TABLE 1

Endogenous ligands and primary biologic activities of NR1 subgroup receptors NR1H1 is the insect ecdysone receptor.

Receptor Major Sites of Expression Endogenous Ligand/Activator Primary Function
LXRα (NR1H3) Liver, intestine, fat, lung, macrophage Oxysterols Cholesterol homeostasis
LXRβ (NR1H2) Broadly expressed Oxysterols Cholesterol homeostasis
FXR (NR1H4) Liver, intestine, kidney Bile acids Bile acid homeostasis
VDR (NR1I1) Intestine, thyroid, kidney 1,25(OH)2D3 Calcium homeostasis
CAR (NR1I2) Liver, intestine, choroid plexus Bile acids,a bilirubina Detoxification
PXR (NR1I3) Liver, intestine Bile acids Detoxification
  • a Elevated levels of bile acids and bilirubin activate CAR indirectly via induction of nuclear translocation, not by functioning directly as agonists