SPECT Measurement of Benzodiazepine Receptors in Human Brain with Iodine-123-Iomazenil: Kinetic and Equilibrium Paradigms
Iodine-123-iomazenil binding to benzodiazepine receptors in human brain was measured with SPECT using kinetic and equilibrium methods. In the kinetic experiments (n = 6), regional time-activity curves after a single bolus injection of the tracer were fit to a three-compartment model to provide estim...
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| Veröffentlicht in: | The Journal of nuclear medicine (1978) 1994-02, Vol.35 (2), p.228-238 |
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| container_title | The Journal of nuclear medicine (1978) |
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| creator | Abi-Dargham, Anissa Laruelle, Marc Seibyl, John Rattner, Zachary Baldwin, Ronald M Zoghbi, Sami S Zea-Ponce, Yolanda Bremner, J. Douglas Hyde, Thomas M Charney, Dennis S Hoffer, Paul B Innis, Robert B |
| description | Iodine-123-iomazenil binding to benzodiazepine receptors in human brain was measured with SPECT using kinetic and equilibrium methods.
In the kinetic experiments (n = 6), regional time-activity curves after a single bolus injection of the tracer were fit to a three-compartment model to provide estimates of the rate constants K1 to k4. The binding potential (equal to the product of the receptor density and affinity) was derived from the rate constants. In the equilibrium method (n = 8), the tracer bolus injection was followed by a constant tracer infusion to induce a sustained equilibrium state. The regional equilibrium volume of distribution was calculated as the ratio of the regional brain concentration-to-the free parent tracer steady-state plasma concentration. In three experiments, a receptor-saturating dose of flumazenil was injected for direct measurement of the nondisplaceable compartment distribution volume.
The kinetic and equilibrium method results were in good agreement in all regions investigated. Iodine-125-iomazenil binding potential measured in vitro in 12 postmortem samples was found to be consistent with SPECT in vivo measurements.
These studies demonstrated the feasibility of quantification of receptor binding with SPECT. |
| format | Article |
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In the kinetic experiments (n = 6), regional time-activity curves after a single bolus injection of the tracer were fit to a three-compartment model to provide estimates of the rate constants K1 to k4. The binding potential (equal to the product of the receptor density and affinity) was derived from the rate constants. In the equilibrium method (n = 8), the tracer bolus injection was followed by a constant tracer infusion to induce a sustained equilibrium state. The regional equilibrium volume of distribution was calculated as the ratio of the regional brain concentration-to-the free parent tracer steady-state plasma concentration. In three experiments, a receptor-saturating dose of flumazenil was injected for direct measurement of the nondisplaceable compartment distribution volume.
The kinetic and equilibrium method results were in good agreement in all regions investigated. Iodine-125-iomazenil binding potential measured in vitro in 12 postmortem samples was found to be consistent with SPECT in vivo measurements.
These studies demonstrated the feasibility of quantification of receptor binding with SPECT.</description><identifier>ISSN: 0161-5505</identifier><identifier>EISSN: 1535-5667</identifier><identifier>PMID: 8294990</identifier><language>eng</language><publisher>United States: Soc Nuclear Med</publisher><subject>Adult ; Brain Chemistry ; Female ; Flumazenil - analogs & derivatives ; Humans ; Iodine Radioisotopes ; Kinetics ; Male ; Receptors, GABA-A - analysis ; Reference Values ; Tomography, Emission-Computed, Single-Photon</subject><ispartof>The Journal of nuclear medicine (1978), 1994-02, Vol.35 (2), p.228-238</ispartof><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,776,780</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/8294990$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Abi-Dargham, Anissa</creatorcontrib><creatorcontrib>Laruelle, Marc</creatorcontrib><creatorcontrib>Seibyl, John</creatorcontrib><creatorcontrib>Rattner, Zachary</creatorcontrib><creatorcontrib>Baldwin, Ronald M</creatorcontrib><creatorcontrib>Zoghbi, Sami S</creatorcontrib><creatorcontrib>Zea-Ponce, Yolanda</creatorcontrib><creatorcontrib>Bremner, J. Douglas</creatorcontrib><creatorcontrib>Hyde, Thomas M</creatorcontrib><creatorcontrib>Charney, Dennis S</creatorcontrib><creatorcontrib>Hoffer, Paul B</creatorcontrib><creatorcontrib>Innis, Robert B</creatorcontrib><title>SPECT Measurement of Benzodiazepine Receptors in Human Brain with Iodine-123-Iomazenil: Kinetic and Equilibrium Paradigms</title><title>The Journal of nuclear medicine (1978)</title><addtitle>J Nucl Med</addtitle><description>Iodine-123-iomazenil binding to benzodiazepine receptors in human brain was measured with SPECT using kinetic and equilibrium methods.
In the kinetic experiments (n = 6), regional time-activity curves after a single bolus injection of the tracer were fit to a three-compartment model to provide estimates of the rate constants K1 to k4. The binding potential (equal to the product of the receptor density and affinity) was derived from the rate constants. In the equilibrium method (n = 8), the tracer bolus injection was followed by a constant tracer infusion to induce a sustained equilibrium state. The regional equilibrium volume of distribution was calculated as the ratio of the regional brain concentration-to-the free parent tracer steady-state plasma concentration. In three experiments, a receptor-saturating dose of flumazenil was injected for direct measurement of the nondisplaceable compartment distribution volume.
The kinetic and equilibrium method results were in good agreement in all regions investigated. Iodine-125-iomazenil binding potential measured in vitro in 12 postmortem samples was found to be consistent with SPECT in vivo measurements.
These studies demonstrated the feasibility of quantification of receptor binding with SPECT.</description><subject>Adult</subject><subject>Brain Chemistry</subject><subject>Female</subject><subject>Flumazenil - analogs & derivatives</subject><subject>Humans</subject><subject>Iodine Radioisotopes</subject><subject>Kinetics</subject><subject>Male</subject><subject>Receptors, GABA-A - analysis</subject><subject>Reference Values</subject><subject>Tomography, Emission-Computed, Single-Photon</subject><issn>0161-5505</issn><issn>1535-5667</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1994</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpFkEFLwzAcxYsoc04_gpCTt0KTNE3qzY3phopD57mk6b9rRpNuScPYPr0VB57e4_F77_AuojFmlMUsy_hlNE5whmPGEnYd3Xi_TZIkE0KMopEgeZrnyTg6fq3mszV6B-mDAwO2R12NpmBPXaXlCXbaAvoEBbu-cx5pixbBSIumTg7-oPsGLQfSQowJjZedGTpWt4_odch6rZC0FZrvg2516XQwaCWdrPTG-Nvoqpath7uzTqLv5_l6tojfPl6Ws6e3uCGU97FKFVMYKHCOuSpxXqeQZhxTXItSAGDOBDBZsoqqlCoFIhGc8ZwIhjHBmE6ih7_dnev2AXxfGO0VtK200AVf8IymOMV8AO_PYCgNVMXOaSPdsTh_9T_U6E1z0A4KG1QL0v3CW2soK0hBiKA_bfRzwQ</recordid><startdate>19940201</startdate><enddate>19940201</enddate><creator>Abi-Dargham, Anissa</creator><creator>Laruelle, Marc</creator><creator>Seibyl, John</creator><creator>Rattner, Zachary</creator><creator>Baldwin, Ronald M</creator><creator>Zoghbi, Sami S</creator><creator>Zea-Ponce, Yolanda</creator><creator>Bremner, J. Douglas</creator><creator>Hyde, Thomas M</creator><creator>Charney, Dennis S</creator><creator>Hoffer, Paul B</creator><creator>Innis, Robert B</creator><general>Soc Nuclear Med</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>7X8</scope></search><sort><creationdate>19940201</creationdate><title>SPECT Measurement of Benzodiazepine Receptors in Human Brain with Iodine-123-Iomazenil: Kinetic and Equilibrium Paradigms</title><author>Abi-Dargham, Anissa ; Laruelle, Marc ; Seibyl, John ; Rattner, Zachary ; Baldwin, Ronald M ; Zoghbi, Sami S ; Zea-Ponce, Yolanda ; Bremner, J. Douglas ; Hyde, Thomas M ; Charney, Dennis S ; Hoffer, Paul B ; Innis, Robert B</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-h237t-c4c5c1e3e7717cb19f4e467131f8b8ee1758e5ab5d3c43cce8087579285112113</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1994</creationdate><topic>Adult</topic><topic>Brain Chemistry</topic><topic>Female</topic><topic>Flumazenil - analogs & derivatives</topic><topic>Humans</topic><topic>Iodine Radioisotopes</topic><topic>Kinetics</topic><topic>Male</topic><topic>Receptors, GABA-A - analysis</topic><topic>Reference Values</topic><topic>Tomography, Emission-Computed, Single-Photon</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Abi-Dargham, Anissa</creatorcontrib><creatorcontrib>Laruelle, Marc</creatorcontrib><creatorcontrib>Seibyl, John</creatorcontrib><creatorcontrib>Rattner, Zachary</creatorcontrib><creatorcontrib>Baldwin, Ronald M</creatorcontrib><creatorcontrib>Zoghbi, Sami S</creatorcontrib><creatorcontrib>Zea-Ponce, Yolanda</creatorcontrib><creatorcontrib>Bremner, J. Douglas</creatorcontrib><creatorcontrib>Hyde, Thomas M</creatorcontrib><creatorcontrib>Charney, Dennis S</creatorcontrib><creatorcontrib>Hoffer, Paul B</creatorcontrib><creatorcontrib>Innis, Robert B</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>MEDLINE - Academic</collection><jtitle>The Journal of nuclear medicine (1978)</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Abi-Dargham, Anissa</au><au>Laruelle, Marc</au><au>Seibyl, John</au><au>Rattner, Zachary</au><au>Baldwin, Ronald M</au><au>Zoghbi, Sami S</au><au>Zea-Ponce, Yolanda</au><au>Bremner, J. Douglas</au><au>Hyde, Thomas M</au><au>Charney, Dennis S</au><au>Hoffer, Paul B</au><au>Innis, Robert B</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>SPECT Measurement of Benzodiazepine Receptors in Human Brain with Iodine-123-Iomazenil: Kinetic and Equilibrium Paradigms</atitle><jtitle>The Journal of nuclear medicine (1978)</jtitle><addtitle>J Nucl Med</addtitle><date>1994-02-01</date><risdate>1994</risdate><volume>35</volume><issue>2</issue><spage>228</spage><epage>238</epage><pages>228-238</pages><issn>0161-5505</issn><eissn>1535-5667</eissn><abstract>Iodine-123-iomazenil binding to benzodiazepine receptors in human brain was measured with SPECT using kinetic and equilibrium methods.
In the kinetic experiments (n = 6), regional time-activity curves after a single bolus injection of the tracer were fit to a three-compartment model to provide estimates of the rate constants K1 to k4. The binding potential (equal to the product of the receptor density and affinity) was derived from the rate constants. In the equilibrium method (n = 8), the tracer bolus injection was followed by a constant tracer infusion to induce a sustained equilibrium state. The regional equilibrium volume of distribution was calculated as the ratio of the regional brain concentration-to-the free parent tracer steady-state plasma concentration. In three experiments, a receptor-saturating dose of flumazenil was injected for direct measurement of the nondisplaceable compartment distribution volume.
The kinetic and equilibrium method results were in good agreement in all regions investigated. Iodine-125-iomazenil binding potential measured in vitro in 12 postmortem samples was found to be consistent with SPECT in vivo measurements.
These studies demonstrated the feasibility of quantification of receptor binding with SPECT.</abstract><cop>United States</cop><pub>Soc Nuclear Med</pub><pmid>8294990</pmid><tpages>11</tpages></addata></record> |
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| ispartof | The Journal of nuclear medicine (1978), 1994-02, Vol.35 (2), p.228-238 |
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| source | MEDLINE; EZB-FREE-00999 freely available EZB journals |
| subjects | Adult Brain Chemistry Female Flumazenil - analogs & derivatives Humans Iodine Radioisotopes Kinetics Male Receptors, GABA-A - analysis Reference Values Tomography, Emission-Computed, Single-Photon |
| title | SPECT Measurement of Benzodiazepine Receptors in Human Brain with Iodine-123-Iomazenil: Kinetic and Equilibrium Paradigms |
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