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Ceruletide (Caerulein)

Catalog No.GC30008

Ceruletide (Caerulein) Chemical Structure

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.

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Sample solution is provided at 25 µL, 10mM.

Quality Control

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Protocol

Cell experiment [1]:

Cell lines

Isolated rat pancreatic glands

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).

Reaction Conditions

1x10-8 M; 60 or 240 min

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]:

Animal models

Rats

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).

Dosage form

5 μg/kg/h; i.v.

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.

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.

Background

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.

Chemical Properties

Cas No. 17650-98-5 SDF
Synonyms N/A
Chemical Name N/A
Canonical SMILES {pGlu}-Gln-Asp-Tyr(SO3H)-Thr-Gly-Trp-Met-Asp-Phe-NH2
Formula C58H73N13O21S2 M.Wt 1352.41
Solubility H2O : ≥ 100 mg/mL (73.94 mM);DMSO : ≥ 100 mg/mL (73.94 mM) Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

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Research Update

Bombesin and ceruletide-induced grooming and inhibition of ingestion in the rat

Ann N Y Acad Sci1988;525:201-18.PMID: 3291665DOI: 10.1111/j.1749-6632.1988.tb38606.x

Peptides of diverse structure stimulate grooming in rodents and other mammals. Peptide-induced grooming may be observed in several motivational contexts, with or without strong alternative response tendencies. Bombesin-like peptides elicit grooming route dependently in the rat and hamster, independently of, or concomitantly with, changes in ingestive behaviors or resting. The pattern of body surfaces groomed after i.c.v. BBS is in proportion to the representation of body surfaces in somatosensory but not motor cortex of rat. A bombesin-like peptide may be a neurotransmitter in somatosensory afferent processing, and grooming after i.c.v. BBS may reflect a response to alteration of cutaneous sensation. Bombesin is a putative satiety signal in the control of feeding and ethanol intake, but the satiation effects of systemic BBS can be dissociated from the grooming effect of central BBS. Thus, bombesin may perform independent and site-specific functions in the control of behavior. Grooming produced by BBS is not affected by naloxone, involves a different proportion of motor acts than is observed in normal or ACTH-induced grooming, and no cross-tolerance has been reported between ACTH and BBS in the rat. These properties of bombesin-induced grooming indicate multiple, separable mechanisms of peptide-induced grooming and scratching. Cholecystokinin-like peptide-induced grooming is observed after central injection in the rat and is unaccompanied by changes in feeding or resting. The well-documented satiety action of systemic CCK-like peptides is not accompanied by excessive grooming, so multiple, site-specific behavioral roles are also indicated for CCK-like peptides in control of behavior. CCK-8 exhibits short-term cross-tolerance with ACTH in elicitation of grooming, and central CCK-8 is co-localized with CRF and stimulates ACTH and corticosterone release in the rat. Thus, CCK-8 may induce grooming by increasing CRF or ACTH activity. These properties of CCK-like peptide-induced grooming indicate convergent neuroendocrine mechanisms that may explain some, but not all, peptide-induced grooming syndromes. Further characterization of the qualitative topographic, neuropharmacological, and neuroanatomical differences and species specificities of peptide-induced excessive grooming should provide a basis for understanding how brains coordinate grooming. Knowledge of the processes of neuropeptide control of grooming may provide potential peptide-based controls of grooming-related clinical disorders such as pruritus and allergic reactions.(ABSTRACT TRUNCATED AT 400 WORDS)

Caerulein (ceruletide). A review

Acta Gastroenterol Belg1976;39(5-6):169-85.PMID: 797214DOI: 10.1002/j.1875-9114.1982.tb03189.x

Ceruletide, a decapeptide, is a potent cholecystokinetic agent with a direct spasmogenic effect on the gallbladder muscle and bile ducts in humans and animals. It was recently approved by the Food and Drug Administration for use as an adjunct in x-ray examination of the gallbladder and small bowel. The drug causes a coordinated propulsive activity from the duodenum to the ileum and segmenting activity in the colon. Because of this stimulatory effect, ceruletide is useful not only diagnostically as an aid in x-ray examination of the small bowel, but also therapeutically for treatment of postoperative ileus, intestinal atonia, and chronic fecal statis. Because of its pancreatic stimulatory action, it is useful in evaluation of exocrine pancreatic function. In therapeutic doses the adverse effects noted are mild, transient extensions of the drug's pharmacologic actions and are manifest as nausea, vomiting, abdominal pain, and rarely hypotension and tachycardia. On the basis of current evidence, ceruletide is a safe and effective cholecystokinetic agent and small bowel and exocrine pancreatic stimulant.

Pharmacology, clinical uses, and adverse effects of ceruletide, a cholecystokinetic agent

Pharmacotherapy1982 Jul-Aug;2(4):223-34.PMID: 6763205DOI: 10.1002/j.1875-9114.1982.tb03189.x

Ceruletide, a decapeptide, is a potent cholecystokinetic agent with a direct spasmogenic effect on the gallbladder muscle and bile ducts in humans and animals. It was recently approved by the Food and Drug Administration for use as an adjunct in x-ray examination of the gallbladder and small bowel. The drug causes a coordinated propulsive activity from the duodenum to the ileum and segmenting activity in the colon. Because of this stimulatory effect, ceruletide is useful not only diagnostically as an aid in x-ray examination of the small bowel, but also therapeutically for treatment of postoperative ileus, intestinal atonia, and chronic fecal statis. Because of its pancreatic stimulatory action, it is useful in evaluation of exocrine pancreatic function. In therapeutic doses the adverse effects noted are mild, transient extensions of the drug's pharmacologic actions and are manifest as nausea, vomiting, abdominal pain, and rarely hypotension and tachycardia. On the basis of current evidence, ceruletide is a safe and effective cholecystokinetic agent and small bowel and exocrine pancreatic stimulant.

Ceruletide for schizophrenia: a double-blind study

Biol Psychiatry1985 May;20(5):533-8.PMID: 2859054DOI: 10.1016/0006-3223(85)90024-1

Ceruletide, an analog of cholecystokinin (CCK), has been reported to have neuroleptic-like activity in mice, and, in three open studies, to benefit schizophrenic patients. This study evaluated ceruletide in schizophrenia using a double-blind design. Subjects were 17 chronic schizophrenics with residual symptoms following stabilization with neuroleptics. Patients randomly received two injections, 1 week apart, of either ceruletide (0.6 microgram/kg im) or placebo, while continuing neuroleptics; this regimen was found helpful in earlier studies. Evaluation included ratings of 29 variables related to prognosis in schizophrenia (e.g., age, number of previous hospitalizations), regular BPRSs and SCL-90s, and psychiatrist, patient, and relative ratings of global improvement. Results showed few significant differences between ceruletide and placebo, with exceptions as likely to favor placebo as ceruletide. Among the patients on ceruletide, no predictors of benefit were found. Possible reasons for the negative results are discussed.

Ceruletide and Alpha-1 Antitrypsin as a Novel Combination Therapy for Ischemic Stroke

Neurotherapeutics2022 Mar;19(2):513-527.PMID: 35226340DOI: 10.1007/s13311-022-01203-0

Ischemic stroke is a primary cause of morbidity and mortality worldwide. Beyond the approved thrombolytic therapies, there is no effective treatment to mitigate its progression. Drug repositioning combinational therapies are becoming promising approaches to identify new uses of existing drugs to synergically target multiple disease-response mechanisms underlying complex pathologies. Here, we used a systems biology-based approach based on artificial intelligence and pattern recognition tools to generate in silico mathematical models mimicking the ischemic stroke pathology. Combinational treatments were acquired by screening these models with more than 5 million two-by-two combinations of drugs. A drug combination (CA) formed by ceruletide and alpha-1 antitrypsin showing a predicted value of neuroprotection of 92% was evaluated for their synergic neuroprotective effects in a mouse pre-clinical stroke model. The administration of both drugs in combination was safe and effective in reducing by 39.42% the infarct volume 24 h after cerebral ischemia. This neuroprotection was not observed when drugs were given individually. Importantly, potential incompatibilities of the drug combination with tPA thrombolysis were discarded in vitro and in vivo by using a mouse thromboembolic stroke model with t-PA-induced reperfusion, revealing an improvement in the forepaw strength 72 h after stroke in CA-treated mice. Finally, we identified the predicted mechanisms of action of ceruletide and alpha-1 antitrypsin and we demonstrated that CA modulates EGFR and ANGPT-1 levels in circulation within the acute phase after stroke. In conclusion, we have identified a promising combinational treatment with neuroprotective effects for the treatment of ischemic stroke.

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