Local anaesthetic activity of (+)- and (-)-menthol
Local anaesthetic activity of (+)- and (-)-menthol
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DOI：
10.1055/s-2001-11515
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发表时间：
2001-03-01
期刊：
影响因子：
2.7
通讯作者：
Bartolini, A
中科院分区：
文献类型：
--
作者：
Galeotti, N;Ghelardini, C;Bartolini, A
在这项工作中，我们研究了(+)-和(-)-薄荷醇的局部麻醉活性，薄荷醇是一种在局部应用后引起凉爽感的物质。我们将其活性与两种化学相关化合物百里香酚和(-)-薄荷酮进行了比较。在兔结膜反射试验和大鼠膈神经半膈膜制剂中对麻醉活性进行了体内评价。薄荷醇的两种对映体（10(-4)-1马克/毫升），而百里香酚和(-)-薄荷酮则不能，以剂量依赖的方式显著减少大鼠膈半膈的电诱发收缩。在兔结膜反射试验中，用(+)-和（-）薄荷醇溶液（30-100马克杯/毫升）处理，可以使引起反射所需的刺激次数呈剂量依赖性增加，从而在体内证实了在体外观察到的局部麻醉活性。与体外实验结果相似，百里香酚和(-)-薄荷酮在体内试验中也无效。总之，这些数据证明了薄荷醇的局部麻醉活性，这似乎严格依赖于其化学结构。
In this work we studied the local anaesthetic activity of (+)- and (-)-menthol, a substance used after topical application to induce a feeling of coolness. We compared its activity to two chemically related compounds thymol and (-)-menthone. Anaesthetic activity was evaluated in vivo in the rabbit conjunctival reflex test and in vitro in a rat phrenic nerve hemidiaphragm preparation. Both enatiomers of menthol (10(-4)-1 mug/ml), but not thymol and (-)-menthone, were able to drastically reduce, in a dose-dependent manner, the electrically evoked contractions of rat phrenic hemidiaphragm. In the rabbit: conjunctival reflex test, treatment with a solution of (+)- and (-)menthol (30-100 mug/ml) allowed a dose-dependent increase in the number of stimuli necessary to provoke the reflex, thus confirming in vivo the local anaesthetic activity observed in vitro. Similar to the in vitro results, thymol and (-)-menthone were ineffective also in the in vivo test. In conclusion, these data evidence the local anaesthetic activity of menthol, which appears to be strictly dependent on its chemical structure.