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A new antiinflammatory compound, timegadine (N-cyclohexyl-N"-4-[2-methylquinolyl]-N'-2-thiazolylguanidine), which inhibits both prostaglandin and 12-hydroxyeicosatetraenoic acid (12-HETE) formation.

作者信息

Ahnfelt-Rønne I, Arrigoni-Martelli E

出版信息

Biochem Pharmacol. 1980 Dec;29(24):3265-9. doi: 10.1016/0006-2952(80)90301-9.

DOI:10.1016/0006-2952(80)90301-9
PMID:6783045
Abstract
摘要

相似文献

1
A new antiinflammatory compound, timegadine (N-cyclohexyl-N"-4-[2-methylquinolyl]-N'-2-thiazolylguanidine), which inhibits both prostaglandin and 12-hydroxyeicosatetraenoic acid (12-HETE) formation.一种新的抗炎化合物，替马加定（N-环己基-N''-4-[2-甲基喹啉基]-N'-2-噻唑基胍），它能抑制前列腺素和12-羟基二十碳四烯酸（12-HETE）的形成。
Biochem Pharmacol. 1980 Dec;29(24):3265-9. doi: 10.1016/0006-2952(80)90301-9.
2
Basic antiinflammatory compounds. N,N',N''-Trisubstituted guanidines.基本抗炎化合物。N,N',N''-三取代胍
J Med Chem. 1980 Jan;23(1):13-20. doi: 10.1021/jm00175a004.
3
The antiinflammatory action of guanabenz is mediated through 5-lipoxygenase and cyclooxygenase inhibition.胍那苄的抗炎作用是通过抑制5-脂氧合酶和环氧化酶介导的。
Eur J Pharmacol. 1987 Oct 13;142(2):197-205. doi: 10.1016/0014-2999(87)90108-7.
4
Multiple effects of a new anti-inflammatory agent, timegadine, on arachidonic acid release and metabolism in neutrophils and platelets.新型抗炎药替马地定对中性粒细胞和血小板中花生四烯酸释放及代谢的多种作用
Biochem Pharmacol. 1982 Aug 15;31(16):2619-24. doi: 10.1016/0006-2952(82)90708-0.
5
5-Hydroxytryptamine and the metabolism of arachidonic acid by the lipoxygenase and cyclooxygenase of washed human platelets.5-羟色胺与洗涤过的人血小板中脂氧合酶和环氧化酶对花生四烯酸的代谢
Biochem Pharmacol. 1990 Jul 15;40(2):309-14. doi: 10.1016/0006-2952(90)90693-f.
6
Stimulation of 12-HETE production in human platelets by an immunomodulator, LF 1695. Evidence for activation of arachidonate liberation coupled to cyclo-oxygenase inhibition.免疫调节剂LF 1695对人血小板中12-羟基二十碳四烯酸（12-HETE）生成的刺激作用。花生四烯酸释放激活与环氧化酶抑制相关的证据。
Biochem Pharmacol. 1989 Sep 1;38(17):2763-72. doi: 10.1016/0006-2952(89)90429-2.
7
In vitro inhibition of granulocyte function by timegadine, a new anti-inflammatory agent.
Int J Tissue React. 1984;6(1):9-15.
8
Adjuvant arthritic rat serum enhances HETE1 biosynthesis.佐剂性关节炎大鼠血清增强HETE1生物合成。
Agents Actions. 1980 Dec;10(6):550-3. doi: 10.1007/BF02024163.
9
Ketoconazole inhibits the biosynthesis of leukotrienes in vitro and in vivo.酮康唑在体内外均可抑制白三烯的生物合成。
Biochem Pharmacol. 1986 Mar 15;35(6):883-91. doi: 10.1016/0006-2952(86)90072-9.
10
Feedback regulation of platelet function by 12S-hydroxyeicosatetraenoic acid: inhibition of arachidonic acid liberation from phospholipids.12S-羟基二十碳四烯酸对血小板功能的反馈调节：抑制花生四烯酸从磷脂中的释放。
Biochim Biophys Acta. 1990 May 1;1044(1):165-8. doi: 10.1016/0005-2760(90)90232-m.

引用本文的文献

1
12-lipoxygenase: a potential target for novel anti-platelet therapeutics.12-脂氧合酶：新型抗血小板治疗的潜在靶点。
Cardiovasc Hematol Agents Med Chem. 2011 Jul 1;9(3):154-64. doi: 10.2174/187152511797037619.
2
Chronic inflammation in adjuvant arthritic rats correlates with enhancement of 12-L-HETE-synthesis.佐剂性关节炎大鼠的慢性炎症与12-L-羟基二十碳四烯酸合成增强相关。
Agents Actions. 1981 Dec;11(6-7):587-9. doi: 10.1007/BF01978753.
3
An unusual profile of activity of a new basic anti-inflammatory drug, timegadine.一种新型碱性抗炎药物替米加定的异常活性谱。
Agents Actions. 1981 Jul;11(4):402-9. doi: 10.1007/BF01982478.
4
The influence of food intake on the bioavailability of timegadine, a novel non-steroidal anti-inflammatory drug.食物摄入对新型非甾体抗炎药替马加定生物利用度的影响。
Br J Clin Pharmacol. 1983 Apr;15(4):495-8. doi: 10.1111/j.1365-2125.1983.tb01537.x.
5
Timegadine: long-term open study in rheumatoid arthritis.替美加定：类风湿关节炎的长期开放性研究。
Clin Rheumatol. 1983 Dec;2(4):363-7. doi: 10.1007/BF02041556.
6
The protein binding of timegadine determined by equilibrium dialysis.通过平衡透析法测定替马加汀的蛋白质结合率。
Br J Clin Pharmacol. 1984 Nov;18(5):785-90. doi: 10.1111/j.1365-2125.1984.tb02543.x.
7
Comparison of timegadine and naproxen in rheumatoid arthritis. A placebo controlled trial.替马加定与萘普生治疗类风湿性关节炎的比较：一项安慰剂对照试验。
Clin Rheumatol. 1983 Dec;2(4):357-61. doi: 10.1007/BF02041555.
8
Histamine, 5-hydroxytryptamine and compound 48/80 activate PMN-leucocyte collagenase of the rat.组胺、5-羟色胺和化合物48/80可激活大鼠的多形核白细胞胶原酶。
Agents Actions. 1984 Apr;14(3-4):451-3. doi: 10.1007/BF01973847.
9
Comparison timegadine versus naproxen in rheumatoid arthritis.替美加定与萘普生治疗类风湿性关节炎的比较。
Clin Rheumatol. 1985 Sep;4(3):362-3. doi: 10.1007/BF02031625.
10
The pharmacokinetics of timegadine and two of its metabolites after multiple oral dosing, and the effects of concomitant administration of ibuprofen.
Eur J Clin Pharmacol. 1986;29(5):581-6. doi: 10.1007/BF00635896.