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Pentagastrin (ICI-50123) Sale

(Synonyms: 五肽胃泌素; ICI-50123) 目录号 : GC32776

A CCK2 receptor agonist

Pentagastrin (ICI-50123) Chemical Structure

Cas No.:5534-95-2

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10mM (in 1mL DMSO)
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5mg
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10mg
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25mg
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50mg
¥2,321.00
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100mg
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产品描述

Pentagastrin is a synthetic polypeptide and cholecystokinin-2 (CCK2) receptor agonist.1 It binds selectively to CCK2 receptors in guinea pig brain over CCK1 receptors in rat pancreas (IC50s = 11 and 1,100 nM, respectively). Pentagastrin increases calcium influx and polyphosphoinositide turnover in rat GH3 pituitary cells (EC50s = 23 and 3.9 nM, respectively). It also increases histidine decarboxylase activity in mucous- and endocrine cell-enriched isolated rabbit fundic mucosal cells (EC50 = 2.9 nM).2 Pentagastrin induces contraction of isolated pig ileum smooth muscle cells in vitro (EC50 = 30 pM).3 It increases gastric acid and pepsin secretion in conscious cats in vivo (ED50s = 1.29 and 57.3 nmol/kg2 per hour, respectively).4 Formulations containing pentagastrin have previously been used as a diagnostic aid to evaluate gastric acid secretory function.

1.Smith, A.J., and Freedman, S.B.CCK-B receptor-mediated stimulation of polyphosphoinositide turnover in GH3 pituitary cells in response to cholecystokinin and pentagastrinLife Sci.58(11)883-895(1996) 2.Hollande, F., Bali, J.P., and Magous, R.Neurohormonal regulation of histamine synthesis in isolated rabbit fundic mucosal cellsAm. J. Physiol.266(3 Pt. 1)G395-G405(1994) 3.Botella, A., Delvaux, M., Berry, P., et al.Cholecystokinin and gastrin induce cell contraction in pig ileum by interacting with different receptor subtypesGastroenterology102(3)779-786(1992) 4.Vagne, M., Collinet, M., Cuber, J.C., et al.Effect of porcine gastrin releasing peptide on gastric secretion and motility and the release of hormonal peptides in conscious cats.Peptides8(3)423-430(1987)

Chemical Properties

Cas No. 5534-95-2 SDF
别名 五肽胃泌素; ICI-50123
Canonical SMILES O=C(N[C@@H](CCSC)C(N[C@@H](CC(O)=O)C(N[C@H](C(N)=O)CC1=CC=CC=C1)=O)=O)[C@@H](NC(CCNC(OC(C)(C)C)=O)=O)CC2=CNC3=C2C=CC=C3
分子式 C37H49N7O9S 分子量 767.89
溶解度 DMSO : ≥ 34 mg/mL (44.28 mM) 储存条件 -20°C, protect from light
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1 mM 1.3023 mL 6.5113 mL 13.0227 mL
5 mM 0.2605 mL 1.3023 mL 2.6045 mL
10 mM 0.1302 mL 0.6511 mL 1.3023 mL
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Research Update

Hemodynamic actions of Pentagastrin

Scand J Gastroenterol 1980;15(1):7-15.PMID:7367825DOI:10.3109/00365528009181424

Pentagastrin (Peptavlon, ICI 50123) is known as a powerful stimulator of gastric acid secretion. Several authors have demonstrated a close relationship between gastric acid secretion and gastric blood flow. In this study the general hemodynamic properties of Pentagastrin were investigated qualitatively and quantitatively. The study was performed on anesthetized mongrel dogs. Blood flow was assessed with non-cannulating electromagnetic flow probes. Pentagastrin was injected intravenously at intervals of 2 min in amounts between 1 ng and 8192 ng/kg, following a logarithmic scale. Pentagastrin dose-dependently increased splanchnic blood flow in a reversed U-shaped manner. The major vasoactivity occurred in two organ areas--the gastric area and the pancreatico-duodenal area. Pentagastrin increased blood flow in these areas to 300% and 350% of initial value, respectively, at a dose of 2-4 microgram/kg. Since heart rate, cardiac output, and arterial pressure were not influenced, Pentagastrin had no general hemodynamic effect. This was confirmed by blood flow measurements in the renal a., common carotid a., and femoral a. It was therefore concluded that the splanchnic blood flow increase was due to an extreme decrease of splanchnic vascular resistance.