Effects of IY-81149, a newly developed proton pump inhibitor, on gastric acid secretion in vitro and in vivo
DC Field | Value | Language |
---|---|---|
dc.contributor.author | Kwon, D | - |
dc.contributor.author | Chae, JB | - |
dc.contributor.author | Park, CW | - |
dc.contributor.author | Kim, YS | - |
dc.contributor.author | Lee, SM | - |
dc.contributor.author | Kim, EJ | - |
dc.contributor.author | Huh, IH | - |
dc.contributor.author | Kim, DY | - |
dc.contributor.author | Cho, KD | - |
dc.date.accessioned | 2021-06-18T14:42:18Z | - |
dc.date.available | 2021-06-18T14:42:18Z | - |
dc.date.issued | 2001-01 | - |
dc.identifier.issn | 0004-4172 | - |
dc.identifier.uri | https://scholarworks.bwise.kr/cau/handle/2019.sw.cau/47281 | - |
dc.description.abstract | The inhibitory effects of IY-81149 (2-[[(4methoxy-3-methyl) -2-pyridinyl] methylsulfinyl] -5-(1H-pyrol-1-yl)-1H-benzimidazole, CAS 172152-36-2), a newly developed proton pump inhibitor (PPI) on gastric acid secretion were investigated in vitro and in vivo. In rabbit parietal cell preparation, IY-81149 irreversibly inhibited H+/K+-ATPase in dose-dependent manner With an ICS, of pump inhibitory activity of 6.0 x 10(-6) mol/l and that of omeprazole (CAS 73590-58-6) was 1 x 10(-4) mol/l at pH 7.4. On cumulation of C-14-aminopyrine in histamine stimulated parietal cells, the IC50 of IY-81149 was 9.0 x 10(-9) mol/l and that of omeprazole was 1.9 x 10(-8) mol/l. The inhibition rates of IY-81149 and omeprazole at a concentration of 1 x 10-9 moU1 in human parietal cells were 137 % and 64 %, respectively. In pylorus-ligated rats, IY-81149 showed a 2-3 times stronger inhibitory activity than omeprazole against gastric acid secretion. The ED50 of IY-81149 and omeprazole administered intraduodenally was 1.6 mg/kg and 3.8 mg/kg, In the case of oral administration, the ED50 of IY81149 and omeprazole was 1.94 mg/kg and 5.64 mg/kg, respectively. But after 24 h administration, the anti-secretory activity of IY-81149 was lower than that of omeprazole at all doses tested. In anesthetized rats, IY-81149 dose-dependently increased gastric pH which was lowered by histamine infusion. In the case of i.v. injection, the ED50 of IY-81149 and omeprazole was 1.2 and 1.4 mg/kg and in the case of i.d. administration, the ED50 of IY-81149 and omeprazole was 3.9 and 4.1 mg/kg, respectively. IY-81149 also significantly inhibited pentagastrin-stimulated gastric secretion. Its ED50 was 2.1 mg/kg and that of omeprazole was 3.5 mg/kg with i.d. administration. In the case of i.v. injection, IY-81149 was equipotent to omeprazole. IY-81149 also inhibited gastric acid secretion strongly in fistular rats. The EDS, of TY-81149 administered intraduodenally was 0.43 mg/kg and that of omeprazole was 0.68 mg/kg. In Heidenhain pouch dogs, the acid output was completely blocked at 0.3 mg/kg, 135 min after i.v. administration. Omeprazole showed a similar effect as IY81149. The histamine induced increase of acid output in the Heidenhain pouch dog was blocked by 71 % 150 min after oral administration of enteric-coated IV-81149 at a dose of S mg/kg, and omeprazole showed similar effects. In conclusion, IY-81149 revealed the characteristics as a strong proton pump inhibitor, and its potency against gastric acid secretion was superior to that of the reference drug, omeprazole. | - |
dc.format.extent | 10 | - |
dc.language | 영어 | - |
dc.language.iso | ENG | - |
dc.publisher | ECV-EDITIO CANTOR VERLAG MEDIZIN NATURWISSENSCHAFTEN | - |
dc.title | Effects of IY-81149, a newly developed proton pump inhibitor, on gastric acid secretion in vitro and in vivo | - |
dc.type | Article | - |
dc.identifier.bibliographicCitation | ARZNEIMITTEL-FORSCHUNG-DRUG RESEARCH, v.51, no.3, pp 204 - 213 | - |
dc.description.isOpenAccess | N | - |
dc.identifier.wosid | 000167932200003 | - |
dc.identifier.scopusid | 2-s2.0-0035081562 | - |
dc.citation.endPage | 213 | - |
dc.citation.number | 3 | - |
dc.citation.startPage | 204 | - |
dc.citation.title | ARZNEIMITTEL-FORSCHUNG-DRUG RESEARCH | - |
dc.citation.volume | 51 | - |
dc.type.docType | Article | - |
dc.publisher.location | 독일 | - |
dc.subject.keywordAuthor | antiulcer drug | - |
dc.subject.keywordAuthor | CAS 73590-58-6 | - |
dc.subject.keywordAuthor | CAS 172152-36-2 | - |
dc.subject.keywordAuthor | TY-81149, dog, gerenal pharmacology, rat | - |
dc.subject.keywordAuthor | 2-[[(4-methoxy-3-methyl)-2-pyridinyl]methylsulfinyl]-5-(1H-pyrol-1-yl)-1 H-benzimidazole | - |
dc.subject.keywordAuthor | omeprazole | - |
dc.subject.keywordAuthor | proton pump inhibitors | - |
dc.subject.keywordPlus | SECRETAGOGUES | - |
dc.subject.keywordPlus | ATPASE | - |
dc.relation.journalResearchArea | Pharmacology & Pharmacy | - |
dc.relation.journalResearchArea | Chemistry | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Medicinal | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Multidisciplinary | - |
dc.relation.journalWebOfScienceCategory | Pharmacology & Pharmacy | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
Items in ScholarWorks are protected by copyright, with all rights reserved, unless otherwise indicated.
84, Heukseok-ro, Dongjak-gu, Seoul, Republic of Korea (06974)02-820-6194
COPYRIGHT 2019 Chung-Ang University All Rights Reserved.
Certain data included herein are derived from the © Web of Science of Clarivate Analytics. All rights reserved.
You may not copy or re-distribute this material in whole or in part without the prior written consent of Clarivate Analytics.