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The Novel Pimavanserin Derivative ST-2300 with Histamine H₃ Receptor Affinity Shows Reduced 5-HT_2A Binding, but Maintains Antidepressant- and Anxiolytic-like Properties in Mice.

ABSTRACT: The therapy of depression is challenging and still unsatisfactory despite the presence of many antidepressant drugs on the market. Consequently, there is a continuous need to search for new, safer, and more effective antidepressant therapeutics. Previous studies have suggested a potential association of brain histaminergic/serotoninergic signaling and antidepressant- and anxiolytic-like effects. Here, we evaluated the in vivo antidepressant- and anxiolytic-like effects of the newly developed multiple-active ligand ST-2300. ST-2300 was developed from 5-HT_2A/2C inverse agonist pimavanserin (PIM, ACP-103) and incorporates a histamine H₃ receptor (H₃R) antagonist pharmacophore. Despite its parent compound, ST-2300 showed only moderate serotonin 5-HT_2A

SUBMITTER: Venkatachalam K

PROVIDER: S-EPMC9138994 | biostudies-literature | 2022 May

REPOSITORIES: biostudies-literature

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The Novel Pimavanserin Derivative ST-2300 with Histamine H₃ Receptor Affinity Shows Reduced 5-HT_2A Binding, but Maintains Antidepressant- and Anxiolytic-like Properties in Mice.

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The Novel Pimavanserin Derivative ST-2300 with Histamine H3 Receptor Affinity Shows Reduced 5-HT2A Binding, but Maintains Antidepressant- and Anxiolytic-like Properties in Mice.

OmicsDI is part of the ELIXIR infrastructure

Tweets

The Novel Pimavanserin Derivative ST-2300 with Histamine H₃ Receptor Affinity Shows Reduced 5-HT_2A Binding, but Maintains Antidepressant- and Anxiolytic-like Properties in Mice.