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学科主题: 药学
题名:
Antinociceptive effects of the novel spirocyclopiperazinium salt compound LXM-10 in mice
作者: Yue, Cai-Qin1; Ye, Jia1; Li, Chang-Ling1; Li, Run-Tao1; Sun, Qi1
关键词: LXM-10 ; antinociception
刊名: PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR
发表日期: 2007-04-01
DOI: 10.1016/j.pbb.2007.02.009
卷: 86, 期:4, 页:643-650
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Behavioral Sciences ; Neurosciences ; Pharmacology & Pharmacy
研究领域[WOS]: Behavioral Sciences ; Neurosciences & Neurology ; Pharmacology & Pharmacy
关键词[WOS]: NICOTINIC ACETYLCHOLINE-RECEPTOR ; ISOLATED RAT SKIN ; ANALGESIC ACTIVITY ; NEUROPATHIC PAIN ; TEMPERATURE
英文摘要:

The compound LXM-10 (2,4-dimethyl-9-beta-phenylethyl-3-oxo-6, 9-diazaspiro [5.5]undecane chloride) is a new spirocyclopiperazinium salt compound. This is the first article to evaluate its antinociceptive effect in the abdominal constriction test induced by acetic acid and the hot-plate test. In the abdominal constriction test, LXM-10 had a significant dose-response effect, and the maximal inhibition ratio was 79.2%. In the hotplate test, LXM-10 had significant dose-response and time-response effects. The antinociceptive effect began at 1.0 h, peaked at 2.0 h, and persisted 3.0 h after s.c. administration. The hot-plate latency was increased by 126.8% at the dose of 12.0 mg/kg. The antinociceptive effect of LXM-10 was blocked by mccamylamine (a central and peripheral neuronal nicotinic acetylcholine receptor antagonist, 0.25, 0.5, 1.0 mg/kg, i.p.), hexamethonium (a peripheral neuronal nicotinic acetylcholine receptor antagonist, 0.2, 1.0, 5.0 mg/kg, i.p.), atropine (a central and peripheral muscarmic acetylcholine receptor antagonist, 0.2, 1.0, 5.0 mg/kg, i.p.), and atropine methylnitrate (a peripheral muscarmic acetylcholine receptor antagonist, 0.2, 1.0, 5.0 mg/kg, i.p.) in a dose-dependent fashion. In contrast, the effect was not blocked by naloxone (a non-selective opioid receptor antagonist, 2.0 mg/kg, i.p.) or yohimbine (a alpha(2)-adrenergic receptor antagonist, 1.0, 2.5, 5.0 mg/kg, i.p.) in the hot-plate test. Therefore, the antinociceptive effects of LXM-10 involve the peripheral neuronal nicotinic and muscarinic acetylcholine receptors; they are not related to opioid receptors or alpha(2)-adrenergic receptors. LXM-10 did not affect motor coordination, spontaneous activity, or body temperature. These findings with LXM-10 suggest that spirocyclopiperazinium derivatives could provide insight on new analgesics. (c) 2007 Elsevier Inc. All rights reserved.

语种: 英语
WOS记录号: WOS:000247642600006
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/52309
Appears in Collections:北京大学药学院_期刊论文

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作者单位: 1.Peking Univ, Dept Mol & Cellular Pharmacol, Sch Pharmaceut Sci, Beijing 100083, Peoples R China
2.Peking Univ, Dept Biol Chem, Sch Pharmaceut Sci, Beijing 100083, Peoples R China

Recommended Citation:
Yue, Cai-Qin,Ye, Jia,Li, Chang-Ling,et al. Antinociceptive effects of the novel spirocyclopiperazinium salt compound LXM-10 in mice[J]. PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR,2007,86(4):643-650.
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