Menthol: a natural analgesic compound
Menthol: a natural analgesic compound
复制标题
DOI：
10.1016/s0304-3940(01)02527-7
复制
发表时间：
2002-04-12
影响因子：
2.5
通讯作者：
Ghelardini, C
中科院分区：
文献类型：
--
作者：
Galeotti, N;Mannelli, LD;Ghelardini, C
薄荷醇在局部使用后，通过抑制神经细胞膜上的钙电流，刺激“冷”受体，引起凉爽的感觉。由于钙通道阻滞剂具有镇痛作用，本研究旨在探讨薄荷醇的潜在抗伤害性作用。(-)-薄荷醇可剂量依赖性地提高小鼠热板痛阈值(3-10 mg kg(-1)P.O.)腹缩试验(3~10 mg kg(-1)P.O.；10杯/只小鼠侧脑室注射)。非选择性阿片受体拮抗剂纳洛酮和选择性K受体拮抗剂Nor-NBI可拮抗薄荷脑的抗伤害性作用。反之，L拮抗剂CTOP、Delta(1)拮抗剂7-亚苄基曲松酮和Delta(2)拮抗剂纳曲本不能阻断(-)-薄荷醇的抗伤害性作用。在这两个试验中，(+)-薄荷脑(10-50 mg kg(-1)P.O.；10-30杯/只小鼠静脉注射)无法修改疼痛阈值。这些结果表明，(-)-薄荷醇通过选择性激活kappa-阿片受体而具有镇痛作用。(C)2002爱思唯尔科学爱尔兰有限公司。保留所有权利。
Menthol, after topical application, causes a feeling of coolness due to stimulation of 'cold' receptors by inhibiting Ca++ currents of neuronal membranes. Since Ca++ channel blockers are endowed with analgesic properties, the aim of the present study was to investigate the potential antinociceptive effect of menthol. (-)-Menthol produced a dose-dependent increase in the pain threshold in the mouse hot-plate (3-10 mg kg(-1) p.o.) and abdominal constriction (3-10 mg kg(-1) p.o.; 10 mug per mouse intracerebroventricularly (i.c.v.))tests. The antinociceptive effect of H-menthol was antagonised by the unselective opioid antagonist naloxone and by the selective K-antagonist nor-NBI. Conversely, CTOP ( L-antagonist), 7-benzylidenenal-trexone (delta(1) antagonist) and naltriben (delta(2) antagonist) did not prevent (-)-menthol antinociception. In both tests, (+)-menthol (10-50 mg kg(-1) p.o.; 10-30 mug per mouse i.c.v.) was unable to modify the pain threshold. These results indicate that (-)-menthol is endowed with analgesic properties mediated through a selective activation Of kappa-opioid receptors. (C) 2002 Elsevier Science Ireland Ltd. All rights reserved.