Imaging Histamine H3 Receptors with Positron Emission Tomography.
Histamine H3 receptors
Human brain
Pitolisant
Positron emission tomography
Receptor occupancy study
[11C]GSK189254
[11C]MK8278
[11C]TASP457
[18F]FMH3
Journal
Current topics in behavioral neurosciences
ISSN: 1866-3370
Titre abrégé: Curr Top Behav Neurosci
Pays: Germany
ID NLM: 101535383
Informations de publication
Date de publication:
2022
2022
Historique:
pubmed:
30
12
2021
medline:
1
10
2022
entrez:
29
12
2021
Statut:
ppublish
Résumé
Positron emission tomography (PET) provides a unique tool to study the biochemistry of the human brain in vivo. By using PET probes that are binding selectively to certain receptor subtypes, brain PET allows the quantification of receptor levels in various brain areas of human subjects. This approach has the potential to reveal abnormal receptor expressions that may contribute to the physiopathology of some psychiatric and neurological disorders. This approach also has the potential to assist in the drug development process by determining receptor occupancy in vivo allowing selection of proper drug dosage to produce therapeutic effects. Several PET tracers have been developed for histamine H3 receptors (H3R). However, despite the potential of PET to elucidate the role of H3R in vivo, only limited work has been conducted so far. This article reviews the work that has been done in this area. Notably, we will cover the limitations of the first-generation PET radioligand for H3R and present the advantages of novel radioligands that promise an explosion of clinical PET research on the role of H3R in vivo.
Identifiants
pubmed: 34964937
doi: 10.1007/7854_2021_285
doi:
Substances chimiques
Carbon Radioisotopes
0
Receptors, Histamine H3
0
Types de publication
Journal Article
Review
Langues
eng
Sous-ensembles de citation
IM
Pagination
147-167Informations de copyright
© 2021. The Author(s), under exclusive license to Springer Nature Switzerland AG.
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