Source:http://linkedlifedata.com/resource/pubmed/id/20571518
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
1
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pubmed:dateCreated |
2011-1-4
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pubmed:abstractText |
Positron emission tomography studies of 5-hydroxytryptamine (5-HT)(1A) receptors have hitherto been limited to antagonist radiotracers. Antagonists do not distinguish high/low-affinity conformations of G protein-coupled receptors and are less likely to be sensitive to intrasynaptic serotonin levels. We developed a novel 5-HT(1A) agonist radiotracer [(11)C]CUMI-101. This study evaluates the sensitivity of [(11)C]CUMI-101 binding to increases in intrasynaptic serotonin induced by intravenous citalopram and fenfluramine. Two Papio anubis were scanned, using [(11)C]CUMI-101 intravenous bolus of 4.5 ± 1.5 mCi. Binding potential (BP(F)=B(avail)/K(D)) was measured before (n=10) and 20 minutes after elevation of intrasynaptic serotonin by intravenous citalopram (2 mg/kg, n=3; 4 mg/kg, n=3) and fenfluramine (2.5 mg/kg, n=3) using a metabolite-corrected arterial input function. Occupancy was also estimated by the Lassen graphical approach. Both citalopram and fenfluramine effects were significant for BP(F) (P=0.031, P=0.049, respectively). The Lassen approach estimated 15.0, 30.4, and 23.7% average occupancy after citalopram 2 mg/kg, 4 mg/kg, and fenfluramine 2.5 mg/kg, respectively. [(11)C]CUMI-101 binding is sensitive to a large increase in intrasynaptic serotonin in response to robust pharmacological challenges. These modest changes in BP(F) may make it unlikely that this ligand will detect changes in intrasynaptic 5-HT under physiologic conditions; future work will focus on evaluating its utility in measuring the responsiveness of the 5-HT system to pharmacological challenges.
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pubmed:grant | |
pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/2-(4-(4-(2-methoxyphenyl)piperazin-1...,
http://linkedlifedata.com/resource/pubmed/chemical/Citalopram,
http://linkedlifedata.com/resource/pubmed/chemical/Fenfluramine,
http://linkedlifedata.com/resource/pubmed/chemical/Piperazines,
http://linkedlifedata.com/resource/pubmed/chemical/Radiopharmaceuticals,
http://linkedlifedata.com/resource/pubmed/chemical/Receptor, Serotonin, 5-HT1A,
http://linkedlifedata.com/resource/pubmed/chemical/Serotonin,
http://linkedlifedata.com/resource/pubmed/chemical/Serotonin Uptake Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Triazines
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pubmed:status |
MEDLINE
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pubmed:month |
Jan
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pubmed:issn |
1559-7016
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pubmed:author | |
pubmed:issnType |
Electronic
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pubmed:volume |
31
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
243-9
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pubmed:dateRevised |
2011-4-8
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pubmed:meshHeading |
pubmed-meshheading:20571518-Animals,
pubmed-meshheading:20571518-Binding, Competitive,
pubmed-meshheading:20571518-Citalopram,
pubmed-meshheading:20571518-Fenfluramine,
pubmed-meshheading:20571518-Image Processing, Computer-Assisted,
pubmed-meshheading:20571518-Injections, Intravenous,
pubmed-meshheading:20571518-Male,
pubmed-meshheading:20571518-Papio anubis,
pubmed-meshheading:20571518-Piperazines,
pubmed-meshheading:20571518-Positron-Emission Tomography,
pubmed-meshheading:20571518-Radiopharmaceuticals,
pubmed-meshheading:20571518-Receptor, Serotonin, 5-HT1A,
pubmed-meshheading:20571518-Serotonin,
pubmed-meshheading:20571518-Serotonin Uptake Inhibitors,
pubmed-meshheading:20571518-Synapses,
pubmed-meshheading:20571518-Triazines
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pubmed:year |
2011
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pubmed:articleTitle |
In vivo serotonin-sensitive binding of [11C]CUMI-101: a serotonin 1A receptor agonist positron emission tomography radiotracer.
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pubmed:affiliation |
Department of Psychiatry, Columbia University, College of Physicians and Surgeons, New York, New York 10032, USA. mm2354@columbia.edu
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pubmed:publicationType |
Journal Article,
Research Support, N.I.H., Extramural
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