. 2017 Dec 28;9:102. doi: 10.1186/s13098-017-0299-9

Table 1.

Bile acid receptors, ligands and cardiometabolic physiological effects

Receptor	Natural and synthetic ligands	Serum concentration (nM) [107]	Relative potency	Reported physiological effects
Receptor	Natural and synthetic ligands	Serum concentration (nM) [107]	Relative potency	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 [152–154]	↑ 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]	–

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