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- caerulein、ceruletide
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出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2015/03/02 18:37:56」(JST)
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Ceruletide
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Systematic (IUPAC) name |
(3S)-3-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}-3-[(2S)-2-[(2S)-2-{2-[(3R)-2-[(2S)-2-[(2S)-2-[(2S)-4-carbamoyl-2-{[(2S)-5-oxopyrrolidin-2-yl]formamido}butanamido]-3-carboxypropanamido]-3-[4-(sulfooxy)phenyl]propanamido]-3-hydroxybutanamido]acetamido}-3-(1H-indol-3-yl)propanamido]-4-(methylsulfanyl)butanamido]propanoic acid |
Clinical data |
AHFS/Drugs.com |
International Drug Names |
Legal status |
?
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Identifiers |
CAS number |
17650-98-5 Y |
ATC code |
V04CC04 |
PubChem |
CID 16219178 |
DrugBank |
DB00403 |
ChemSpider |
147304 N |
UNII |
888Y08971B N |
KEGG |
D03442 N |
ChEMBL |
CHEMBL1201355 N |
Chemical data |
Formula |
C58H73N13O21S2 |
Molecular mass |
1352.40 g/mol |
N (what is this?) (verify) |
Ceruletide (INN), also known as cerulein or caerulein, is a ten amino acid oligopeptide that stimulates smooth muscle and increases digestive secretions. Ceruletide is similar in action and composition to cholecystokinin. It stimulates gastric, biliary, and pancreatic secretion; and certain smooth muscle. It is used in paralytic ileus and as diagnostic aid in pancreatic malfunction. It is used to induce pancreatitis in experimental animal models.
The tree frog
Litoria caerulae, formerly named
Hyla caerulae.
Ceruletide was discovered and its structure elucidated in 1967 by Australian and Italian scientists from dried skins of the Australian green tree frog (Litoria caerulea, formerly Hyla caerulea). Its amino acid sequence is Pglu-Gln-Asp-Tyr[SO3H]-Thr-Gly-Trp-Met-Asp-Phe-NH2.[1][2]
Induction of pancreatitis
Ceruletide upregulates pancreatic acinar cell intercellular adhesion molecule-1 (ICAM-1) proteins through intracellular upregulation of NF-κB. Surface ICAM-1 in turn promotes neutrophil adhesion onto acinar cells enhancing pancreatic inflammation.[3] In addition to promoting the inflammatory cell reaction to acinar cells, ceruletide induces pancreatitis through dysregulation of digestive enzyme production and cytoplasmic vacuolization, leading to acinar cell death and pancreatic edema. Ceruletide also activates NADPH oxidase, a source of reactive oxygen species contributing to inflammation, as well as the Janus kinase/signal transducer, another inflammation inducer.[4]
See also
References
- ^ A. Anastasi, V. Erspamer, and R. Endean (1967). "Isolation and structure of caerulein, an active decapeptide from the skin ofHyla caerulea". Experentia 23 (9): 699–700. doi:10.1007/BF02154119.
- ^ G. De Caro, R. Endean, V. Esparmer, and M. Roseghini (1968). "Occurrence of caerulein in extracts of the skin of Hyla caerulea and other Australian hylids". Br J of Pharmac Chemother 33 (1): 48–58. PMC 1570274. PMID 5660165.
- ^ V. Zaninovic, A. S. Gukovskaya, I. Gukovsky, M. Mouria and S. J. Pandol (2000). "Cerulein upregulates ICAM-1 in pancreatic acinar cells, which mediates neutrophil adhesion to these cells". Am J Physiol Gastrointest Liver Physiol 279 (4): G666–676. PMID 11005752.
- ^ H. Kim (2008). "Cerulein Pancreatitis: Oxidative Stress, Inflammation, and Apoptosis". Gut and liver 167 (2): 74–80. doi:10.5009/gnl.2008.2.2.74. PMC 2871591. PMID 20485614.
Diagnostic agents (V04)
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Digestive system |
Diabetes
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Fat absorption
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Bile duct patency
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- Ceruletide
- Magnesium sulfate
- Sincalide
- Sorbitol
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Liver functional capacity
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- Galactose
- Sulfobromophthalein
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Gastric secretion
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- Betazole
- Caffeine and sodium benzoate
- Cation exchange resins
- Histamine phosphate
- Methylthioninium chloride
- Pentagastrin
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Exocrine pancreatic function
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- Bentiromide
- Pancreozymin
- Secretin
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Endocrine system |
Pituitary function
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Thyroid function
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Fertility disturbances
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Tuberculosis |
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Renal function |
- Alsactide
- Aminohippuric acid
- Indigo carmine
- Inulin and other polyfructosans
- Phenolsulfonphthalein
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UpToDate Contents
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- 1. 急性膵炎の発症機序 pathogenesis of acute pancreatitis
- 2. 膵外分泌機能検査 pancreatic exocrine function tests
English Journal
- Aprotinin revisited: formulation, characterization, biodistribution and therapeutic potential of new aprotinin microemulsion in acute pancreatitis.
- Karasulu HY1, Oruç N, Üstündağ-Okur N, İlem Özdemir D, Ay Şenyiğit Z, Barbet Yılmaz F, Aşıkoğlu M, Özkılıç H, Akçiçek E, Güneri T, Özütemiz Ö.
- Journal of drug targeting.J Drug Target.2015 Mar 4:1-13. [Epub ahead of print]
- Abstract The aim of this study was to develop aprotinin-loaded microemulsion (MA) for intravenous administration and evaluate the biodistribution and therapeutic potential of developed formulation in acute pancreatitis models in rats. Phase diagrams were constructed to identify microemulsion region
- PMID 25738992
- Lipolysis of visceral adipocyte triglyceride by pancreatic lipases converts mild acute pancreatitis to severe pancreatitis independent of necrosis and inflammation.
- Patel K1, Trivedi RN1, Durgampudi C2, Noel P1, Cline RA2, DeLany JP2, Navina S3, Singh VP4.
- The American journal of pathology.Am J Pathol.2015 Mar;185(3):808-19. doi: 10.1016/j.ajpath.2014.11.019. Epub 2015 Jan 8.
- Visceral fat necrosis has been associated with severe acute pancreatitis (SAP) for over 100 years; however, its pathogenesis and role in SAP outcomes are poorly understood. Based on recent work suggesting that pancreatic fat lipolysis plays an important role in SAP, we evaluated the role of pancreat
- PMID 25579844
- The ACE2-angiotensin-(1-7)-Mas axis protects against pancreatic cell damage in cell culture.
- Wang J1, Liu R, Qi H, Wang Y, Cui L, Wen Y, Li H, Yin C.
- Pancreas.Pancreas.2015 Mar;44(2):266-72. doi: 10.1097/MPA.0000000000000247.
- OBJECTIVE: Angiotensin-converting enzyme 2 (ACE2), its product angiotensin-(1-7), and its receptor Mas have been shown to moderate the adverse effects of the ACE-angiotensin II-AT1 axis in many diseases. The aim of this study was to determine whether the ACE2-Ang-(1-7)-Mas axis could have similar ef
- PMID 25426615
Japanese Journal
- Pomalidomide suppresses cerulein-induced acute pancreatitis in mice
- TSAI Ming Jen,CHEN Chinpiao,CHEN Sung-Ho,HUANG Yen Ta,CHIU Ted H.
- Journal of gastroenterology 46(6), 822-833, 2011-06-01
- NAID 10029029845
- ビタミンK3による膵炎抑制効果 (特集 重症急性膵炎の病態解明と治療の新展開)
Related Links
- cerulein ce·ru·le·in (sə-rōō'lē-ən) n. A decapeptide that stimulates smooth muscle, especially gallbladder contraction, and increases digestive secretions.
- Definition of cerulein in the Medical Dictionary. cerulein explanation. Information about cerulein in Free online English dictionary. What is cerulein? Meaning of cerulein medical term. What does cerulein mean? cerulein - definition of ...
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