6-Alkoxyisoindolin-1-one based dopamine D2 partial agonists as potential antipsychotics.

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Favor DA, Powers JJ, White AD, Fitzgerald LW, Groppi V, Serpa KA

6-Alkoxyisoindolin-1-one based dopamine D2 partial agonists as potential antipsychotics.

Bioorg Med Chem Lett. 2010 Oct 1;20(19):5666-9. doi: 10.1016/j.bmcl.2010.08.023. Epub 2010 Aug 8.

PubMed ID

20801650 [ View in PubMed

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Abstract

A series of 6-alkoxyisoindolin-1-ones with a magic shotgun pharmacological profile are presented as potential antipsychotics. The in vitro pharmacological profile includes D(2) partial agonism (30-55%), 5-HT(1A) partial agonism (60-90%), and 5-HT(2A) antagonism. Selected compounds in this series displayed good in vivo activity and potency.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Aripiprazole	5-hydroxytryptamine receptor 1A	Ki (nM)	7	N/A	N/A	Details
Aripiprazole	5-hydroxytryptamine receptor 2A	Ki (nM)	4	N/A	N/A	Details
Aripiprazole	Dopamine D2 receptor	Ki (nM)	4	N/A	N/A	Details