Altanserin
Altanserin is a compound that binds to the 5-HT2A receptor (5-Hydroxytryptamine (serotonin) 2A receptor). Labeled with the isotope fluorine-18 it is used as a radioligand in positron emission tomography (PET) studies of the brain, i.e., studies of the 5-HT2Aneuroreceptors. Besides human neuroimaging studies altanserin has also been used in the study of rats.
An alternative for PET imaging the 5-HT2A receptor is the [11C]MDL 100,907 radioligand. Fluorine-18-altanserin and tritium-MDL 100,907 have shown very comparable binding. Both altanserin and MDL 100,907 are 5-HT2A receptor antagonists. [18F]-setoperone can also be used in PET.
An alternative SPECT radioligand is the [123I]-5-I-R91150 receptor antagonist.
A rapid chemical synthesis of fluorine-18 and H-2 dual-labeled altanserin has been described.
Other ligands for other parts of the serotonin system used in PET studies are, e.g., DASB, ketanserin and WAY-100635.
Human brain mapping studies with altanserin
As of 2007 altanserin is probably not used in clinical routine. However, there have been performed several research-based neuroimaging studies with the compound in humans since the 1990s. Some of these studies have considered methodogical issues such as the reproducibility of the method or whether to use constant infusion or bolus-infusion delivery of altanserin. Other studies have compared altanserin binding to subject variables such as age, personality trait and neuropsychiatric disorder.
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