[3H]RP 62203, a ligand of choice to label in vivo brain 5-HT2 receptors

Fajolles, Christophe; Boireau, A.; Ponchant, M.; Laduron, Pierre M.

doi:10.1016/0014-2999(92)90208-l

Cited by 20 publications

(4 citation statements)

References 15 publications

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“…258 Biodistribution results in rats showed that [ 3 H]RP62203 had high uptake in 5-HT 2 receptor-rich brain regions like the frontal cortex with a high ratio to the cerebellum of 6−7. 259 [ 18 F]RP62203 ([ 11 C]73, Figure 12) was prepared via a three-step route with a radiochemical yield of 5−12% (decay corrected) in 190−230 min. 260 PET imaging in the rat brain showed that the uptake of [ 11 C]73 in the neocortex was 4-fold higher than that of the cerebellum, consistent with 5-HT 2 receptor expression, and the uptake was abolished by pretreatment with ritanserin.…”

Section: Pet Ligands For 5-ht 2a Receptorsmentioning

confidence: 99%

“…The naphthosultam derivative RP62203 (namely, fananserin) is an antagonist of 5-HT 2 receptors with a high affinity of 0.26 nM and displays high selectivity toward α 1 AR ( K i = 38 nM), D 2 , 5-HT 1A ( K i = 70 nM), and 5-HT 3 receptors . Biodistribution results in rats showed that [ 3 H]RP62203 had high uptake in 5-HT 2 receptor-rich brain regions like the frontal cortex with a high ratio to the cerebellum of 6–7 . [ 18 F]RP62203 ([ 11 C] 73 , Figure ) was prepared via a three-step route with a radiochemical yield of 5–12% (decay corrected) in 190–230 min .…”

Section: Pet Ligands For 5-ht2a Receptorsmentioning

confidence: 99%

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Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors

Rong

Chen

et al. 2022

J. Med. Chem.

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Serotonin (5-hydroxytryptamine, 5-HT) and 5-HT receptors (5-HTRs) have crucial roles in various neuropsychiatric disorders and neurodegenerative diseases, making them attractive diagnostic and therapeutic targets. Positron emission tomography (PET) is a noninvasive nuclear molecular imaging technique and is an essential tool in clinical diagnosis and drug discovery. In this context, numerous PET ligands have been developed for "visualizing" 5-HTRs in the brain and translated into human use to study disease mechanisms and/or support drug development. Herein, we present a comprehensive repertoire of 5-HTR PET ligands by focusing on their chemotypes and performance in PET imaging studies. Furthermore, this Perspective summarizes recent 5-HTR-focused drug discovery, including biased agonists and allosteric modulators, which would stimulate the development of more potent and subtype-selective 5-HTR PET ligands and thus further our understanding of 5-HTR biology.

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Section: Pet Ligands For 5-ht 2a Receptorsmentioning

confidence: 99%

Section: Pet Ligands For 5-ht2a Receptorsmentioning

confidence: 99%

Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors

Rong

Chen

et al. 2022

J. Med. Chem.

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“…Given that the SGA amisulpride does not exert any 5-HT 2 -receptor antagonism, and whereas some FGAs (e.g. pipamperone, melperone, and perphenazine) in fact exert some relevant 5-HT 2 -antagonism [28,63] , it seems that the 5-HT 2 / D 2ratio is not suffi cient to explain atypical properties.…”

Section: The 5-ht 2 / D 2 -Ratiomentioning

confidence: 99%

Imaging Studies – Differential Action of Typical and Atypical Antipsychotics in a Network Perspective

Vernaleken

Cumming²,

Gründer³

2008

Pharmacopsychiatry

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Dopamine transmission remains central to our understanding of neurocircuitry models of schizophrenia, and to the mechanism of action of typical antipsychotic medications, which preferentially block D (2)-receptors in striatum. In cerebral cortex, D (2)- and D (1)- mediated transmission modulates information processing, and tunes the activity of the cortico-striato-thalamic loops, in which dopaminergic, glutamatergic, GABAergic and serotonergic projections are integrated and interconnected. Molecular imaging techniques, especially positron emission tomography, have been used to investigate the spatial pattern of the binding properties of antipsychotic medications. We now summarize the state of development of molecular imaging, integrated into a model of schizophrenia emphasizing dysfunction of a complex loop, rather than a discrete abnormality in the basal ganglia, as had been implicitly assumed in the classic dopamine model of psychosis. Finally, hypotheses are proposed to explain differences between first- and second generation antipsychotics with respect of regional selectivity for dopamine and serotonin neurons.

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“…Today, various PET radioligands to study the 5‐HT 2A R system exist and have been evaluated, for example, [ 11 C]ketanserin, [ 18 F]flouroethylketanserin, [ 11 C] N ‐methylspiperone, N 1 ‐([ 11 C]methyl)‐2‐Br‐LSD, [ 18 F]setoperone, [ 18 F]MH.MZ, ( R )‐[ 18 F]MH.MZ, [ 18 F]altanserin, [ 18 F]deuteroaltanserin, [ 11 C]MDL 100907, [ 18 F]fananserin, and [ 11 C]Cimbi‐36 . Paterson et al .…”

Section: Introductionmentioning

confidence: 99%

Current radiosynthesis strategies for 5‐HT_2A receptor PET tracers

Herth

Knudsen

2015

Labelled Comp Radiopharmac

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Serotonin 2A receptors have been implicated in various psychophysiological functions and disorders such as depression, Alzheimer's disease, or schizophrenia. Therefore, neuroimaging of this specific receptor is of significant clinical interest, and it is not surprising that many attempts have been made to develop a suitable 5-HT2A R positron emission tomography-tracer. In this review, we give an overview on the precursor, reference compound synthesis, and the preparation of promising 5-HT2A R radiopharmaceuticals applied in positron emission tomography. We also highlight possible learning outcomes that can be made from these tracer development processes.

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[3H]RP 62203, a ligand of choice to label in vivo brain 5-HT2 receptors

Cited by 20 publications

References 15 publications

Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors

Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors

Imaging Studies – Differential Action of Typical and Atypical Antipsychotics in a Network Perspective

Current radiosynthesis strategies for 5‐HT_2A receptor PET tracers

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[3H]RP 62203, a ligand of choice to label in vivo brain 5-HT2 receptors

Cited by 20 publications

References 15 publications

Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors

Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors

Imaging Studies – Differential Action of Typical and Atypical Antipsychotics in a Network Perspective

Current radiosynthesis strategies for 5‐HT2A receptor PET tracers

Contact Info

Product

Resources

About

Current radiosynthesis strategies for 5‐HT_2A receptor PET tracers