontrib><creatorcontrib>QUACK, G</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>MEDLINE - Academic</collection><jtitle>Nuclear medicine and biology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>AMETAMEY, S. M</au><au>BRUEHLMEIER, M</au><au>SCHUBIGER, P. A</au><au>KNEIFEL, S</au><au>KOKIC, M</au><au>HONER, M</au><au>ARIGONI, M</au><au>BUCK, A</au><au>BURGER, C</au><au>SAMNICK, S</au><au>QUACK, G</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>PET studies of 18F-memantine in healthy volunteers</atitle><jtitle>Nuclear medicine and biology</jtitle><addtitle>Nucl Med Biol</addtitle><date>2002-02</date><risdate>2002</risdate><volume>29</volume><issue>2</issue><spage>227</spage><epage>231</epage><pages>227-231</pages><issn>0969-8051</issn><eissn>1872-9614</eissn><abstract>Previous studies in mice and PET investigations in a Rhesus monkey showed that the regional uptake of 18F-memantine could be blocked by pharmacological doses of memantine and (+)-MK-801. In the present study, the binding characteristics of 18F-memantine was examined in five healthy volunteers. In humans, 18F-memantine was homogeneously distributed in gray matter i.e. cortex and basal ganglia regions, as well as the cerebellum. No radioactive metabolites were detected in plasma during the time-frame of the PET studies. The uptake of 18F-memantine in receptor-rich regions such as striatum and frontal cortex could be well described by a 1-tissue compartment model. The DV" values of all gray matter regions were similar and ranged from 15 to 20 ml/ml. The white matter showed lower DV" values of 15 +/- 1.4 ml/ml. These results suggest that 18F-memantine distribution in human brain does not reflect the regional NMDA receptor concentration, and therefore, this radioligand is not suitable for the PET imaging of the NMDA receptors.</abstract><cop>Amsterdam</cop><pub>Elsevier</pub><pmid>11823128</pmid><tpages>5</tpages></addata></record> |
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subjects | Adult Biological and medical sciences Brain - diagnostic imaging Brain - metabolism Humans Investigative techniques, diagnostic techniques (general aspects) Male Medical sciences Memantine - analogs & derivatives Memantine - blood Memantine - pharmacokinetics Nervous system Radioligand Assay Radionuclide investigations Radiopharmaceuticals - blood Radiopharmaceuticals - pharmacokinetics Receptors, N-Methyl-D-Aspartate - analysis Receptors, N-Methyl-D-Aspartate - metabolism Reference Values Tomography, Emission-Computed |
title | PET studies of 18F-memantine in healthy volunteers |
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