5-HT1A Assay(s)

Background Information

Gi-coupled serotonin receptor expressed as somatodendritic autoreceptors on raphe nucleus neurons and postsynaptically in hippocampus and cortex. 5-HT1A autoreceptor desensitization is a proposed mechanism of delayed SSRI therapeutic onset. Partial agonists are approved for anxiety and MDD. 5-HT1A activity contributes to the pharmacological mechanisms of vilazodone, vortioxetine, and aripiprazole.

Family: GPCR
Protein Name: 5-HT1A
Gene Name: HTR1A

Organism: Human
Therapeutic Area: Neuropsychiatry

Assay Information

Validated Assay(s): Gi/o GPCR-GIRK Thallium Flux Assay
Assay type: Cell-based
Method: Fluorescence

Instrumentation: Flexstation
Plate Format: 96-well
Expression: Transient 
Cell type: HEK293

Testing Information

Functional Mode(s): Agonist
Reference compound(s): Serotonin

Serotonin concentration-response curve for the human 5-HT1A Gαi/o GPCR-GIRK thallium flux assay in HEK293 cells.
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