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Pentagastrin

CAS No. : 5534-95-2

MCE 站：Pentagastrin

产品活性：Pentagastrin (ICI-50123) 是胆囊收缩素 B (CCK_B) 受体的选择性激动剂，IC₅₀ 为 11 nM。可增强胃粘膜对酸的防御机制，并保护胃粘膜免受损伤。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：Cholecystokinin Receptor

In Vitro: 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.

In Vivo: Pentagastrin (80 ?g/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.

相关产品：Drug Repurposing Compound Library Plus  |  FDA-Approved Drug Library Plus  |  FDA-Approved Drug Library Mini  |  Bioactive Compound Library Plus  |  GPCR/G Protein Compound Library  |  Neuronal Signaling Compound Library  |  FDA-Approved Drug Library  |  Anti-Cancer Compound Library  |  Drug Repurposing Compound Library  |  Endocrinology Compound Library  |  Anti-COVID-19 Compound Library  |  NMPA-Approved Drug Library  |  Neurotransmitter Receptor Compound Library  |  FDA Approved & Pharmacopeial Drug Library  |  Drug-Induced Liver Injury (DILI) Compound Library  |  Ceruletide  |  Gastrin I, human  |  Loxiglumide  |  Sograzepide  |  Lorglumide sodium salt  |  Devazepide  |  Nastorazepide  |  CCK-B Receptor Antagonist 2  |  Proglumide  |  SR 146131  |  CCK-B Receptor Antagonist 1  |  Dexloxiglumide  |  Lintitript  |  Mini Gastrin I, human TFA  |  Gastrin I, rat  |  Tarazepide  |  CCK-A receptor inhibitor 1  |  CHEMBL333994  |  Gastrin/CCK antagonist 1  |  GI 181771

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