Forskning
Udskriv Udskriv
Switch language
Region Hovedstaden - en del af Københavns Universitetshospital
Udgivet

Serotonin 2A receptor agonist binding in the human brain with [¹¹C]Cimbi-36

Publikation: Bidrag til tidsskriftTidsskriftartikelForskningpeer review

DOI

  1. Parkinson patients have a presynaptic serotonergic deficit: A dynamic deep brain stimulation PET study

    Publikation: Bidrag til tidsskriftTidsskriftartikelForskningpeer review

  2. False positive rates in positron emission tomography (PET) voxelwise analyses

    Publikation: Bidrag til tidsskriftTidsskriftartikelForskningpeer review

  3. Cerebrovascular effects of glibenclamide investigated using high-resolution magnetic resonance imaging in healthy volunteers

    Publikation: Bidrag til tidsskriftTidsskriftartikelForskningpeer review

  4. High spatiotemporal vessel-specific hemodynamic mapping with multi-echo single-vessel fMRI

    Publikation: Bidrag til tidsskriftTidsskriftartikelForskningpeer review

  1. Hot and cold cognitive disturbances in antidepressant-free patients with major depressive disorder: a NeuroPharm study

    Publikation: Bidrag til tidsskriftTidsskriftartikelForskningpeer review

  2. Structural brain abnormalities associated with cognitive impairments in bipolar disorder

    Publikation: Bidrag til tidsskriftTidsskriftartikelForskningpeer review

  3. NeuroPharm study: EEG wakefulness regulation as a biomarker in MDD

    Publikation: Bidrag til tidsskriftTidsskriftartikelForskningpeer review

  4. Parkinson patients have a presynaptic serotonergic deficit: A dynamic deep brain stimulation PET study

    Publikation: Bidrag til tidsskriftTidsskriftartikelForskningpeer review

Vis graf over relationer

[(11)C]Cimbi-36 was recently developed as a selective serotonin 2A (5-HT(2A)) 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 [(11)C]Cimbi-36. In 29 healthy volunteers, we found high brain uptake and distribution according to 5-HT(2A) receptors with [(11)C]Cimbi-36 PET. The two-tissue compartment model using arterial input measurements provided the most optimal quantification of cerebral [(11)C]Cimbi-36 binding. Reference tissue modeling was feasible as it induced a negative but predictable bias in [(11)C]Cimbi-36 PET outcome measures. In five subjects, pretreatment with the 5-HT(2A) receptor antagonist ketanserin before a second PET scan significantly decreased [(11)C]Cimbi-36 binding in all cortical regions with no effects in cerebellum. These results confirm that [(11)C]Cimbi-36 binding is selective for 5-HT(2A) receptors in the cerebral cortex and that cerebellum is an appropriate reference tissue for quantification of 5-HT(2A) receptors in the human brain. Thus, we here describe [(11)C]Cimbi-36 as the first agonist PET radioligand to successfully image and quantify 5-HT(2A) receptors in the human brain.

OriginalsprogEngelsk
TidsskriftJournal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism
Vol/bind34
Udgave nummer7
Sider (fra-til)1188-96
Antal sider9
ISSN0271-678X
DOI
StatusUdgivet - jul. 2014

ID: 44558452