Comparison of the ability of opioid analgesics to increase endogenous opioid-like activity in the cerebrospinal fluid of rabbits.

Comparison of the ability of opioid analgesics to increase endogenous opioid-like activity in the cerebrospinal fluid of rabbits.
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阿片类镇痛药增加兔脑脊液内源性阿片样活性的能力比较。

DOI:
10.1016/0024-3205(85)90613-7
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发表时间:
1985
期刊:
影响因子:
6.1
通讯作者:
Dewey,WL
Dewey,WL
中科院分区:
医学2区
文献类型:
--
作者:
Kachur,JF;Rosemond,R;Welch,S;Bowman,ER;Martin,BR;Brase,DA;Dewey,WL

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我们以前已经证明,急性给药吗啡增加了内源性物质的水平,具有抗伤害性的活动,在脑脊液(CSF)。本研究旨在确定其他阿片类镇痛药是否具有类似的作用。在s.c.注射哌替啶、喷他佐辛、左啡烷和美沙酮,并在小鼠甩尾和苯醌扭体试验中生物测定阿片样活性。哌替啶(50 mg/kg)给药后60 min采集的CSF的阿片样活性在两种生物测定中均显著增加,而哌替啶的CSF水平不足以解释这种效应。喷他佐辛(25-75 mg/kg)也能显著增加兔脑脊液中阿片样物质的活性,而美沙酮(5-10 mg/kg)和左啡诺(20 mg/kg)的作用不明显。右啡烷(20 mg/kg)、地西泮(10 mg/kg)和戊巴比妥(20 mg/kg)给药未显著增加CSF中的阿片样活性。结论:某些阿片类镇痛药的抗伤害作用可能部分是通过内源性抗伤害物质的释放来介导的。
We have previously demonstrated that the acute administration of morphine increases the level of endogenous substances, which have antinociceptive activity, in cerebrospinal fluid (CSF). The present study was conducted to determine whether other opioid analgesics exert a similar effect. CSF was withdrawn from the cisterna magna of anesthetized rabbits before and after s.c. injections of meperidine, pentazocine, levorphanol and methadone, and was bioassayed for opioid-like activity in the mouse tail-flick and phenylquinone writhing tests. The opioid-like activity of CSF taken 60 min after meperidine (50 mg/kg) was significantly increased in both bioassays, and the CSF level of meperidine was insufficient to account for this effect. Pentazocine (25–75 mg/kg) also significantly increased opioid-like activity in rabbit CSF, but the effects of methadone (5–10 mg/kg) and levorphanol (20 mg/kg) were less marked. Dextrorphan (20 mg/kg), diazepam (10 mg/kg) and pentobarbital (20 mg/kg) administration did not significantly increase opioid-like activity in CSF. It is concluded that the antinociceptive action of some opioid analgesics in rabbits may be mediated in part by the release of endogenous antino-ciceptive substances.
微生物来源的酶抑制剂。
DOI: 10.1098/rstb.1980.0095
发表时间: 1980
期刊: Philosophical transactions of the Royal Society of London. Series B, Biological sciences
影响因子: --
作者:
P. Schindler
通讯作者: P. Schindler