CCK2 Assay(s)

Background Information

Gq-coupled CCK/gastrin receptor mediating gastric acid secretion in the stomach and anxiogenic effects in the CNS. CCK-4 (tetrapeptide) infusion reliably induces acute panic attacks in humans via CCK2, establishing it as a validated panic disorder target. CCK2 antagonists were developed for panic disorder in clinical trials.

Family: GPCR
Protein Name: CCK2 Receptor
Gene Name: CCKBR

Organism: Human
Therapeutic Area: Metabolic, Neuropsychiatry

Assay Information

Validated Assay(s): cAMP, 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): CCK-8

CCK-8 concentration-response curve for the human CCK2 receptor in a Brilliant Calcium fluorescence assay using HEK293T cells.
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