Opposite alterations of 5HT2A receptor brain density in subjects with schizophrenia: relevance of radiotracers pharmacological profile
Translational Psychiatry May 20, 2021 Rebeca Dı́ez-alarcia, Carolina Muguruza, Guadalupe Rivero et al. 27 citations
Serotonin 5-HT2A receptor density in the prefrontal cortex of people with schizophrenia depends on which radiotracer is used to measure it, because different tracers bind different receptor conformations. Using the inverse agonist [18F]altanserin, receptor density appeared decreased; using the agonist [3H]LSD, it appeared increased; and using the antagonist [3H]MDL100907, it was unchanged. These differences were more pronounced in schizophrenia subjects who were antipsychotic-free at death. The findings suggest a shift toward the active functional conformation of the 5-HT2A receptor in schizophrenia, consistent with increased cortical serotonin 2A receptor activity.