Serotonin-releasing agents with reduced off-target effects.
Journal
Molecular psychiatry
ISSN: 1476-5578
Titre abrégé: Mol Psychiatry
Pays: England
ID NLM: 9607835
Informations de publication
Date de publication:
02 2023
02 2023
Historique:
received:
11
03
2022
accepted:
12
10
2022
revised:
06
10
2022
pubmed:
10
11
2022
medline:
11
2
2023
entrez:
9
11
2022
Statut:
ppublish
Résumé
Increasing extracellular levels of serotonin (5-HT) in the brain ameliorates symptoms of depression and anxiety-related disorders, e.g., social phobias and post-traumatic stress disorder. Recent evidence from preclinical and clinical studies established the therapeutic potential of drugs inducing the release of 5-HT via the 5-HT-transporter. Nevertheless, current 5-HT releasing compounds under clinical investigation carry the risk for abuse and deleterious side effects. Here, we demonstrate that S-enantiomers of certain ring-substituted cathinones show preference for the release of 5-HT ex vivo and in vivo, and exert 5-HT-associated effects in preclinical behavioral models. Importantly, the lead cathinone compounds (1) do not induce substantial dopamine release and (2) display reduced off-target activity at vesicular monoamine transporters and 5-HT
Identifiants
pubmed: 36352123
doi: 10.1038/s41380-022-01843-w
pii: 10.1038/s41380-022-01843-w
pmc: PMC9645344
doi:
Substances chimiques
Serotonin
333DO1RDJY
Dopamine
VTD58H1Z2X
Carrier Proteins
0
Types de publication
Journal Article
Research Support, N.I.H., Extramural
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
722-732Informations de copyright
© 2022. The Author(s).
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