Abstract:
BACKGROUND AND PURPOSE:This study examined the antinociceptive effects of sinomenine in a rat model of postoperative pain. EXPERIMENTAL APPROACH:Male and female rats were subjected to a surgical incision in the right hind paw, and the von Frey filament test was used to measure mechanical hypersensitivity after drug or vehicle treatment (p.o. or i.p.). Rats were treated daily with sinomenine before or after the surgery and the AUCs of the antinociceptive effects measured during a 4 h period were calculated to determine the ED50 values of sinomenine. The anti-hyperalgesic effects of different doses of a combination of sinomenine and acetaminophen (paracetamol) were assessed in another group of rats. Dose combinations were determined by using a fixed ratio dose-addition analysis method. KEY RESULTS:Sinomenine (5-80 mg·kg(-1) ) produced dose-dependent antinociceptive effects in rats that had been subjected to surgery and this effect lasted for 4 h. The potency of sinomenine, given i.p. or p.o., did not differ between male and female rats. However, sinomenine was fourfold more potent when given i.p. than p.o. The GABAA receptor antagonist bicuculline blocked the antinociceptive effects of sinomenine. The antinociceptive effect of a daily treatment with sinomenine remained stable throughout the course of postoperative pain. Pretreatment with sinomenine did not alter the mechanical hypersensitivity post-surgery. The combination of sinomenine with acetaminophen produced an infra-additive interaction. CONCLUSIONS AND IMPLICATIONS:Sinomenine demonstrated significant antinociceptive activity against postoperative pain and may be a useful novel pharmacotherapy for the management of postoperative pain.
journal_name
Br J Pharmacoljournal_title
British journal of pharmacologyauthors
Zhu Q,Sun Y,Mao L,Liu C,Jiang B,Zhang W,Li JXdoi
10.1111/bph.13470subject
Has Abstractpub_date
2016-05-01 00:00:00pages
1693-702issue
10eissn
0007-1188issn
1476-5381journal_volume
173pub_type
杂志文章abstract::1 Weighed stripped vasa deferentia were incubated in Holman's solution containing (a) [14C]-sorbitol 0.014 mm, (b) [3H]-noradrenaline ([3H]-NA) 12.31 nM, (c) [3H]-tetrahydrocannabinol ([3H]-delta1-THC) 1 mug/ml for 5, 10, 20 and 30 minutes. 2 Tissues were washed, dissolved in Protosol, counted by standard scintillatio...
journal_title:British journal of pharmacology
pub_type: 杂志文章
doi:10.1111/j.1476-5381.1976.tb07451.x
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journal_title:British journal of pharmacology
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doi:10.1038/sj.bjp.0705874
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doi:10.1038/sj.bjp.0701610
更新日期:1998-01-01 00:00:00
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pub_type: 杂志文章,评审
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journal_title:British journal of pharmacology
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journal_title:British journal of pharmacology
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journal_title:British journal of pharmacology
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doi:10.1111/j.1476-5381.1980.tb10422.x
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abstract:BACKGROUND AND PURPOSE:P2X(7), receptors are potently inhibited by extracellular acidification. The underlying molecular basis remains unknown. This study aimed to examine the role of extracellular histidine, lysine, aspartic acid and glutamic acid residues in the functional inhibition of rat P2X(7) receptors by acidic...
journal_title:British journal of pharmacology
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doi:10.1111/j.1476-5381.2008.00002.x
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journal_title:British journal of pharmacology
pub_type: 杂志文章
doi:10.1111/j.1476-5381.1977.tb07735.x
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abstract::1. Fenclozic acid (2-(4-chlorophenyl)thiazol-4-ylacetic acid; I.C.I. 54,450; "Myalex") is one representative of a new class of compounds with antiinflammatory, analgesic and antipyretic properties as evidenced by its activity in a variety of tests in rats, mice and guinea-pigs.2. In tests of short duration the potency...
journal_title:British journal of pharmacology
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journal_title:British journal of pharmacology
pub_type: 杂志文章
doi:10.1111/j.1476-5381.1989.tb11890.x
更新日期:1989-04-01 00:00:00
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journal_title:British journal of pharmacology
pub_type: 杂志文章
doi:10.1111/j.1476-5381.1971.tb08035.x
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journal_title:British journal of pharmacology
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doi:10.1111/j.1476-5381.1976.tb07445.x
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更新日期:2004-11-01 00:00:00
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journal_title:British journal of pharmacology
pub_type: 杂志文章
doi:10.1111/j.1476-5381.1996.tb15759.x
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pub_type: 杂志文章
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journal_title:British journal of pharmacology
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doi:10.1111/j.1476-5381.2011.01462.x
更新日期:2012-05-01 00:00:00
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journal_title:British journal of pharmacology
pub_type: 杂志文章
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更新日期:2010-07-01 00:00:00