MOR Assay(s)

Background Information

Gi-coupled opioid receptor mediating the profound analgesic, sedative, euphoric, and respiratory-depressant actions of endogenous beta-endorphin and clinical opiates. Signaling downstream inhibits adenylyl cyclase, closes presynaptic voltage-gated Ca2+ channels, and activates postsynaptic GIRK channels in spinal and supraspinal pain pathways. Primary molecular target of prescription analgesics and opioid use disorder therapies; principal site for opioid dependence, tolerance, and fatal overdose liabilities.

Family: GPCR
Protein Name: MOR
Gene Name: OPRM1

Organism: Human
Therapeutic Area: Pain, Neuropsychiatry

Assay Information

Validated Assay(s): Calcium Assay
Assay type: Cell-based
Method: Fluorescence

Instrumentation: FLIPR
Plate Format: 384-well
Expression: Transient
Cell type: HEK293T

Testing Information

Functional Mode(s): Agonist, Antagonist
Reference compound(s): DAMGO