To further validate its use in positron emission tomography (PET), we studied the binding of [18F]altanserin, a specific 5HT2 radioligand, in the rat brain using in vivo autoradiography. Distribution of [18F]altanserin binding was comparable to the in vitro mapping of 5HT2 receptors reported in the literature. Selective displacers were used to test the reversibility and the selectivity of this radioligand. Specific binding of [18F]altanserin in the rat frontal cortex was quantified by direct counting with an electronic imaging system and by quantification on digitalized autoradiograms. Close results of about 30 pmol/g were obtained with both methods. Our data confirmed that [18F]altanserin is a valid tracer for 5HT2 receptors binding studies.
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http://dx.doi.org/10.1016/s0969-8051(97)00054-1 | DOI Listing |
Br J Psychiatry
December 2024
Neurobiology Research Unit, Copenhagen University Hospital - Rigshospitalet, Copenhagen, Denmark.
Background: Using [F]altanserin, a serotonin 2A receptor (5-HTR) antagonist Positron Emission Tomography (PET) tracer, a positive association between cortical 5-HTR binding and the inward-directed facets of neuroticism has been demonstrated in healthy individuals. Psilocybin, a 5-HTR agonist, shows promise for the treatment of depression, reducing neuroticism and mood symptoms potentially via hypothalamic-pituitary-adrenal (HPA) modulation. 5-HTR and neuroticism are both modulated by HPA axis function.
View Article and Find Full Text PDFBehav Brain Res
July 2024
Clinic of Nuclear Medicine, Medical Faculty, Heinrich-Heine University, Moorenstr. 5, Düsseldorf D-40225, Germany.
Both dopamine (DA) and serotonin (5-HT) play key roles in numerous functions including motor control, stress response and learning. So far, there is scarce or conflicting evidence about the effects of 5-HT1A and 5-HT2A receptor (R) agonists and antagonists on recognition memory in the rat. This also holds for their effect on cerebral DA as well as 5-HT release.
View Article and Find Full Text PDFBr J Pharmacol
April 2024
Department of Pharmacology, University of the Basque Country UPV/EHU, Leioa, Spain.
Background And Purpose: Whereas biased agonism on the 5-HT receptor has been ascribed to hallucinogenic properties of psychedelics, no information about biased inverse agonism on this receptor is available. In schizophrenia, increased 5-HT receptor constitutive activity has been suggested, highlighting the therapeutic relevance of inverse agonism. This study characterized the modulation of G protein activity promoted by different drugs, commonly considered as 5-HT receptor antagonists, in post-mortem human brain cortex.
View Article and Find Full Text PDFBrain Imaging Behav
June 2022
Department of Functional Brain Imaging, Institute for Quantum Medical Science, National Institutes for Quantum Science and Technology, Chiba, 263-8555, Japan.
The tendency to avoid punishment, called behavioral inhibition system, is an essential aspect of motivational behavior. Behavioral inhibition system is related to negative affect, such as anxiety, depression and pain, but its neural basis has not yet been clarified. To clarify the association between individual variations in behavioral inhibition system and brain 5-HT receptor availability and specify which brain networks were involved in healthy male subjects, using [F]altanserin positron emission tomography and resting-state functional magnetic resonance imaging.
View Article and Find Full Text PDFFront Neurosci
August 2021
Clinic of Nuclear Medicine, University Hospital Düsseldorf, Düsseldorf, Germany.
The 5-HT receptor (R) is known to modulate dopamine (DA) release in the mammalian brain. Altanserin (ALT) and 2,5-dimethoxy-4-iodoamphetamine (DOI) act as 5-HTR antagonist and agonist, respectively. In the present study, we assessed the effects of ALT and DOI on motor and exploratory behaviors and on DR binding in the rat brain with imaging methods.
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