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左那曲朵对小鼠的镇痛作用的药理学分析。

A pharmacological analysis of levonantradol antinociception in mice.

作者信息

Jacob J J, Ramabadran K, Campos-Medeiros M

出版信息

J Clin Pharmacol. 1981 Aug-Sep;21(S1):327S-333S. doi: 10.1002/j.1552-4604.1981.tb02611.x.

DOI:10.1002/j.1552-4604.1981.tb02611.x
PMID:7197690
Abstract

Using the hot plate test, the potency and mechanism of the analgesic activity of levonantradol was studied in mice. Levonantradol is 10 to 30 times more potent than morphine; the antinociception can be only partially blocked by naloxone. Similar limited antagonism by cholinergics indicates possible opiodergic mechanism. The role of serotoninergic pathways is unclear; antinociception is partially blocked by 5,7-dihydroxytryptamine, unaffected by p-chlorophenylalanine, and potentiated by cyproheptadine. Levonantradol blocks naloxone-induced signs of abstinence in morphine-dependent mice, being 3000 times more potent than morphine and 300 times more potent than delta 9-tetrahydrocannabinol (THC).

摘要

利用热板试验,在小鼠中研究了左那曲朵镇痛活性的效能和机制。左那曲朵的效能是吗啡的10至30倍;其抗伤害感受作用仅能被纳洛酮部分阻断。胆碱能药物类似的有限拮抗作用表明可能存在阿片样物质机制。血清素能途径的作用尚不清楚;抗伤害感受作用可被5,7 - 二羟基色胺部分阻断,不受对氯苯丙氨酸影响,而被赛庚啶增强。左那曲朵可阻断吗啡依赖小鼠中纳洛酮诱导的戒断症状,其效能是吗啡的3000倍,是δ9 - 四氢大麻酚(THC)的300倍。

相似文献

1
A pharmacological analysis of levonantradol antinociception in mice.左那曲朵对小鼠的镇痛作用的药理学分析。
J Clin Pharmacol. 1981 Aug-Sep;21(S1):327S-333S. doi: 10.1002/j.1552-4604.1981.tb02611.x.
2
Levonantradol: a role for central prostanoid mechanisms?左诺曲朵:中枢前列腺素机制的作用?
J Clin Pharmacol. 1981 Aug-Sep;21(S1):367S-374S. doi: 10.1002/j.1552-4604.1981.tb02616.x.
3
Behavioral effects of levonantradol and nantradol in the rhesus monkey.左纳曲朵和纳曲朵对恒河猴的行为影响。
J Clin Pharmacol. 1981 Aug-Sep;21(S1):348S-360S. doi: 10.1002/j.1552-4604.1981.tb02614.x.
4
Modulation of oral morphine antinociceptive tolerance and naloxone-precipitated withdrawal signs by oral Delta 9-tetrahydrocannabinol.口服Δ⁹-四氢大麻酚对口服吗啡镇痛耐受性及纳洛酮诱发戒断症状的调节作用
J Pharmacol Exp Ther. 2003 Jun;305(3):812-7. doi: 10.1124/jpet.102.046870. Epub 2003 Feb 11.
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The attenuation of delta 9-tetrahydrocannabinol and morphine of the quasi-morphine withdrawal syndrome in rats.大鼠中δ9-四氢大麻酚和吗啡对拟吗啡戒断综合征的缓解作用
Psychopharmacology (Berl). 1979 Mar 22;61(2):207-16. doi: 10.1007/BF00426738.
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A comparison of some pharmacological actions of morphine and delta9-tetrahydrocannabinol in the mouse.吗啡与δ9-四氢大麻酚在小鼠体内的某些药理作用比较。
Psychopharmacology (Berl). 1978 May 31;57(3):243-8. doi: 10.1007/BF00426745.
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Antagonism by naloxone of morphine-induced single-dose dependence and antinociception in mice.纳洛酮对小鼠吗啡诱导的单剂量依赖性及抗伤害感受的拮抗作用。
Res Commun Chem Pathol Pharmacol. 1976 Dec;15(4):689-96.
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Evidence that 5-hydroxytryptamine in the forebrain is involved in naloxone-precipitated jumping in morphine-dependent rats.有证据表明,前脑内的5-羟色胺参与了吗啡依赖大鼠中纳洛酮诱发的跳跃反应。
Br J Pharmacol. 1983 Aug;79(4):993-6. doi: 10.1111/j.1476-5381.1983.tb10546.x.
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Prohormone convertase 2 (PC2) null mice have increased mu opioid receptor levels accompanied by altered morphine-induced antinociception, tolerance and dependence.激素原转化酶2(PC2)基因敲除小鼠的μ阿片受体水平升高,同时吗啡诱导的镇痛、耐受性和依赖性也发生改变。
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Enhancement mu opioid antinociception by oral delta9-tetrahydrocannabinol: dose-response analysis and receptor identification.口服δ9-四氢大麻酚增强μ阿片类药物的镇痛作用:剂量反应分析和受体鉴定。
J Pharmacol Exp Ther. 1999 May;289(2):859-67.

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Inhalation exposure to smoke from synthetic "marijuana" produces potent cannabimimetic effects in mice.吸入合成“大麻”产生的烟雾会使老鼠产生强烈的大麻样效应。
Drug Alcohol Depend. 2012 Dec 1;126(3):316-23. doi: 10.1016/j.drugalcdep.2012.05.034. Epub 2012 Jul 7.
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Determination of naphthalen-1-yl-(1-pentylindol-3-yl)methanone (JWH-018) in mouse blood and tissue after inhalation exposure to 'buzz' smoke by HPLC/MS/MS.
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4
Suppression of noxious stimulus-evoked activity in the ventral posterolateral nucleus of the thalamus by a cannabinoid agonist: correlation between electrophysiological and antinociceptive effects.大麻素激动剂对丘脑腹后外侧核中伤害性刺激诱发活动的抑制作用:电生理效应与抗伤害感受作用之间的相关性
J Neurosci. 1996 Oct 15;16(20):6601-11. doi: 10.1523/JNEUROSCI.16-20-06601.1996.
5
Electric shock titration in squirrel monkeys following administration of nantradol, levonantradol, or N-methyl levonantradol.给予纳曲多、左啡诺或N-甲基左啡诺后松鼠猴的电击滴定法
Psychopharmacology (Berl). 1983;79(4):322-4. doi: 10.1007/BF00433410.
6
Effects of single and repeated daily injections of morphine, clonidine, and l-nantradol on avoidance responding of rats.每日单次及重复注射吗啡、可乐定和左旋纳曲多对大鼠回避反应的影响。
Psychopharmacology (Berl). 1985;87(4):425-9. doi: 10.1007/BF00432507.
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Effects of fixed-interval duration on the development of tolerance to decreased responding by l-nantradol.
Psychopharmacology (Berl). 1987;91(1):127-30. doi: 10.1007/BF00690941.
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Effects of fixed-ratio length on the development of tolerance to decreased responding by l-nantradol.
Psychopharmacology (Berl). 1986;90(2):259-62. doi: 10.1007/BF00181253.
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Differential effects of opioid and nonopioid analgesics on conditional discriminations in pigeons.阿片类和非阿片类镇痛药对鸽子条件辨别能力的不同影响。
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