First Evaluation of [11C]R116301 as an In Vivo Tracer of NK1 Receptors in Man
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 stud...
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| Veröffentlicht in: | Molecular imaging and biology 2009-07, Vol.11 (4), p.241-245 |
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| creator | Wolfensberger, Saskia P. A. van Berckel, Bart N. M. Airaksinen, Anu J. Maruyama, Kaoru Lubberink, Mark Boellaard, Ronald Carey, William D. H. Reddingius, Wieb Veltman, Dick J. Windhorst, Albert D. Leysen, Josée E. Lammertsma, Adriaan A. |
| description | 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. |
| doi_str_mv | 10.1007/s11307-009-0204-5 |
| format | Article |
| fullrecord | <record><control><sourceid>proquest_pubme</sourceid><recordid>TN_cdi_pubmedcentral_primary_oai_pubmedcentral_nih_gov_2693769</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>21322158</sourcerecordid><originalsourceid>FETCH-LOGICAL-c498t-ab75b313813c9bbb2f0360c94477152456831c5b56c96fa2aef125cfc3942bad3</originalsourceid><addsrcrecordid>eNp1kV9LHDEUxUOxqF37AXyR4EPfxt6bTDKTl0JZtIr_YNn2pZSQiRk7MpusycxCv71ZdlEr-HDJhfs75-ZyCDlEOEGA6mtC5FAVAKoABmUhPpB9rCUUDIDt5F5wWaDkbI98SukBACtkfJfsoeKcSyH2yfVZF9NAT1emH83QBU9DS38jTv_MMCsBqUnUeHrh6a9uFeg8GuviGrq5RDpz1i2HEBPtPL02_oB8bE2f3OftOyE_z07n0_Pi6vbHxfT7VWFLVQ-FaSrRcOQ1cquapmEtcAlWlWVVoWClkDVHKxohrZKtYca1yIRtLVcla8wdn5BvG9_l2CzcnXV-iKbXy9gtTPyng-n0_xPf_dX3YaWZVLzKNSFftgYxPI4uDXrRJev63ngXxqQZcsZQ1Bk8fgM-hDH6fJxmgFApqEWGcAPZGFKKrn3-CYJeJ6U3SemclF4npdeao9cnvCi20WSAbYCUR_7exZfN77s-AeZ9mus</addsrcrecordid><sourcetype>Open Access Repository</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>201079085</pqid></control><display><type>article</type><title>First Evaluation of [11C]R116301 as an In Vivo Tracer of NK1 Receptors in Man</title><source>MEDLINE</source><source>Springer Nature - Complete Springer Journals</source><creator>Wolfensberger, Saskia P. A. ; van Berckel, Bart N. M. ; Airaksinen, Anu J. ; Maruyama, Kaoru ; Lubberink, Mark ; Boellaard, Ronald ; Carey, William D. H. ; Reddingius, Wieb ; Veltman, Dick J. ; Windhorst, Albert D. ; Leysen, Josée E. ; Lammertsma, Adriaan A.</creator><creatorcontrib>Wolfensberger, Saskia P. A. ; van Berckel, Bart N. M. ; Airaksinen, Anu J. ; Maruyama, Kaoru ; Lubberink, Mark ; Boellaard, Ronald ; Carey, William D. H. ; Reddingius, Wieb ; Veltman, Dick J. ; Windhorst, Albert D. ; Leysen, Josée E. ; Lammertsma, Adriaan A.</creatorcontrib><description>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.</description><identifier>ISSN: 1536-1632</identifier><identifier>EISSN: 1860-2002</identifier><identifier>DOI: 10.1007/s11307-009-0204-5</identifier><identifier>PMID: 19333655</identifier><language>eng</language><publisher>New York: Springer-Verlag</publisher><subject>Adult ; Aprepitant ; Brain - diagnostic imaging ; Brain - metabolism ; Brief ; Brief Article ; Butanols - administration & dosage ; Butanols - pharmacokinetics ; Carbon Isotopes - administration & dosage ; Carbon Isotopes - pharmacokinetics ; Female ; Humans ; Image Processing, Computer-Assisted ; Imaging ; Ligands ; Malates ; Male ; Medicine ; Medicine & Public Health ; Middle Aged ; Morpholines - administration & dosage ; Pilot Projects ; Piperidines ; Positron-Emission Tomography - methods ; Radiology ; Radiopharmaceuticals - administration & dosage ; Radiopharmaceuticals - pharmacokinetics ; Receptors, Neurokinin-1 - metabolism</subject><ispartof>Molecular imaging and biology, 2009-07, Vol.11 (4), p.241-245</ispartof><rights>The Author(s) 2009</rights><rights>Academy of Molecular Imaging 2009</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c498t-ab75b313813c9bbb2f0360c94477152456831c5b56c96fa2aef125cfc3942bad3</citedby><cites>FETCH-LOGICAL-c498t-ab75b313813c9bbb2f0360c94477152456831c5b56c96fa2aef125cfc3942bad3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://link.springer.com/content/pdf/10.1007/s11307-009-0204-5$$EPDF$$P50$$Gspringer$$Hfree_for_read</linktopdf><linktohtml>$$Uhttps://link.springer.com/10.1007/s11307-009-0204-5$$EHTML$$P50$$Gspringer$$Hfree_for_read</linktohtml><link.rule.ids>230,314,777,781,882,27905,27906,41469,42538,51300</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/19333655$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Wolfensberger, Saskia P. A.</creatorcontrib><creatorcontrib>van Berckel, Bart N. M.</creatorcontrib><creatorcontrib>Airaksinen, Anu J.</creatorcontrib><creatorcontrib>Maruyama, Kaoru</creatorcontrib><creatorcontrib>Lubberink, Mark</creatorcontrib><creatorcontrib>Boellaard, Ronald</creatorcontrib><creatorcontrib>Carey, William D. H.</creatorcontrib><creatorcontrib>Reddingius, Wieb</creatorcontrib><creatorcontrib>Veltman, Dick J.</creatorcontrib><creatorcontrib>Windhorst, Albert D.</creatorcontrib><creatorcontrib>Leysen, Josée E.</creatorcontrib><creatorcontrib>Lammertsma, Adriaan A.</creatorcontrib><title>First Evaluation of [11C]R116301 as an In Vivo Tracer of NK1 Receptors in Man</title><title>Molecular imaging and biology</title><addtitle>Mol Imaging Biol</addtitle><addtitle>Mol Imaging Biol</addtitle><description>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.</description><subject>Adult</subject><subject>Aprepitant</subject><subject>Brain - diagnostic imaging</subject><subject>Brain - metabolism</subject><subject>Brief</subject><subject>Brief Article</subject><subject>Butanols - administration & dosage</subject><subject>Butanols - pharmacokinetics</subject><subject>Carbon Isotopes - administration & dosage</subject><subject>Carbon Isotopes - pharmacokinetics</subject><subject>Female</subject><subject>Humans</subject><subject>Image Processing, Computer-Assisted</subject><subject>Imaging</subject><subject>Ligands</subject><subject>Malates</subject><subject>Male</subject><subject>Medicine</subject><subject>Medicine & Public Health</subject><subject>Middle Aged</subject><subject>Morpholines - administration & dosage</subject><subject>Pilot Projects</subject><subject>Piperidines</subject><subject>Positron-Emission Tomography - methods</subject><subject>Radiology</subject><subject>Radiopharmaceuticals - administration & dosage</subject><subject>Radiopharmaceuticals - pharmacokinetics</subject><subject>Receptors, Neurokinin-1 - metabolism</subject><issn>1536-1632</issn><issn>1860-2002</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2009</creationdate><recordtype>article</recordtype><sourceid>C6C</sourceid><sourceid>EIF</sourceid><sourceid>ABUWG</sourceid><sourceid>AFKRA</sourceid><sourceid>AZQEC</sourceid><sourceid>BENPR</sourceid><sourceid>CCPQU</sourceid><sourceid>DWQXO</sourceid><sourceid>GNUQQ</sourceid><recordid>eNp1kV9LHDEUxUOxqF37AXyR4EPfxt6bTDKTl0JZtIr_YNn2pZSQiRk7MpusycxCv71ZdlEr-HDJhfs75-ZyCDlEOEGA6mtC5FAVAKoABmUhPpB9rCUUDIDt5F5wWaDkbI98SukBACtkfJfsoeKcSyH2yfVZF9NAT1emH83QBU9DS38jTv_MMCsBqUnUeHrh6a9uFeg8GuviGrq5RDpz1i2HEBPtPL02_oB8bE2f3OftOyE_z07n0_Pi6vbHxfT7VWFLVQ-FaSrRcOQ1cquapmEtcAlWlWVVoWClkDVHKxohrZKtYca1yIRtLVcla8wdn5BvG9_l2CzcnXV-iKbXy9gtTPyng-n0_xPf_dX3YaWZVLzKNSFftgYxPI4uDXrRJev63ngXxqQZcsZQ1Bk8fgM-hDH6fJxmgFApqEWGcAPZGFKKrn3-CYJeJ6U3SemclF4npdeao9cnvCi20WSAbYCUR_7exZfN77s-AeZ9mus</recordid><startdate>20090701</startdate><enddate>20090701</enddate><creator>Wolfensberger, Saskia P. A.</creator><creator>van Berckel, Bart N. M.</creator><creator>Airaksinen, Anu J.</creator><creator>Maruyama, Kaoru</creator><creator>Lubberink, Mark</creator><creator>Boellaard, Ronald</creator><creator>Carey, William D. 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A. ; van Berckel, Bart N. M. ; Airaksinen, Anu J. ; Maruyama, Kaoru ; Lubberink, Mark ; Boellaard, Ronald ; Carey, William D. 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A.</creatorcontrib><creatorcontrib>van Berckel, Bart N. M.</creatorcontrib><creatorcontrib>Airaksinen, Anu J.</creatorcontrib><creatorcontrib>Maruyama, Kaoru</creatorcontrib><creatorcontrib>Lubberink, Mark</creatorcontrib><creatorcontrib>Boellaard, Ronald</creatorcontrib><creatorcontrib>Carey, William D. H.</creatorcontrib><creatorcontrib>Reddingius, Wieb</creatorcontrib><creatorcontrib>Veltman, Dick J.</creatorcontrib><creatorcontrib>Windhorst, Albert D.</creatorcontrib><creatorcontrib>Leysen, Josée E.</creatorcontrib><creatorcontrib>Lammertsma, Adriaan A.</creatorcontrib><collection>Springer Nature OA Free Journals</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>ProQuest Central (Corporate)</collection><collection>Biotechnology Research Abstracts</collection><collection>Nursing & Allied Health Database</collection><collection>Health & Medical Collection</collection><collection>ProQuest Central (purchase pre-March 2016)</collection><collection>Medical Database (Alumni Edition)</collection><collection>ProQuest Pharma Collection</collection><collection>Technology Research Database</collection><collection>ProQuest SciTech Collection</collection><collection>ProQuest Technology Collection</collection><collection>ProQuest Natural Science Collection</collection><collection>Hospital Premium Collection</collection><collection>Hospital Premium Collection (Alumni Edition)</collection><collection>ProQuest Central (Alumni) (purchase pre-March 2016)</collection><collection>Materials Science & Engineering Collection</collection><collection>ProQuest Central (Alumni Edition)</collection><collection>ProQuest Central UK/Ireland</collection><collection>ProQuest Central Essentials</collection><collection>Biological Science Collection</collection><collection>ProQuest Central</collection><collection>Technology Collection</collection><collection>Natural Science Collection</collection><collection>ProQuest One Community College</collection><collection>ProQuest Central Korea</collection><collection>Engineering Research Database</collection><collection>Health Research Premium Collection</collection><collection>Health Research Premium Collection (Alumni)</collection><collection>ProQuest Central Student</collection><collection>SciTech Premium Collection</collection><collection>ProQuest Health & Medical Complete (Alumni)</collection><collection>Nursing & Allied Health Database (Alumni Edition)</collection><collection>ProQuest Engineering Collection</collection><collection>ProQuest Biological Science Collection</collection><collection>Health & Medical Collection (Alumni Edition)</collection><collection>Medical Database</collection><collection>Biological Science Database</collection><collection>Engineering Database</collection><collection>Nursing & Allied Health Premium</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>ProQuest One Academic Eastern Edition (DO NOT USE)</collection><collection>ProQuest One Academic</collection><collection>ProQuest One Academic UKI Edition</collection><collection>ProQuest Central China</collection><collection>Engineering Collection</collection><collection>Neurosciences Abstracts</collection><collection>PubMed Central (Full Participant titles)</collection><jtitle>Molecular imaging and biology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Wolfensberger, Saskia P. A.</au><au>van Berckel, Bart N. M.</au><au>Airaksinen, Anu J.</au><au>Maruyama, Kaoru</au><au>Lubberink, Mark</au><au>Boellaard, Ronald</au><au>Carey, William D. H.</au><au>Reddingius, Wieb</au><au>Veltman, Dick J.</au><au>Windhorst, Albert D.</au><au>Leysen, Josée E.</au><au>Lammertsma, Adriaan A.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>First Evaluation of [11C]R116301 as an In Vivo Tracer of NK1 Receptors in Man</atitle><jtitle>Molecular imaging and biology</jtitle><stitle>Mol Imaging Biol</stitle><addtitle>Mol Imaging Biol</addtitle><date>2009-07-01</date><risdate>2009</risdate><volume>11</volume><issue>4</issue><spage>241</spage><epage>245</epage><pages>241-245</pages><issn>1536-1632</issn><eissn>1860-2002</eissn><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.</abstract><cop>New York</cop><pub>Springer-Verlag</pub><pmid>19333655</pmid><doi>10.1007/s11307-009-0204-5</doi><tpages>5</tpages><oa>free_for_read</oa></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 1536-1632 |
| ispartof | Molecular imaging and biology, 2009-07, Vol.11 (4), p.241-245 |
| issn | 1536-1632 1860-2002 |
| language | eng |
| recordid | cdi_pubmedcentral_primary_oai_pubmedcentral_nih_gov_2693769 |
| source | MEDLINE; Springer Nature - Complete Springer Journals |
| subjects | Adult Aprepitant Brain - diagnostic imaging Brain - metabolism Brief Brief Article Butanols - administration & dosage Butanols - pharmacokinetics Carbon Isotopes - administration & dosage Carbon Isotopes - pharmacokinetics Female Humans Image Processing, Computer-Assisted Imaging Ligands Malates Male Medicine Medicine & Public Health Middle Aged Morpholines - administration & dosage Pilot Projects Piperidines Positron-Emission Tomography - methods Radiology Radiopharmaceuticals - administration & dosage Radiopharmaceuticals - pharmacokinetics Receptors, Neurokinin-1 - metabolism |
| title | First Evaluation of [11C]R116301 as an In Vivo Tracer of NK1 Receptors in Man |
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