Bibliographic Details
| Title: |
Serotonin 2A receptor agonist binding in the human brain with [11C]Cimbi-36. |
| Authors: |
Ettrup, Anders, da Cunha-Bang, Sophie, McMahon, Brenda, Lehel, Szabolcs, Dyssegaard, Agnete, Skibsted, Anine W, Jørgensen, Louise M, Hansen, Martin, Baandrup, Anders O, Bache, Søren, Svarer, Claus, Kristensen, Jesper L, Gillings, Nic, Madsen, Jacob, Knudsen, Gitte M |
| Source: |
Journal of Cerebral Blood Flow & Metabolism; Jul2014, Vol. 34 Issue 7, p1188-1196, 9p |
| Subject Terms: |
SEROTONIN receptors, SEROTONIN antagonists, RADIOACTIVE substances, BRAIN imaging, POSITRON emission tomography, CLINICAL trials, HEALTH outcome assessment |
| Abstract: |
[11C]Cimbi-36 was recently developed as a selective serotonin 2A (5-HT2A) receptor agonist radioligand for positron emission tomography (PET) brain imaging. Such an agonist PET radioligand may provide a novel, and more functional, measure of the serotonergic system and agonist binding is more likely than antagonist binding to reflect 5-HT levels in vivo. Here, we show data from a first-in-human clinical trial with [11C]Cimbi-36. In 29 healthy volunteers, we found high brain uptake and distribution according to 5-HT2A receptors with [11C]Cimbi-36 PET. The two-tissue compartment model using arterial input measurements provided the most optimal quantification of cerebral [11C]Cimbi-36 binding. Reference tissue modeling was feasible as it induced a negative but predictable bias in [11C]Cimbi-36 PET outcome measures. In five subjects, pretreatment with the 5-HT2A receptor antagonist ketanserin before a second PET scan significantly decreased [11C]Cimbi-36 binding in all cortical regions with no effects in cerebellum. These results confirm that [11C]Cimbi-36 binding is selective for 5-HT2A receptors in the cerebral cortex and that cerebellum is an appropriate reference tissue for quantification of 5-HT2A receptors in the human brain. Thus, we here describe [11C]Cimbi-36 as the first agonist PET radioligand to successfully image and quantify 5-HT2A receptors in the human brain. [ABSTRACT FROM AUTHOR] |
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| Database: |
Complementary Index |
