Cited 5 times in
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 |
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dc.contributor.author | 김경환 | - |
dc.contributor.author | 문석준 | - |
dc.contributor.author | 서정택 | - |
dc.contributor.author | 안정미 | - |
dc.contributor.author | 이승일 | - |
dc.date.accessioned | 2015-07-14T16:46:39Z | - |
dc.date.available | 2015-07-14T16:46:39Z | - |
dc.date.issued | 2004 | - |
dc.identifier.issn | 0014-2999 | - |
dc.identifier.uri | https://ir.ymlib.yonsei.ac.kr/handle/22282913/111568 | - |
dc.description.abstract | We 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.statementOfResponsibility | open | - |
dc.format.extent | 61~66 | - |
dc.relation.isPartOf | EUROPEAN JOURNAL OF PHARMACOLOGY | - |
dc.rights | CC BY-NC-ND 2.0 KR | - |
dc.rights.uri | https://creativecommons.org/licenses/by-nc-nd/2.0/kr/ | - |
dc.subject.MESH | Alanine/analogs & derivatives* | - |
dc.subject.MESH | Alanine/metabolism | - |
dc.subject.MESH | Alanine/pharmacology* | - |
dc.subject.MESH | Amylases/metabolism* | - |
dc.subject.MESH | Animals | - |
dc.subject.MESH | Antioxidants/metabolism | - |
dc.subject.MESH | Antioxidants/pharmacology | - |
dc.subject.MESH | Binding, Competitive | - |
dc.subject.MESH | Calcium/metabolism* | - |
dc.subject.MESH | Cells, Cultured | - |
dc.subject.MESH | Cholecystokinin/pharmacology | - |
dc.subject.MESH | Dose-Response Relationship, Drug | - |
dc.subject.MESH | Iodine Radioisotopes | - |
dc.subject.MESH | Kinetics | - |
dc.subject.MESH | Pancreas/cytology | - |
dc.subject.MESH | Pancreas/drug effects* | - |
dc.subject.MESH | Pancreas/metabolism | - |
dc.subject.MESH | Quinolones/metabolism | - |
dc.subject.MESH | Quinolones/pharmacology* | - |
dc.subject.MESH | Rats | - |
dc.subject.MESH | Receptor, Cholecystokinin A/agonists | - |
dc.subject.MESH | Receptor, Cholecystokinin A/metabolism* | - |
dc.subject.MESH | Sincalide/analogs & derivatives* | - |
dc.subject.MESH | Sincalide/metabolism | - |
dc.subject.MESH | Sincalide/pharmacology | - |
dc.subject.MESH | Succinimides/metabolism | - |
dc.title | Pharmacological characterization of rebamipide: its cholecystokinin CCK1 receptor binding profile and effects on Ca2+ mobilization and amylase release in rat pancreatic acinar cells | - |
dc.type | Article | - |
dc.contributor.college | College of Medicine (의과대학) | - |
dc.contributor.department | Dept. of Pharmacology (약리학) | - |
dc.contributor.googleauthor | Seok Jun Moon | - |
dc.contributor.googleauthor | Jeong Mi An | - |
dc.contributor.googleauthor | Jeong Taeg Seo | - |
dc.contributor.googleauthor | Kyung Hwan Kim | - |
dc.contributor.googleauthor | Wooin Ahn | - |
dc.contributor.googleauthor | Syng-Ill Lee | - |
dc.contributor.googleauthor | Juyeon Kim | - |
dc.identifier.doi | 10.1016/j.ejphar.2004.10.032 | - |
dc.admin.author | false | - |
dc.admin.mapping | false | - |
dc.relation.journalcode | J00842 | - |
dc.identifier.eissn | 1879-0712 | - |
dc.identifier.pmid | 15556137 | - |
dc.identifier.url | http://www.sciencedirect.com/science/article/pii/S0014299904012166 | - |
dc.subject.keyword | Rebamipide | - |
dc.subject.keyword | Cholecystokinin CCK1 receptor | - |
dc.subject.keyword | [Ca2+]i oscillation | - |
dc.subject.keyword | Amylase | - |
dc.contributor.alternativeName | Kim, Kyung Hwan | - |
dc.contributor.alternativeName | Moon, Seok Jun | - |
dc.contributor.alternativeName | Seo, Jeong Taeg | - |
dc.contributor.alternativeName | An, Jeong Mi | - |
dc.contributor.alternativeName | Lee, Syng Ill | - |
dc.rights.accessRights | not free | - |
dc.citation.volume | 505 | - |
dc.citation.number | 1-3 | - |
dc.citation.startPage | 61 | - |
dc.citation.endPage | 66 | - |
dc.identifier.bibliographicCitation | EUROPEAN JOURNAL OF PHARMACOLOGY, Vol.505(1-3) : 61-66, 2004 | - |
dc.identifier.rimsid | 34925 | - |
dc.type.rims | ART | - |
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