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Pentagastrin
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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 (CCKB) 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
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 CCKB receptors. The selective CCKB 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 CCKB receptor agonist Pentagastrin (100 nM) was dose dependently blocked by the CCKB 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 (pHi) 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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