Pentagastrin (ICI-50123)
(Synonyms: 五肽胃泌素; ICI-50123) 目录号 : GC32776A CCK2 receptor agonist
Cas No.:5534-95-2
Sample solution is provided at 25 µL, 10mM.
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- Purity: >98.00%
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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)
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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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
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 |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
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1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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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.