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Table 1 Bile acid receptors, ligands and cardiometabolic physiological effects

From: Bile acids at the cross-roads of gut microbiome–host cardiometabolic interactions

Receptor Natural and synthetic ligands Serum concentration (nM) [107] Relative potency Reported physiological effects
Adiposity glucose metabolism Lipid metabolism Vascular disease HF and HTN
FXR CDCA 380 ↑ BAT [39] ↓ Glucose
↓ Insulin [147]
↓ TAG [147] ↑ RCT [86] ↓ BP [98]
CA 440
DCA 320
LCA < LOD
UDCA 43
WAY-362450 N/A   ↓ TAG [148]
↓ Cholesterol [89, 149]
↓ Atherosclerosis [88, 89]
GW4064 N/A ↑ Glycogen [150]
↑ Insulin sensitivity [151]
↓ Glucose
↓ TAG/FFA
↓ Cholesterol [152,153,154]
↑ RCT [87]
OCA N/A ↑ BAT
↓ WAT [113]
↓ Glucose [113] ↑ LDL [113]
↓ HDL [117]
↑ RCT [155] ↓ BP [78]
Fexaramine N/A ↑ BAT [52] ↓ Glucose
↓ Gluconeogenesis
↓ Insulin [52]
↓ Cholesterol [52]
TGR5 LCA < LOD ↑ BAT
↑ T4 T3 [40]
↓ Glucose
↓ Insulin [40]
↑ NO
↓ Monocyte infiltration [94]
TLCA 0.33
CA 440
DCA 320
CDCA 380
6-EMCA/INT-777 N/A   ↑ BAT
↓ WAT [156]
↑ GLP-1 [156] ↓ TAG/NEFA [156] ↓ Atherosclerosis
↓ Foam cell [93]
  1. BAT brown adipose tissue, WAT white adipose tissue, T4 thyroxine, T3 triiodothyronine, GLP-1 glucagon-like peptide-1, TAG triacylglycerides, FFA free fatty acids, NEFA non-esterified fatty acids, RCT reverse cholesterol transport, NO nitric oxide, BP blood pressure, LOD limit of detection, N/A not applicable