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Pharmacological characterization of rebamipide: its cholecystokinin CCK1 receptor binding profile and effects on Ca2+ mobilization and amylase release in rat pancreatic acinar cells

DC Field Value Language
dc.contributor.author김경환-
dc.contributor.author문석준-
dc.contributor.author서정택-
dc.contributor.author안정미-
dc.contributor.author이승일-
dc.date.accessioned2015-07-14T16:46:39Z-
dc.date.available2015-07-14T16:46:39Z-
dc.date.issued2004-
dc.identifier.issn0014-2999-
dc.identifier.urihttps://ir.ymlib.yonsei.ac.kr/handle/22282913/111568-
dc.description.abstractWe previously reported that rebamipide (2-(4-chlorobenzoylamino)-3-[2(1H)-quinolinon-4-yl]-propionic acid) generated oscillations of intracellular Ca2+ concentration ([Ca2+]i) probably through the activation of cholecystokinin type 1 (CCK1) receptors in rat pancreatic acinar cells. Therefore, in the present study, we aimed to establish the pharmacological characteristics of rebamipide in rat pancreatic acinar cells. CCK-8S and rebamipide inhibited [125I]BH-CCK-8S binding to rat pancreatic acinar cell membranes with IC50 values of 3.13 nM and 37.7 μM, respectively. CCK-8S usually evoked [Ca2+]i oscillations at concentrations lower than 50 pM, and it induced biphasic [Ca2+]i increases at higher concentrations. In contrast to CCK-8S, rebamipide only induced [Ca2+]i oscillations at all the concentrations we used in this study. In addition, rebamipide was shown to inhibit high concentrations of CCK-8S-induced biphasic increases in [Ca2+]i, suggesting that rebamipide might be a partial agonist at cholecystokinin CCK1 receptors. Although rebamipide induced [Ca2+]i oscillations by activating the cholecystokinin CCK1 receptors, rebamipide did not cause amylase release and only inhibited CCK-stimulated amylase release reversibly and dose-dependently. However, rebamipide did not inhibit carbachol-, vasoactive intestinal polypeptide (VIP)-, and forskolin-induced amylase releases. These data indicate that rebamipide functions as a partial agonist for Ca2+-mobilizing action, and it is also an antagonist for the amylase-releasing action of CCK.-
dc.description.statementOfResponsibilityopen-
dc.format.extent61~66-
dc.relation.isPartOfEUROPEAN JOURNAL OF PHARMACOLOGY-
dc.rightsCC BY-NC-ND 2.0 KR-
dc.rights.urihttps://creativecommons.org/licenses/by-nc-nd/2.0/kr/-
dc.subject.MESHAlanine/analogs & derivatives*-
dc.subject.MESHAlanine/metabolism-
dc.subject.MESHAlanine/pharmacology*-
dc.subject.MESHAmylases/metabolism*-
dc.subject.MESHAnimals-
dc.subject.MESHAntioxidants/metabolism-
dc.subject.MESHAntioxidants/pharmacology-
dc.subject.MESHBinding, Competitive-
dc.subject.MESHCalcium/metabolism*-
dc.subject.MESHCells, Cultured-
dc.subject.MESHCholecystokinin/pharmacology-
dc.subject.MESHDose-Response Relationship, Drug-
dc.subject.MESHIodine Radioisotopes-
dc.subject.MESHKinetics-
dc.subject.MESHPancreas/cytology-
dc.subject.MESHPancreas/drug effects*-
dc.subject.MESHPancreas/metabolism-
dc.subject.MESHQuinolones/metabolism-
dc.subject.MESHQuinolones/pharmacology*-
dc.subject.MESHRats-
dc.subject.MESHReceptor, Cholecystokinin A/agonists-
dc.subject.MESHReceptor, Cholecystokinin A/metabolism*-
dc.subject.MESHSincalide/analogs & derivatives*-
dc.subject.MESHSincalide/metabolism-
dc.subject.MESHSincalide/pharmacology-
dc.subject.MESHSuccinimides/metabolism-
dc.titlePharmacological characterization of rebamipide: its cholecystokinin CCK1 receptor binding profile and effects on Ca2+ mobilization and amylase release in rat pancreatic acinar cells-
dc.typeArticle-
dc.contributor.collegeCollege of Medicine (의과대학)-
dc.contributor.departmentDept. of Pharmacology (약리학)-
dc.contributor.googleauthorSeok Jun Moon-
dc.contributor.googleauthorJeong Mi An-
dc.contributor.googleauthorJeong Taeg Seo-
dc.contributor.googleauthorKyung Hwan Kim-
dc.contributor.googleauthorWooin Ahn-
dc.contributor.googleauthorSyng-Ill Lee-
dc.contributor.googleauthorJuyeon Kim-
dc.identifier.doi10.1016/j.ejphar.2004.10.032-
dc.admin.authorfalse-
dc.admin.mappingfalse-
dc.relation.journalcodeJ00842-
dc.identifier.eissn1879-0712-
dc.identifier.pmid15556137-
dc.identifier.urlhttp://www.sciencedirect.com/science/article/pii/S0014299904012166-
dc.subject.keywordRebamipide-
dc.subject.keywordCholecystokinin CCK1 receptor-
dc.subject.keyword[Ca2+]i oscillation-
dc.subject.keywordAmylase-
dc.contributor.alternativeNameKim, Kyung Hwan-
dc.contributor.alternativeNameMoon, Seok Jun-
dc.contributor.alternativeNameSeo, Jeong Taeg-
dc.contributor.alternativeNameAn, Jeong Mi-
dc.contributor.alternativeNameLee, Syng Ill-
dc.rights.accessRightsnot free-
dc.citation.volume505-
dc.citation.number1-3-
dc.citation.startPage61-
dc.citation.endPage66-
dc.identifier.bibliographicCitationEUROPEAN JOURNAL OF PHARMACOLOGY, Vol.505(1-3) : 61-66, 2004-
dc.identifier.rimsid34925-
dc.type.rimsART-
Appears in Collections:
1. College of Medicine (의과대학) > Dept. of Pharmacology (약리학교실) > 1. Journal Papers
2. College of Dentistry (치과대학) > Dept. of Oral Biology (구강생물학교실) > 1. Journal Papers

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