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利美索龙(Org 6216)在纤维蛋白诱导的单关节炎和佐剂诱导的关节炎中的局部抗炎活性。

The local anti-inflammatory activity of rimexolone (Org 6216) in fibrin-induced monoarticular arthritis and adjuvant-induced arthritis.

作者信息

Lewis A J

出版信息

Agents Actions. 1980 Jun;10(3):258-65. doi: 10.1007/BF02025945.

DOI:10.1007/BF02025945
PMID:7405753
Abstract

The effects of a number of steroids administered intra-articularly in a chronic model of fibrin-induced monoarticular arthritis in the rabbit have been investigated. Org 6216 hydrocortisone acetate, prednisolone tertiary butyl acetate and triamcinolone hexacetonide each suppressed the joint swelling produced 14 days after antigen challenge. These anti-inflammatory effects lasted for at least 7 days. Hydrocortisone semisuccinate was inactive in this model. In addition, the effects of the same compounds and several other anti-inflammatory steroids and indomethacin administered locally with adjuvant was assessed on the resultant paw oedema produced in the rat. The local anti-inflammatory activity, the duration of action and the systemic effects of these drugs varied considerably and only Org 6216, hydrocortisone acetate, prednisolone tertiary butyl acetate and indomethacin produced anti-inflammatory effects throughout the 4 days of the experiments and were devoid of significant adrenolytic and thymolytic activity.

摘要

研究了在兔纤维蛋白诱导的单关节炎慢性模型中关节内注射多种类固醇的效果。Org 6216、醋酸氢化可的松、叔丁醋酸泼尼松龙和己曲安奈德均能抑制抗原攻击14天后产生的关节肿胀。这些抗炎作用至少持续7天。半琥珀酸氢化可的松在该模型中无活性。此外,还评估了相同化合物以及其他几种抗炎类固醇和吲哚美辛与佐剂局部给药对大鼠产生的爪部水肿的影响。这些药物的局部抗炎活性、作用持续时间和全身作用差异很大,只有Org 6216、醋酸氢化可的松、叔丁醋酸泼尼松龙和吲哚美辛在整个4天的实验中产生了抗炎作用,且没有明显的肾上腺溶解和胸腺溶解活性。

相似文献

1
The local anti-inflammatory activity of rimexolone (Org 6216) in fibrin-induced monoarticular arthritis and adjuvant-induced arthritis.利美索龙(Org 6216)在纤维蛋白诱导的单关节炎和佐剂诱导的关节炎中的局部抗炎活性。
Agents Actions. 1980 Jun;10(3):258-65. doi: 10.1007/BF02025945.
2
The persistence and effects of rimexolone in arthritic and normal rabbit knee joints.利美索龙在兔关节炎和正常膝关节中的持久性及作用
Arzneimittelforschung. 1980;30(10):1646-9.
3
Selective local anti-inflammatory activity of THS-201, a new intra-articular steroid, in cotton pellet granuloma and monoarticular arthritis.新型关节内注射用类固醇THS-201在棉球肉芽肿和单关节炎模型中的选择性局部抗炎活性
Arch Int Pharmacodyn Ther. 1986 Mar;280(1):153-64.
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Protective effect of rimexolone on cartilage damage in arthritic mice: a comparative study with triamcinolone hexacetonide.利美索龙对关节炎小鼠软骨损伤的保护作用:与曲安奈德六醋酸酯的比较研究
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Some further effects of prednisolone and triamcinolone hexacetonide on experimental arthritis in rabbits.泼尼松龙和己曲安奈德对兔实验性关节炎的一些进一步影响。
Agents Actions. 1981 Nov;11(5):490-8. doi: 10.1007/BF02004711.
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[Anti-inflammatory effect of THS-201, a new intra-articular steroid].
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引用本文的文献

1
Binding affinities of rimexolone (ORG 6216), flunisolide and their putative metabolites for the glucocorticoid receptor of human synovial tissue.利美索龙(ORG 6216)、氟尼缩松及其假定代谢产物与人滑膜组织糖皮质激素受体的结合亲和力。
Agents Actions. 1990 Jun;30(3-4):377-80. doi: 10.1007/BF01966302.
2
Protective effect of rimexolone on cartilage damage in arthritic mice: a comparative study with triamcinolone hexacetonide.利美索龙对关节炎小鼠软骨损伤的保护作用:与曲安奈德六醋酸酯的比较研究
Agents Actions. 1990 Aug;31(1-2):135-42. doi: 10.1007/BF02003233.

本文引用的文献

1
The production of arthritis in rabbits by an immunological reaction to fibrin.通过对纤维蛋白的免疫反应在兔子身上诱发关节炎。
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2
Deleterious effect of intra-articular hydrocortisone.关节腔内注射氢化可的松的有害作用。
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Triamcinolone hexacetonide. A new corticosteroid for intra-articular therapy.己曲安奈德。一种用于关节内治疗的新型皮质类固醇。
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[Local effects of triamcinolone hexacetonide administered intra-articularly].[关节腔内注射己曲安奈德的局部效应]
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A sensitive method for the comparative bioassay of nonsteroidal anti-inflammatory compounds in adjuvant-induced primary inflammation in the rat.一种用于大鼠佐剂诱导的原发性炎症中甾体抗炎化合物比较生物测定的灵敏方法。
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The effect of drugs in established rabbit monoarticular arthritis.药物对已建立的兔单关节关节炎的影响。
Agents Actions. 1977 Oct;7(4):473-80. doi: 10.1007/BF01966856.
8
A thermographic assessment of three intra-articular prednisolone analogues given in rheumatoid synovitis.类风湿性滑膜炎中三种关节内注射泼尼松龙类似物的热成像评估。
Br J Clin Pharmacol. 1978 May;5(5):447-51. doi: 10.1111/j.1365-2125.1978.tb01653.x.
9
Comparison of intra-articular methotrexate with intra-articular triamcinolone hexacetonide by thermography.
Curr Med Res Opin. 1977;5(2):141-6. doi: 10.1185/03007997709110154.