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. 2020 Nov 30;12(12):3709. doi: 10.3390/nu12123709

Table 6.

Potential drawbacks associated with GPBAR-1 activation.

Site Mechanism(s)/Evidence Model(s)

  • Gallbladder

  • Increased refilling (relaxation of smooth muscle cells) [100]

  • Gallstone formation (likely due to increased gallbladder stasis and cholesterol accumulation in the gallbladder) [101]

  • Targeted deletion of Gpbar-1 protects mice from cholesterol gallstone formation [101]

 Animal

  • Pancreas

  • GPBAR-1 mediated pancreatic damage (pancreatitis) [221]

 Animal

  • Peptidergic neurons of mouse dorsal root ganglia and spinal cord

  • Dermal macrophages that contain opioids

  • Pruritus [222]

  • Analgesia [222]

  • Likely mediated by bile acid activation of GPBAR-1 at specific sites [222]

  • Effects attenuated in GPBAR-1 KO mice and exacerbated in GPBAR-1-Tg mice (overexpressing mouse GPBAR-1) [222]

 Animal

  • Endothelial cells

  • Reduced blood pressure with GPBA-1 agonists [220]

  • Activation of GPBAR-1 in endothelial cells [220]

 Animal

  • Cholangiocytes

  • Increased proliferation [58]

  • Reduced apoptosis [58]

  • Tumorigenesis (cholangiocarcinoma) [58]

 Animal

  • Oesophagus

  • GPBAR-1 highly expressed in oesophageal adenocarcinoma and precancerous lesions (histology) [223]

  • GPBAR-1 stimulation: Increased proliferation in oesophageal adenocarcinoma cells and gastric cancer cells [82,188]

 Human (in vivo, in vitro)