Pentagastrin (ICI-50123) is a selective agonist of Cholecystokinin B (CCKB) receptor with an IC50 of 11 nM. Pentagastrin enhances gastric mucosal defence mechanisms against acid and protects the gastric mucosa from experimental injury.
IC50&Target
IC50: 11 nM (CCKB receptor)
体外研究
Cholecystokinin receptors on GH3 rat anterior pituitary cells have been characterised using radioligand binding and Ca mobilisation. Competition curve with Pentagastrin (IC50 of 25 nM) is consistent with a population predominantly of CCKB receptors. The selective CCKB receptor agonist, Pentagastrin, (0.1 nM-100 μM) dose dependently increased intracellular Ca with a maximal increase of 2.77-fold. Binding of 50 pM [I]BHCCK to GH 3 cells is dose dependently inhibited by Pentagastrin IC50 of 45 nM. Response to a submaximal dose of the CCKB receptor agonist Pentagastrin (100 nM) was dose dependently blocked by the CCKB receptor antagonist L-365,260.
体内研究
Pentagastrin (80 µg/kg/h; intravenous injection; male Sprague-Dawley rats) treatment protects rat gastric mucosa from acidified aspirin injury. Pentagastrin induces a hyperaemic response to luminal acid challenge, increases mucus gel thickness, and elevates intracellular pH (pHi) during acid challenge.
Animal Model:
Male Sprague-Dawley rats (approximately 200 g)
Dosage:
80 µg/kg/h
Administration:
Intravenous injection
Result:
Protected rat gastric mucosa from acidified aspirin injury. Induced a hyperaemic response to luminal acid challenge, increased mucus gel thickness, and elevated pHi during acid challenge.
分子式
C37H49N7O9S
分子量
767.89
CAS号
5534-95-2
中文名称
五肽胃泌素;五肽胃必素;五肽促胃液素
运输条件
Room temperature in continental US; may vary elsewhere.