Anti-inflammatory activity of a non-steroidal anti-inflammatory agent, oxaprozin, in experimental models
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- HIGUCHI Shohei
- Research Center, Taisho Pharmaceutical Co. Ltd.
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- OSADA Yuuko
- Research Center, Taisho Pharmaceutical Co. Ltd.
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- SHIOIRI Yoko
- Research Center, Taisho Pharmaceutical Co. Ltd.
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- NAKAIKE Shiro
- Research Center, Taisho Pharmaceutical Co. Ltd.
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- MURAMATSU Makoto
- Research Center, Taisho Pharmaceutical Co. Ltd.
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- TANAKA Makoto
- Research Center, Taisho Pharmaceutical Co. Ltd.
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- ARAI Iwao
- Research Center, Taisho Pharmaceutical Co. Ltd.
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- AMANUMA Fusao
- Research Center, Taisho Pharmaceutical Co. Ltd.
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- OTOMO Susumu
- Research Center, Taisho Pharmaceutical Co. Ltd.
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- AIHARA Hironaka
- Research Center, Taisho Pharmaceutical Co. Ltd.
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- TSURUFUJI Susumu
- Department of Biochemistry, Faculty of Pharmaceutical Sciences, Tohoku University
Bibliographic Information
- Other Title
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- 非ステロイド性抗炎症薬Oxaprozinの抗炎症作用
- ヒ ステロイドセイ コウ エンショウヤク Oxaprozin ノ コウ エンシ
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Abstract
Anti-inflammatory activity and mode of action of oxaprozin, a new non-steroidal anti-inflammatory agent, were investigated in experimental animal models and in vitro tests. Anti-inflammatory potency of oxaprozin was almost equal to that of aspirin in acetic acid vascular permeability, carrageenin hind paw edema, cotton pellet granuloma and adjuvant arthritis tests in rats. On the other hand, in mice, oxaprozin was more potent than aspirin, ibuprofen and phenylbutazone, and it was as potent as sulindac and fenbufen in acetic acid vascular permeability and carrageenin hind paw edema tests. In adrenalectomized rats, the anti-edema activity of oxaprozin in the carrageenin hind paw edema test was the same as that in intact rats. Oxaprozin inhibited erythema formation induced by ultra-violet rays in guinea pigs. The inhibitory potency of oxaprozin against prostaglandin E2 biosynthesis in vitro was equal to that of ibuprofen. Oxaprozin showed a concentration-dependent inhibition of heat-induced denaturation of bovine serum albumin and lysis of rabbit erythrocytes in vitro. However, oxaprozin did not inhibit rat hind paw edemas induced by dextran, formalin and serotonin. It was suggested from these results that the mode of action of oxaprozin is similar to those of other acidic non-steroidal anti-inflammatory drugs. Ulcerogenicity of oxaprozin was weaker than those of phenylbutazone and aspirin in rats. Species differences in the metabolic rate of oxaprozin were shown. The blood concentration of oxaprozin in rats is extremely low because the metabolic rate of oxaprozin is rapid in rats. Therefore, in rats, oxaprozin exhibited a weak anti-inflammatory effect. However, in mice, oxaprozin had a low metabolic rate, and the effect of oxaprozin was as potent as sulindac and fenbufen. The elimination half-life of oxaprozin is extended, 49 to 69 hr, in humans. It was suggested from these findings that oxaprozin is a potent and long acting anti-inflammatory drug in clinical use.
Journal
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- Folia Pharmacologica Japonica
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Folia Pharmacologica Japonica 83 (5), 383-394, 1984
The Japanese Pharmacological Society
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Keywords
Details 詳細情報について
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- CRID
- 1390282679250553088
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- NII Article ID
- 130000761004
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- NII Book ID
- AN00198335
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- COI
- 1:CAS:528:DyaL2cXktlaqsb0%3D
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- ISSN
- 13478397
- 00155691
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- NDL BIB ID
- 2989717
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- PubMed
- 6432656
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- Text Lang
- ja
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- Data Source
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- JaLC
- NDL
- Crossref
- PubMed
- CiNii Articles
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- Abstract License Flag
- Disallowed