Delta Opioid Receptor Assay(s)

Background Information

Gi-coupled opioid receptor with demonstrated antidepressant and anxiolytic activity in preclinical models and early-stage clinical trials. DOR agonists show less respiratory depression and addiction liability than mu-opioid receptor agonists. ADL5859 and ADL5747 advanced to Phase 2 pain trials. A compelling next-generation analgesic target with psychiatric co-indication potential.

Family: GPCR
Protein Name: DOR
Gene Name: OPRD1

Organism: Human
Therapeutic Area: Pain, Neuropsychiatry

Assay Information

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

Instrumentation: Flexstation; Panoptic
Plate Format: 96- or 384-well
Expression: Transient
Cell type: HEK293; HEK293T

Testing Information

Functional Mode(s): Agonist, Antagonist
Reference compound(s): SNC-80

Agonist concentration-response curve for the human delta opioid receptor in a fluorescence-based Gi/o GPCR assay using HEK293 cells.
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