Table 3.
BA/ligand | Tissue/model | Effect | Signaling/mediator | References |
---|---|---|---|---|
DCT | Rat cardiomyocyte | ↓ Contraction | Not known | 43 |
CA | Rat heart | Bradycardia | ↓ Cholinergic stimulation | 44, 45 |
CT | Rat cardiomyocyte; rabbit sinoatrialnode | ↓ action potential duration | ↓ inward Na+ and Ca2+ currents, and ↑ outward K+ currents | 46, 47 |
CT,CG | Neonatal rat cardiomyocytes | ↓ contraction rate, amplitude and synchronization | Altered intracellular calcium dynamics; M2R‐mediated ↓ cAMP | 33, 49, 50 |
UDCA | Mouse heart | ↓ allograft rejection | Immune‐mediated | 58, 59 |
UDCA | Rat cardiac ischemia‐reperfusion model | ↓ myocyte apoptosis | Activation of PI3K‐AKT | 60 |
DCT, CDCT | Rat aorta, portal vein, mesenteric and carotid arteries | Vasodilation | M3R‐mediated NO release;? VDCC activation | 32, 63, 64 |
DCA, DCT, CDCA | Endothelial cells | NO and K+ current generation | ↑ cytoplasmic [Ca2+] | 68 |
LCT, CT, CDCT | Hepatic sinusoidal endothelial cells | NOS up‐regulation and NO generation | TGR5‐mediated cAMP generation | 36 |
LCA | Cerebral arteries | Vasodilation | BKCa activation | 39, 66 |
CDCA | Endothelial cells | NOS up‐regulation | FXR activation | 75 |
GW4064 | Rabbit mesenteric arteries | ↓ NO sensitivity | ↓ generation of cGMP | 76 |
CDCA | Rat pulmonary artery endothelial cells | ↓ ET‐1 expression | FXR activation | 77 |
CDCA GW4064 | Rat aortic smooth muscle cells | ↑ AT2R expression | FXR activation | 78 |
6ECDCA GW4064 | Rat and human aortic smooth muscle cells | ↓ inflammation and migration | ↓ IL‐1β ‐mediated iNOS and COX2 expression | 79 |
INT‐747 | ApoE–/– mice | ↓ aortic plaque area and calcification | ↓ expression of IL‐1β, IL‐6 and CD11b | 80, 81 |
CDCA | Endothelial cells; human esophageal cancer xenograft | ↑ angiogenesis | FXR activation; COX‐2‐dependent VEGF production | 88, 89 |
UDCA | Chick embryo CAM; laser‐induced CNV | ↓ angiogenesis | Not known | 90, 91 |
↓: decreased; ↑: increased; INT‐747 is a synthetic CDCA derivative. GW4064 and 6α‐ethyl‐chenodeoxycholic acid (6ECDCA) are synthetic FXR agonists; CAM: chorioallantoic membrane assay; CNV: choroidalneovascularization ; VDCC: Voltage‐dependent calcium channels