Visualisation of loss of 5-HT2A receptors with age in healthy volunteers using [18F]altanserin and positron emission tomographic imaging

  title={Visualisation of loss of 5-HT2A receptors with age in healthy volunteers using [18F]altanserin and positron emission tomographic imaging},
  author={Annemie Rosier and Patrick Dupont and Jozef Peuskens and Guy Bormans and Rik Vandenberghe and Michael Maes and Tjibbe de Groot and Christiaan Schiepers and Alfons Verbruggen and Luc J M Mortelmans},
  journal={Psychiatry Research: Neuroimaging},

Quantification of 5-HT2A Receptors in the Human Brain Using [18F]Altanserin-PET and the Bolus/Infusion Approach

  • L. PinborgKaren H. Adams G. Knudsen
  • Biology
    Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism
  • 2003
It is concluded that 5-HT2A receptor studies can be conducted within 2 h of [18F]altanserin infusion, yielding reliable results.

Greater loss of 5-HT(2A) receptors in midlife than in late life.

5-HT(2A) receptor binding decreases dramatically in a variety of brain regions up through midlife, and there was less decrease in late life than in young healthy subjects.

Analyses of [18F]altanserin bolus injection PET data. II: Consideration of radiolabeled metabolites in humans

The most comprehensive and quantitatively valid analysis for bolus injection [18F]altanserin PET data was the dual‐input method that specifically accounted for BBB‐permeable metabolites, although the Logan analysis was preferred because it provided a good compromise between validity, sensitivity, and reliability of implementation.

Regional binding index of the radiolabeled selective 5-HT2A antagonist 123I-5-I-R91150 in the normal canine brain imaged with single photon emission computed tomography.

  • K. PeremansK. Audenaert R. Dierckx
  • Biology
    Veterinary radiology & ultrasound : the official journal of the American College of Veterinary Radiology and the International Veterinary Radiology Association
  • 2003
The 123I labeled serotonin-2A receptor ligand seems to have similar cortical binding in the normal canine brain, as shown in humans and other animal species, in future studies.

Role and distribution of serotonin type 2A receptors in Alzheimer’s disease

  • Biology, Psychology
  • 2003
A generally decreased neocortical BP in AD was found with a significant regional reduction in the orbitofrontal, prefrontal, lateral frontal, cingulate, sensorimotor, parietal inferior, and occipital region, in line with previous postmortem, in vitro, and PET findings.



Loss of brain 5-HT2 receptors in Alzheimer's disease. In vivo assessment with positron emission tomography and [18F]setoperone.

The results demonstrate that the loss in 5-HT2 receptor binding in the cerebral cortex of patients with Alzheimer's disease, long documented by post-mortem studies, can now be assessed in vivo using PET.

Serotonin 5HT2 Receptor Imaging in the Human Brain Using Positron Emission Tomography and a New Radioligand, [18F]Altanserin: Results in Young Normal Controls

  • B. SadzotC. Lemaire G. Franck
  • Biology, Chemistry
    Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism
  • 1995
The results suggest that [18F]altanserin is selective for S2 receptors in vivo as it is in vitro, and indicate that it is suitable for imaging and quantifying S1 receptors with PET in humans.

[In vivo study of central serotoninergic receptors in man using positron tomography].

11C-labeled-ketanserin, a seratonergic antagonist that has high affinity and selectivity for the 5-HT2 receptors in vitro, is used to characterize in vivo the central serotonergic receptors in humans with positron emission tomography (PET).

A Method for the In Vivo Investigation of the Serotonergic 5‐HT2 Receptors in the Human Cerebral Cortex Using Positron Emission Tomography and 18F‐Labeled Setoperone

These data in humans with PET demonstrate that [18F]setoperone labels with high sensitivity and selectivity 5‐HT2 receptors in the frontal cortex are binding to plasma proteins and is significantly metabolized into several labeled metabolites that are much more hydrophilic than setoperone and, hence, presumably do not cross the blood–brain barrier.

Fluorine-18-altanserin: a radioligand for the study of serotonin receptors with PET: radiolabeling and in vivo biologic behavior in rats.

This radiopharmaceutical appears to be more selective for S2 receptor sites than other ligands available today and allows the study of S2 receptors under in vivo conditions.


D2 dopamine and S2 serotonin receptors were imaged and measured in healthy human subjects by positron emission tomography after intravenous injection of 11C-labeled 3-N-methylspiperone and declined over the age span studied.

Localization of serotonin 5‐HT2 receptors in living human brain by positron emission tomography using N1‐([11C]‐methyl)‐2‐BR‐LSD

The studies indicate that [11C]‐MBL is a selective radioligand that can be used to monitor serotonin 5‐HT2 receptor densities in vivo in most regions of the human brain.

Ligands and tracers for PET studies of the 5-HT system--current status.