Tarazepide
(Synonyms: 他折派特) 目录号 : GC31477Tarazepide是一种有效且特异性的CCK-A受体拮抗剂。
Cas No.:141374-81-4
Sample solution is provided at 25 µL, 10mM.
Tarazepide is a potent and specific CCK-A receptor antagonist.
Tarazepide decreases duodenal electric activity, reduces interdigestive pancreatic secretion, especially protein; reduces cephalic and early postprandial (milk) induced secretion of bicarbonate and protein.Pancreatic protein secretion to intravenous CCK-8 was little affected by atropine, but was significantly reduced by Tarazepide±Atropine; in contrast, protein secretion to intraduodenal CCK-8 was abolished by Tarazepide or atropine[1]. Leptin is administered to the animals at doses of 0.1, 1.0 or 10.0 μg/kg i.d. Tarazepide (2.5 mg/kg, i.d.), a CCK(1) receptor antagonist, is given to the rats prior to the application of leptin. CCK plasma level is measured by radioimmunoassay (RIA) following administration of leptin to the rats. Intraduodenal administration of leptin (1.0 or 10.0 microg/kg) to the fasted rats significantly and dose-dependently increases pancreatic protein and amylase outputs. Pancreatic secretory responses to leptin were totally abolished by prior capsaicin deactivation of sensory nerves or by pretreatment of the rats with Tarazepide[2].
[1]. Zabielski R, et al. Effects of intraduodenal administration of tarazepide on pancreatic secretion and duodenal EMG in neonatal calves. Regul Pept. 1998 Nov 30;78(1-3):113-23. [2]. Nawrot-Porabka K, et al. Leptin is able to stimulate pancreatic enzyme secretion via activation of duodeno-pancreatic reflex and CCK release. J Physiol Pharmacol. 2004 Jul;55 Suppl 2:47-57.
Animal experiment: | Calve[1] The 5 to 7-day-old Friesian male calves (42.0±1.5 kg body weight) are used. The study is made on four calves. After recording 2 to 3 preprandial (interdigestive) MMC/PPS cycles, Tarazepide suspension (0.05, 0.5 and 5.0 mg/kg body weight), or vehicle alone (1% methylcellulose) is infused intraduodenally (i.d.). |
References: [1]. Zabielski R, et al. Effects of intraduodenal administration of tarazepide on pancreatic secretion and duodenal EMG in neonatal calves. Regul Pept. 1998 Nov 30;78(1-3):113-23. |
Cas No. | 141374-81-4 | SDF | |
别名 | 他折派特 | ||
Canonical SMILES | O=C(C1=CC2=CC=CC3=C2N1CCC3)N[C@@H]4C(N(C)C5=CC=CC=C5C(C6=CC=CC=C6)=N4)=O | ||
分子式 | C28H24N4O2 | 分子量 | 448.52 |
溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg | |
1 mM | 2.2296 mL | 11.1478 mL | 22.2955 mL |
5 mM | 0.4459 mL | 2.2296 mL | 4.4591 mL |
10 mM | 0.223 mL | 1.1148 mL | 2.2296 mL |
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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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工作液浓度: mg/ml;
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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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