Pentagastrin (ICI-50123) is a selective agonist of Cholecystokinin B (CCKB) receptor with an IC50 of 11 nM. Pentagastrin is a synthetic polypeptide that has effects like gastrin when given parenterally, which can cause the secretion and synthesis of salivary proteins.
Pentagastrin (ICI-50123) is identified as a potent, selective antagonist of the Cholecystokinin B (CCKB) receptor, with IC50 values of 11 nM for CCKB and 1100 nM for CCKA receptors. It plays a significant role in enhancing gastric mucosal defense mechanisms against acid and provides protection to the gastric mucosa from experimental damage[1].[2].
体内研究
In vivo experiments with male Sprague-Dawley rats demonstrate that Pentagastrin (administered intravenously at 80 µg/kg/h) effectively protects gastric mucosa from injuries caused by acidified aspirin[2].
体外研究
In vitro studies involving GH3 cells have shown that Pentagastrin increases intracellular calcium levels in a dose-dependent manner, with the maximum increase observed being approximately 2.77-fold at concentrations ranging from 0.1 to 100 μM[1].
Additionally, Pentagastrin demonstrates dose-dependent binding to GH3 cells within the same concentration range[1].
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