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Potential of [11C]DASB for measuring endogenous serotonin with PET: binding studies
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmaceutical Biosciences, Division of Pharmacokinetics and Drug Therapy. (Hammarlund-Udenaes)
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2005 (English)In: Nuclear Medicine and Biology, ISSN 0969-8051, E-ISSN 1872-9614, Vol. 32, no 2, 129-136 p.Article in journal (Refereed) Published
Abstract [en]

The serotonin transporter radioligand [11C]-3-amino-4-(2-dimethylaminomethylphenylsulfanyl)-benzonitrile, or [11C]DASB, was examined in order to assess its potential for measuring fluctuations in endogenous serotonin concentrations with positron emission tomography. Binding characteristics of [11C]DASB and the propensity for serotonin to displace the tracer were explored in rat brain homogenates. Experiments showed that serotonin displaced [11C]DASB in vitro. Ex vivo experiments performed after tranylcypromine injection (3 or 15 mg/kg) showed a dose-dependent trend in radioactivity uptake and suggested that serotonin may compete with [11C]DASB for transporter binding.

Place, publisher, year, edition, pages
2005. Vol. 32, no 2, 129-136 p.
Keyword [en]
Aniline Compounds/*pharmacokinetics/*therapeutic use, Animals, Brain/*metabolism/*radionuclide imaging, Feasibility Studies, Male, Metabolic Clearance Rate, Neurotransmitter Agents/metabolism, Organ Specificity, Positron-Emission Tomography/*methods, Protein Binding, Radiopharmaceuticals/diagnostic use/pharmacokinetics, Rats, Rats; Sprague-Dawley, Research Support; Non-U.S. Gov't, Serotonin/*metabolism, Sulfides/*pharmacokinetics/*therapeutic use, Tissue Distribution
National Category
Pharmaceutical Sciences
URN: urn:nbn:se:uu:diva-103242DOI: 10.1016/j.nucmedbio.2004.12.001PubMedID: 15721758OAI: oai:DiVA.org:uu-103242DiVA: diva2:217800
Available from: 2009-05-15 Created: 2009-05-15 Last updated: 2010-05-26Bibliographically approved

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