Pentagastrin (ICI-50123) is a selective agonist of Cholecystokinin B (CCK_B) receptor with an IC₅₀ of 11 nM^[1]. Pentagastrin enhances gastric mucosal defence mechanisms against acid and protects the gastric mucosa from experimental injury^[2].

IC50: 11 nM (CCK_B receptor)^[1]

Cholecystokinin receptors on GH3 rat anterior pituitary cells have been characterised using radioligand binding and Ca²⁺ mobilisation. Competition curve with Pentagastrin (IC₅₀ of 25 nM) is consistent with a population predominantly of CCK_B receptors. The selective CCK_B receptor agonist, Pentagastrin, (0.1 nM-100 μM) dose dependently increased intracellular Ca²⁺ with a maximal increase of 2.77-fold. Binding of 50 pM [¹²⁵I]BHCCK to GH 3 cells is dose dependently inhibited by Pentagastrin IC₅₀ of 45 nM. Response to a submaximal dose of the CCK_B receptor agonist Pentagastrin (100 nM) was dose dependently blocked by the CCK_B receptor antagonist L-365,260^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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 (pH_i) during acid challenge^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

767.89

C₃₇H₄₉N₇O₉S

5534-95-2

五肽胃泌素；五肽胃必素；五肽促胃液素

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*

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• 1.

  请依序添加每种溶剂：;10% DMSO ;; 40% PEG300 ;; 5% Tween-80 ;; 45% saline

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  此方案可获得 ≥ 2.08 mg/mL (2.71 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

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• 2.

  请依序添加每种溶剂：;10% DMSO ;; 90% corn oil

  Solubility: ≥ 2.08 mg/mL (2.71 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (2.71 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [1]. Smith AJ, et al. Characterisation of CCKB receptors on GH3 pituitary cells: receptor activation is linked to Ca2+ mobilisation. Eur J Pharmacol. 1994 Apr 15;267(2):215-23.

  [2]. Tanaka S, et al. Pentagastrin gastroprotection against acid is related to H2 receptor activation but not acid secretion. Gut. 1998 Sep;43(3):334-41.