Gracza L
Wissenschaftliche Abteilung der Chemisch-Pharmazeutischen Fabrik Göppingen, Carl Müller, Apotheker, GmbH und Co. KG Göppingen, Bundesrepublik Deutschland.
Planta Med. 1983 Jul;48(7):153-7. doi: 10.1055/s-2007-969912.
The local anaesthetic activity of both phenylpropanoids of ASARUM EUROPAEUM trans-isoasarone and trans-isoeugenol methyl ether were measured in comparison to the unsubstituted propenyl benzene and to the mono methoxy derivative trans-anethole resp. benzocaine, trans-Isosarone shows local anaesthetic activity with an intensity nearly equal to benzocaine. The quantitative structure-activity relationship in the series of phenylpropanoids has been analysed and established that the activity is increasing according to the number of methoxy groups. The results are compared with the lipophility and the surface activity of the substances. Surface activity changes parallel with the anaesthetic activity while the lipophility changes in contrary.
测定了细辛醚中的反式异细辛醚和顺式异丁香酚甲醚这两种苯丙素类化合物的局部麻醉活性，并与未取代的丙烯基苯以及单甲氧基衍生物反式茴香脑和苯佐卡因进行了比较。反式异细辛醚显示出局部麻醉活性，其强度几乎与苯佐卡因相当。分析了苯丙素类化合物系列中的定量构效关系，并确定活性随着甲氧基数量的增加而增强。将结果与这些物质的亲脂性和表面活性进行了比较。表面活性与麻醉活性平行变化，而亲脂性则相反变化。
