Human GPBAR1

Figure. Concentration-dependent activation of GPBAR1 by TGR5 agonist

Reporter cells were transfected with either the expression plasmid for human G protein-coupled bile acid receptor 1 (GPBAR1) or the mock plasmid and treated with various concentrations of TGR5 agonist. Data points shown are the mean ± SEM of an experiment (n = 3), and the curve is a fit to Hill equation with an EC50 of 350 nM.

G protein-coupled bile acid receptor 1
Available assay modes
Agonist, Inverse agonist, Antagonist, PAM, NAM
à la carte, Gastrointestinal, Human non-orphan GPCRs

Bile acid receptor

The bile acid receptor (GPBA) responds to bile acids produced during the liver metabolism of cholesterol. Selective agonists are promising drugs for the treatment of metabolic disorders, such as type II diabetes, obesity and atherosclerosis.
Excerpt from IUPHAR/BPS Guide to Pharmacology

Related Receptors

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