• 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Life sciences >Evidence for hypernociception induction following histamine H1 receptor activation in rodents.
【24h】

Evidence for hypernociception induction following histamine H1 receptor activation in rodents.

机译：啮齿类动物中组胺H1受体激活后诱发高伤害感受的证据。

获取原文
获取原文并翻译 | 示例
           
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

To characterize the mechanism of the analgesic action of H1 antihistaminics the effects of a new, highly selective agonist, 2-(3-trifluoromethylphenyl)histamine dihydrogenmaleate (FMPH), and of the better known H1 agonist, 2-thiazolylethylamine (2-TEA), were studied on pain threshold by means of three different kinds of tests for nociception (mouse hot plate and abdominal constriction, and rat paw pressure tests). Low doses of both substances (2.65 and 6.5 microg/animal i.c.v. for FMPH in the hot plate and paw pressure tests, and 0.3 microg/rat i.c.v. for 2-TEA in the paw pressure test) were slightly but significantly hypernociceptive. The selective H1 receptor antagonist, pyrilamine maleate (10-30 mg/kg s.c.), induced a dose-dependent antinociception in all three tests, and both FMPH and 2-TEA prevented its effect, but not that of morphine, thus indicating action on H1 receptors. The same low doses of FMPH were also able to enhance animals' spontaneous motility and curiosity. High doses of FMPH (13.23-132.3 microg/mouse i.c.v.) raised the pain threshold, but due to the severe motor impairment evidenced by the rota rod test, this cannot be considered as real antinociception. An increase in the pain threshold lacking any motor impairment was observed for tenfold higher doses of 2-TEA (3 and 10 microg/mouse i.c.v.). This may be due to action on H2 receptors, with the reported relative potency of 2-TEA for H1 and H2 receptors being about 12:1. It is therefore suggested that H1 receptor activation increases sensitivity to noxious stimuli.
机译：为了表征H1抗组胺药的镇痛作用机理，研究了一种新型的，高度选择性的激动剂2-（3-三氟甲基苯基）组胺二氢马来酸酯（FMPH）和众所周知的H1激动剂2-噻唑基乙胺（2-TEA）的作用。通过三种不同的伤害感受测试（小鼠热板和腹部收缩以及大鼠爪压测试）研究了疼痛阈值。两种物质的低剂量（在热板和爪压力试验中，FMPH为2.65和6.5微克/动物i.c.v.，在爪压力试验中为2-TEA为0.3微克/大鼠，i.c.v。）有轻微但明显的高伤害感受性。选择性H1受体拮抗剂马来酸吡拉敏（10-30 mg / kg sc）在所有三个测试中均诱导了剂量依赖性抗伤害感受，FMPH和2-TEA均阻止了其伤害作用，但吗啡没有，因此表明对H1受体。同样的低剂量FMPH也能够增强动物的自发运动能力和好奇心。高剂量的FMPH（13.23-132.3 microg /小鼠i.c.v.）提高了疼痛阈值，但是由于旋转棒试验证明了严重的运动障碍，因此不能认为这是真正的镇痛作用。对于高剂量的2-TEA（3和10微克/小鼠i.c.v.），观察到没有任何运动障碍的疼痛阈值增加。这可能是由于对H2受体的作用所致，据报道2-TEA对H1和H2受体的相对效价约为12：1。因此建议H1受体活化增加对有害刺激的敏感性。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号