Ceruletide (Caerulein)
(Synonyms: 雨蛙素; Caerulein; Cerulein; FI-6934) 目录号 : GC30008
Ceruletide (Caerulein) 是一种十肽和有效的胆囊收缩素受体激动剂。
Cas No.:17650-98-5
Sample solution is provided at 25 µL, 10mM.
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| Cell experiment [1]: | |
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Cell lines |
Isolated rat pancreatic glands |
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Preparation Method |
An isolated external perfusion of a rat pancreas included a normal perfusion (KRB, 60 minutes), a long term perfusion (KRB, 240 minutes) and a perfusion (60 minutes) including an additive of the detergents triton x-100 or the cholecystokinin analogue ceruletide (1x10-8 M). |
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Reaction Conditions |
1x10-8 M; 60 or 240 min |
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Applications |
During a perfusion with the cholecystokinin analogue ceruletide (1x108 M), there is an increase of lipase after 30 minutes and an increase of amylase after 50 minutes perfusion. |
| Animal experiment [2]: | |
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Animal models |
Rats |
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Preparation Method |
Rats were i.v. infused for 6 h with either ceruletide (5 μg/kg/h) or ceruletide + Gabexate mesilate (50 mg/kg/h). |
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Dosage form |
5 μg/kg/h; i.v. |
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Applications |
In Gabexate mesilate-treated rats the serum amylase and trypsinogen concentrations were reduced by 60 and 80%, respectively, compared to rats infused with ceruletide alone. |
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References: [1]. Mantke R, et al. Die isolierte extrakorporale Perfusion des Rattenpankreas - Ein Modell zur Untersuchung der Pathophysiologie der akuten Pankreatitis [The isolated perfused rat pancreas - an experimental model for investigation the early events in the pathogenesis of acute pancreatitis]. Zentralbl Chir. 2001 Nov;126(11):929-33. German. [2]. Wisner JR Jr, et al. Gabexate mesilate (FOY) protects against ceruletide-induced acute pancreatitis in the rat. Pancreas. 1987;2(2):181-6. |
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Ceruletide, as a decapeptide and a potent cholecystokinetic agent, has a direct spasmogenic effect on the gallbladder muscle and bile ducts in humans and animals.[1]
In vitro experiment it indicated that at 1, 10, and 100 nmol/L, cerulein induced NF-kB–binding activity in a dose-dependent. But 0.3 nmol/L cerulein had no effect on activation NF-kappaB/Rel.[7]
In vivo, at a dose of 100 μg/kg, ceruletide decreased the rates of spontaneous locomotor activity and rearing, and also inhibited methylphenidate- and methamphetamine-induced hyperactivity in both sham-operated and vagotomized mice to same extent.[2] In vivo efficacy test it shown that rabbits were treated with 8 and 50 μg/kg of ceruletide decreased the plasma homovanillic acid levels, but had no significant differences. 140 and 200 μg/kg ceruletide had remarkable reduction of plasma homovanillic acid.[3] Ceruletide (100 μg/kg, s.c.) influenced the central dopaminergic system, enhanced the central effects of neuroleptics and had the potent therapeutic effects in the clinical trials.[4] In a mouse hypoxia model, treatment with 1-100 μg/kg ceruletide subcutaneously obviously prevented the CO-induced impairment of performance and the amelioration being correlated with the severity of hypoxia.[5] In addition, treatment with 10-300 μg/kg intraperitoneally ceruletide slightly but remarkably decreased the response rate (frequency of shuttles) under a discrete avoidance task in mice.[6]
References:
[1].Vincent ME, et al. Pharmacology, clinical uses, and adverse effects of ceruletide, a cholecystokinetic agent. Pharmacotherapy. 1982 Jul-Aug;2(4):223-34.
[2].Moroji T, Hagino Y. Bilateral subdiaphragmatic vagotomy does not prevent the behavioral effects of systematically administered ceruletide in mice. Neuropeptides. 1987 Apr;9(3):217-24.
[3].Wakata N, et al. Effect of ceruletide on plasma monoamine metabolites in the rabbit. J Neurol Sci. 1991 May;103(1):97-100
[4].Hagino Y, Moroji T. Effect of ceruletide on discriminated avoidance behavior in rats. Neuropeptides. 1987 Nov-Dec;10(4):335-42.
[5].Maurice T, et al. Cholecystokinin-related peptides, after systemic or central administration, prevent carbon monoxide-induced amnesia in mice. J Pharmacol Exp Ther. 1994 May;269(2):665-73.
[6].Kuribara H, et al. Effects of ceruletide, administered singly and in combination with central-acting drugs, on discrete shuttle avoidance response in mice. Jpn J Pharmacol. 1990 Nov;54(3):325-9.
[7].Steinle AU, et al. NF-kappaB/Rel activation in cerulein pancreatitis. Gastroenterology. 1999 Feb;116(2):420-30.
Ceruletide 作为一种十肽和一种有效的胆囊收缩剂，对人类和动物的胆囊肌肉和胆管具有直接的痉挛作用。[1]
体外实验表明，在 1、10 和 100 nmol/L 时，雨蛙素以剂量依赖性方式诱导 NF-kB 结合活性。但0.3 nmol/L的雨蛙素对激活NF-kappaB/Rel没有影响。[7]
在体内，在 100 μg/kg 的剂量下，ceruletide 降低了假手术和迷走神经切断小鼠的自发运动活动和饲养率，并且还在相同程度上抑制了哌醋甲酯和甲基苯丙胺诱导的多动症。[2] 体内药效试验表明，兔用8和50μg/kg的ceruletide处理后血浆高香草酸水平降低，但无显着差异。 140和200 μg/kg ceruletide显着降低血浆高香草酸。[3] Ceruletide (100 μg/kg, s.c.)影响中枢多巴胺能系统，增强精神安定药的中枢作用，具有强效临床试验中的疗效。[4] 在小鼠缺氧模型中，皮下注射 1-100 μg/kg 的 ceruletide 可明显防止 CO 引起的性能损害，并且改善与严重程度相关[5]此外，用 10-300 μg/kg 腹腔注射 ceruletide 治疗小鼠在离散回避任务下的反应率（穿梭频率）略有但显着降低。[ 6]
| Cas No. | 17650-98-5 | SDF | |
| 别名 | 雨蛙素; Caerulein; Cerulein; FI-6934 | ||
| Canonical SMILES | {pGlu}-Gln-Asp-Tyr(SO3H)-Thr-Gly-Trp-Met-Asp-Phe-NH2 | ||
| 分子式 | C58H73N13O21S2 | 分子量 | 1352.41 |
| 溶解度 | DMSO : ≥ 100 mg/mL (73.94 mM); Water : ≥ 100 mg/mL (73.94 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.7394 mL | 3.6971 mL | 7.3942 mL |
| 5 mM | 0.1479 mL | 0.7394 mL | 1.4788 mL |
| 10 mM | 0.0739 mL | 0.3697 mL | 0.7394 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 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
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，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Caerulein (Ceruletide). A review
Acta Gastroenterol Belg 1976;39(5-6):169-85.797214
Ceruletide acts in the abdomen, not in the brain, to produce satiety
Peptides 1984 Nov-Dec;5(6):1149-57.6099563 10.1016/0196-9781(84)90181-5
Ceruletide (Caerulein), a decapeptide extracted from the skin of the frog, Hyla caerulea, is very similar in structure to the C-terminal octapeptide of cholecystokinin (CCK-8). Although ceruletide and CCK-8 act through similar or identical receptors to produce the same visceral effects, previous studies in the rat suggested that peripherally administered ceruletide acted directly on the ventromedial hypothalamic (VMH) area to decrease food intake, but peripherally administered CCK-8 acted at a vagally innervated abdominal site to decrease food intake. Since it is unprecedented for these two peptides to produce the same effect by acting at different sites, we investigated the site of action of ceruletide's satiety effect in the rat and compared it to the site of action of CCK-8. The major results were: (1) intraperitoneal administration of ceruletide and CCK-8 inhibited food intake, but intraventricular administration did not; (2) the satiety effect of ceruletide and CCK-8 was not changed by bilateral lesions of the VMH; and (3) the satiety effect of ceruletide and CCK-8 was abolished or markedly reduced by bilateral abdominal vagotomy. We conclude that ceruletide acts at the same vagally innervated abdominal site to produce satiety as CCK-8 does and that neither peptide acts directly on the VMH area.
Caerulein and its analogues: neuropharmacological properties
Peptides 1985;6 Suppl 3:33-46.3913910 10.1016/0196-9781(85)90348-1
The decapeptide from the frog Hyla caerulea, Caerulein (Caerulein diethylammonium hydrate, Ceruletide, CER) is chemically closely related to the C-terminal octapeptide of cholecystokinin (CCK-8). Like CCK-8, CER and some of its analogues produce many behavioural effects in mammals: inhibition of intake of food and water; antinociception; sedation; catalepsy; ptosis, antistereotypic, anticonvulsive and tremorolytic effects; inhibition of self-stimulation. Effects of CER in man comprise sedation, satiety, changes in mood, analgesia and antipsychotic effects. A modulation of central dopaminergic functions appears to be one possible mechanism of CER and its analogues. A common denominator for all effects of CER is, at present, not evident.
Is Caerulein amphibian CCK?
Peptides 1983 Jul-Aug;4(4):457-62.6606162 10.1016/0196-9781(83)90049-9
The amphibian skin decapeptide Caerulein is structurally related to the mammalian peptides gastrin and CCK, suggesting that the peptides might share a common evolutionary history. It has been suggested that Caerulein is the amphibian counterpart of gastrin and CCK, and that the Amphibia do not possess authentic gastric and CCK. High Performance Liquid Chromatography (HPLC) in conjunction with radioimmunoassay using a caerulein-specific antiserum and C-terminal CCK antisera, was used to characterize CCK-and caerulein-like peptides in amphibian brain and gut. In the brain of Xenopus laevis, two CCK-like peptides were present, one of which was indistinguishable by HPLC from mammalian CCK8. No decapeptide Caerulein was detected in the brain of Xenopus laevis or Rana temporaria. In the stomach of Xenopus and in the intestine of both species studied, CCK-like and caerulein-like peptides were present. The results indicate therefore that the Amphibia possess CCK8-like rather than caerulein-like peptides in brain. In contrast, stomach and intestine contain both CCK-like and caerulein-like peptides, but the latter are however distinguishable from the decapeptide found in skin.