Evaluation of [ 11C]metergoline as a PET radiotracer for 5HTR in nonhuman primates
Metergoline, a serotonin receptor antagonist, was labeled with carbon-11 in order to evaluate its pharmacokinetics and distribution in non-human primates using positron emission tomography. [ 11C]Metergoline had moderate brain uptake and exhibited heterogeneous specific binding, which was blocked by...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry 2010-11, Vol.18 (22), p.7739-7745 |
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| container_title | Bioorganic & medicinal chemistry |
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| creator | Hooker, Jacob M. Kim, Sung Won Reibel, Achim T. Alexoff, David Xu, Youwen Shea, Colleen |
| description | Metergoline, a serotonin receptor antagonist, was labeled with carbon-11 in order to evaluate its pharmacokinetics and distribution in non-human primates using positron emission tomography. [
11C]Metergoline had moderate brain uptake and exhibited heterogeneous specific binding, which was blocked by pretreatment with metergoline and altanserin throughout the cortex. Non-specific binding and insensitivity to changes in synaptic serotonin limit its potential as a PET radiotracer. However, the characterization of [
11C]metergoline pharmacokinetics and binding in the brain and peripheral organs using PET improves our understanding of metergoline drug pharmacology. |
| doi_str_mv | 10.1016/j.bmc.2010.04.039 |
| format | Article |
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11C]Metergoline had moderate brain uptake and exhibited heterogeneous specific binding, which was blocked by pretreatment with metergoline and altanserin throughout the cortex. Non-specific binding and insensitivity to changes in synaptic serotonin limit its potential as a PET radiotracer. However, the characterization of [
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11C]Metergoline had moderate brain uptake and exhibited heterogeneous specific binding, which was blocked by pretreatment with metergoline and altanserin throughout the cortex. Non-specific binding and insensitivity to changes in synaptic serotonin limit its potential as a PET radiotracer. However, the characterization of [
11C]metergoline pharmacokinetics and binding in the brain and peripheral organs using PET improves our understanding of metergoline drug pharmacology.</description><subject>Altanserin</subject><subject>Animals</subject><subject>BASIC BIOLOGICAL SCIENCES</subject><subject>BRAIN</subject><subject>Brain - metabolism</subject><subject>CARBON 11</subject><subject>Carbon Radioisotopes - chemistry</subject><subject>DISTRIBUTION</subject><subject>EVALUATION</subject><subject>LABELLING</subject><subject>Metergoline</subject><subject>Metergoline - chemical synthesis</subject><subject>Metergoline - chemistry</subject><subject>Metergoline - pharmacokinetics</subject><subject>ORGANS</subject><subject>PET</subject><subject>PHARMACOLOGY</subject><subject>POSITRON COMPUTED TOMOGRAPHY</subject><subject>Positron-Emission Tomography</subject><subject>PRIMATES</subject><subject>Protein Binding</subject><subject>RADIATION CHEMISTRY, RADIOCHEMISTRY, AND NUCLEAR CHEMISTRY</subject><subject>Radiopharmaceuticals - chemistry</subject><subject>Radiopharmaceuticals - pharmacokinetics</subject><subject>RECEPTORS</subject><subject>Receptors, Serotonin - chemistry</subject><subject>Receptors, Serotonin - metabolism</subject><subject>SEROTONIN</subject><subject>Tissue Distribution</subject><subject>TRACER TECHNIQUES</subject><subject>UPTAKE</subject><issn>0968-0896</issn><issn>1464-3391</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2010</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kVFrFDEUhYNY7Lb6A3yR4ItPs00ySWaCIJRltUJBKeuTSMgmd7pZZpKazCz47810a2lffAqXfPfcc-9B6C0lS0qovNgvt4NdMlJqwpekVi_QgnLJq7pW9CVaECXbirRKnqKznPeEEMYVfYVOGeGC1qpdoJv1wfSTGX0MOHb4J6Z09WuAEdJt7H0AbDI2-Pt6g5NxPo7JWEi4iwmLq80N9gGHGHbTYAK-S34wI-TX6KQzfYY3D-85-vF5vVldVdffvnxdXV5XVjRirFrlJGecGdmw1nXglFNSME54U7tuSxyvrXSCq9a10jDRdWCJcVJ2rHGO2PocfTrq3k3bAZyFUNz1-t5G-qOj8fr5T_A7fRsPmilBBaFF4P1RIObR62z9CHZnYwhgR10OzOt6hj48TEnx9wR51IPPFvreBIhT1kpw0bSMNoWkR9KmmHOC7tEKJbOc1Htd8tJzXppwXfIqPe-e7vDY8S-gAnw8AlAuefCQZp8QLDifZpsu-v_I_wXb1aV2</recordid><startdate>20101115</startdate><enddate>20101115</enddate><creator>Hooker, Jacob M.</creator><creator>Kim, Sung Won</creator><creator>Reibel, Achim T.</creator><creator>Alexoff, David</creator><creator>Xu, Youwen</creator><creator>Shea, Colleen</creator><general>Elsevier Ltd</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7QO</scope><scope>8FD</scope><scope>FR3</scope><scope>P64</scope><scope>OTOTI</scope><scope>5PM</scope></search><sort><creationdate>20101115</creationdate><title>Evaluation of [ 11C]metergoline as a PET radiotracer for 5HTR in nonhuman primates</title><author>Hooker, Jacob M. ; Kim, Sung Won ; Reibel, Achim T. ; Alexoff, David ; Xu, Youwen ; Shea, Colleen</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c575t-89d64242a6728dfed9d965240473dfb0d43c6d5498d86a25ffec0ad66f27dd0c3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2010</creationdate><topic>Altanserin</topic><topic>Animals</topic><topic>BASIC BIOLOGICAL SCIENCES</topic><topic>BRAIN</topic><topic>Brain - metabolism</topic><topic>CARBON 11</topic><topic>Carbon Radioisotopes - chemistry</topic><topic>DISTRIBUTION</topic><topic>EVALUATION</topic><topic>LABELLING</topic><topic>Metergoline</topic><topic>Metergoline - chemical synthesis</topic><topic>Metergoline - chemistry</topic><topic>Metergoline - pharmacokinetics</topic><topic>ORGANS</topic><topic>PET</topic><topic>PHARMACOLOGY</topic><topic>POSITRON COMPUTED TOMOGRAPHY</topic><topic>Positron-Emission Tomography</topic><topic>PRIMATES</topic><topic>Protein Binding</topic><topic>RADIATION CHEMISTRY, RADIOCHEMISTRY, AND NUCLEAR CHEMISTRY</topic><topic>Radiopharmaceuticals - chemistry</topic><topic>Radiopharmaceuticals - pharmacokinetics</topic><topic>RECEPTORS</topic><topic>Receptors, Serotonin - chemistry</topic><topic>Receptors, Serotonin - metabolism</topic><topic>SEROTONIN</topic><topic>Tissue Distribution</topic><topic>TRACER TECHNIQUES</topic><topic>UPTAKE</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Hooker, Jacob M.</creatorcontrib><creatorcontrib>Kim, Sung Won</creatorcontrib><creatorcontrib>Reibel, Achim T.</creatorcontrib><creatorcontrib>Alexoff, David</creatorcontrib><creatorcontrib>Xu, Youwen</creatorcontrib><creatorcontrib>Shea, Colleen</creatorcontrib><creatorcontrib>BROOKHAVEN NATIONAL LABORATORY (BNL)</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Biotechnology Research Abstracts</collection><collection>Technology Research Database</collection><collection>Engineering Research Database</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>OSTI.GOV</collection><collection>PubMed Central (Full Participant titles)</collection><jtitle>Bioorganic & medicinal chemistry</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Hooker, Jacob M.</au><au>Kim, Sung Won</au><au>Reibel, Achim T.</au><au>Alexoff, David</au><au>Xu, Youwen</au><au>Shea, Colleen</au><aucorp>BROOKHAVEN NATIONAL LABORATORY (BNL)</aucorp><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Evaluation of [ 11C]metergoline as a PET radiotracer for 5HTR in nonhuman primates</atitle><jtitle>Bioorganic & medicinal chemistry</jtitle><addtitle>Bioorg Med Chem</addtitle><date>2010-11-15</date><risdate>2010</risdate><volume>18</volume><issue>22</issue><spage>7739</spage><epage>7745</epage><pages>7739-7745</pages><issn>0968-0896</issn><eissn>1464-3391</eissn><abstract>Metergoline, a serotonin receptor antagonist, was labeled with carbon-11 in order to evaluate its pharmacokinetics and distribution in non-human primates using positron emission tomography. [
11C]Metergoline had moderate brain uptake and exhibited heterogeneous specific binding, which was blocked by pretreatment with metergoline and altanserin throughout the cortex. Non-specific binding and insensitivity to changes in synaptic serotonin limit its potential as a PET radiotracer. However, the characterization of [
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| subjects | Altanserin Animals BASIC BIOLOGICAL SCIENCES BRAIN Brain - metabolism CARBON 11 Carbon Radioisotopes - chemistry DISTRIBUTION EVALUATION LABELLING Metergoline Metergoline - chemical synthesis Metergoline - chemistry Metergoline - pharmacokinetics ORGANS PET PHARMACOLOGY POSITRON COMPUTED TOMOGRAPHY Positron-Emission Tomography PRIMATES Protein Binding RADIATION CHEMISTRY, RADIOCHEMISTRY, AND NUCLEAR CHEMISTRY Radiopharmaceuticals - chemistry Radiopharmaceuticals - pharmacokinetics RECEPTORS Receptors, Serotonin - chemistry Receptors, Serotonin - metabolism SEROTONIN Tissue Distribution TRACER TECHNIQUES UPTAKE |
| title | Evaluation of [ 11C]metergoline as a PET radiotracer for 5HTR in nonhuman primates |
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