Autoradiographic Mapping of 5-HT1B1D Binding Sites in the Rhesus Monkey Brain Using [carbonyl-11C]zolmitriptan
Joint Authors
Bergström, Mats
Almqvist, Per
Kågedal, Matts
Antoni, Gunnar
Gustafsson, Sven-Åke
Nilsson, Dag
Lindhe, Örjan
Source
International Journal of Molecular Imaging
Issue
Vol. 2011, Issue 2011 (31 Dec. 2011), pp.1-6, 6 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2011-10-12
Country of Publication
Egypt
No. of Pages
6
Main Subjects
Abstract EN
Zolmitriptan is a serotonin 5-HT1B/1D receptor agonist that is an effective and well-tolerated drug for migraine treatment.
In a human positron emission tomography study, [11C]zolmitriptan crossed the blood-brain barrier but no clear pattern of regional uptake was discernable.
The objective of this study was to map the binding of [11C]zolmitriptan in Rhesus monkey brain using whole hemisphere in vitro autoradiography with [11C]zolmitriptan as a radioligand.
In saturation studies, [11C]zolmitriptan showed specific (90%) binding to a population of high-affinity binding sites (Kd 0.95–5.06 nM).
There was regional distribution of binding sites with the highest density in the ventral pallidum, followed by the external globus pallidus, substantia nigra, visual cortex, and nucleus accumbens.
In competitive binding studies with 5-HT1 receptor antagonists, [11C]zolmitriptan binding was blocked by selective 5-HT1B and 5-HT1D ligands in all target areas.
There was no appreciable change in binding with the addition of a 5-HT1A receptor antagonist.
American Psychological Association (APA)
Lindhe, Örjan& Almqvist, Per& Kågedal, Matts& Gustafsson, Sven-Åke& Bergström, Mats& Nilsson, Dag…[et al.]. 2011. Autoradiographic Mapping of 5-HT1B1D Binding Sites in the Rhesus Monkey Brain Using [carbonyl-11C]zolmitriptan. International Journal of Molecular Imaging،Vol. 2011, no. 2011, pp.1-6.
https://search.emarefa.net/detail/BIM-491165
Modern Language Association (MLA)
Lindhe, Örjan…[et al.]. Autoradiographic Mapping of 5-HT1B1D Binding Sites in the Rhesus Monkey Brain Using [carbonyl-11C]zolmitriptan. International Journal of Molecular Imaging No. 2011 (2011), pp.1-6.
https://search.emarefa.net/detail/BIM-491165
American Medical Association (AMA)
Lindhe, Örjan& Almqvist, Per& Kågedal, Matts& Gustafsson, Sven-Åke& Bergström, Mats& Nilsson, Dag…[et al.]. Autoradiographic Mapping of 5-HT1B1D Binding Sites in the Rhesus Monkey Brain Using [carbonyl-11C]zolmitriptan. International Journal of Molecular Imaging. 2011. Vol. 2011, no. 2011, pp.1-6.
https://search.emarefa.net/detail/BIM-491165
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-491165