PET technology for drug development in psychiatry.
dopamine D2 receptor
norepinephrine transporter
occupancy
positron emission tomography
serotonin transporter
Journal
Neuropsychopharmacology reports
ISSN: 2574-173X
Titre abrégé: Neuropsychopharmacol Rep
Pays: United States
ID NLM: 101719700
Informations de publication
Date de publication:
06 2020
06 2020
Historique:
received:
09
08
2019
revised:
05
10
2019
accepted:
18
10
2019
pubmed:
29
5
2020
medline:
17
8
2021
entrez:
29
5
2020
Statut:
ppublish
Résumé
Positron emission tomography (PET) is a non-invasive imaging method to measure the molecule in vivo. PET imaging can evaluate the central nervous system drugs as target engagement in the human brain. For antipsychotic drugs, adequate dopamine D2 receptor occupancy ("therapeutic window") is reported to be from 65%-70% to 80% to achieve the antipsychotic effect without extrapyramidal symptoms. For antidepressants, the clinical threshold of serotonin transporter (5-HTT) occupancy is reported to be 70%-80% although the relation between the side effect and 5-HTT occupancy has not yet been established. Evaluation of norepinephrine transporter (NET) occupancy for antidepressant is ongoing as adequate PET radioligands for NET were developed recently. Measurement of the target occupancy has been a key element to evaluate the in vivo target engagement of the drugs. In order to evaluate new drug targets for disease conditions such as negative symptoms/cognitive impairment of schizophrenia and treatment-resistant depression, new PET radioligands need to be developed concurrently with the drug development.
Identifiants
pubmed: 32463584
doi: 10.1002/npr2.12084
pmc: PMC7722687
doi:
Substances chimiques
Antidepressive Agents
0
Antipsychotic Agents
0
DRD2 protein, human
0
Receptors, Dopamine D2
0
Types de publication
Journal Article
Review
Langues
eng
Sous-ensembles de citation
IM
Pagination
114-121Informations de copyright
© 2019 The Authors. Neuropsychopharmacology Reports published by John Wiley & Sons Australia, Ltd on behalf of the Japanese Society of NeuropsychoPharmacology.
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