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Antinociceptive effects of the novel spirocyclopiperazinium salt compound LXM-10 in mice
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
2007-04-01
DOI10.1016/j.pbb.2007.02.009
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
引用统计
被引频次:13[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/52309
专题北京大学药学院
北京大学药学院_化学生物学系
北京大学药学院_分子与细胞药理学系
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
推荐引用方式
GB/T 7714
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.
APA Yue, Cai-Qin,Ye, Jia,Li, Chang-Ling,Li, Run-Tao,&Sun, Qi.(2007).Antinociceptive effects of the novel spirocyclopiperazinium salt compound LXM-10 in mice.PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR,86(4),643-650.
MLA Yue, Cai-Qin,et al."Antinociceptive effects of the novel spirocyclopiperazinium salt compound LXM-10 in mice".PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR 86.4(2007):643-650.
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