Aydin S, Beis R, Oztürk Y, Baser K H
Department of Pharmacology, Faculty of Pharmacy and Medicinal and Aromatic Plant and Drug Research Centre (TBAM), Anadolu University, Eskisehir, Turkey.
J Pharm Pharmacol. 1998 Jul;50(7):813-7. doi: 10.1111/j.2042-7158.1998.tb07145.x.
The essential oils of Nepeta species including Nepeta phyllochlamys P. H. Davis, N. nuda L. ssp. nuda, and N. caesarea Boiss. have been screened by use of the tail-flick and tail immersion (52.5 degrees C) methods. Of the species studied, only N. caesarea showed significant analgesic activity, besides marked sedation, which was also blocked by naloxone, indicating involvement of opioid receptors. Moreover, it was only active on mechanical, not thermal, algesic response which suggests specificity for specific opioid receptor subtypes, excluding mu-opioid receptors. Because 4a alpha,7alpha,7a alpha-nepetalactone is the main component of the essential oil of N. caesarea, and is present at very high levels (92-95%), it is concluded that 4a alpha,7alpha,7a alpha-nepetalactone is the active principle and has a specific opioid receptor subtype agonistic activity.
通过甩尾法和尾浸法（52.5摄氏度）对包括毛萼荆芥（Nepeta phyllochlamys P. H. Davis）、裸花荆芥（N. nuda L. ssp. nuda）和凯撒荆芥（N. caesarea Boiss.）在内的荆芥属植物的精油进行了筛选。在所研究的物种中，只有凯撒荆芥除了具有明显的镇静作用外，还表现出显著的镇痛活性，且该活性也被纳洛酮阻断，表明阿片受体参与其中。此外，它仅对机械性而非热性痛觉反应有活性，这表明其对特定阿片受体亚型具有特异性，排除了μ-阿片受体。由于4aα,7α,7aα-荆芥内酯是凯撒荆芥精油的主要成分，且含量非常高（92-95%），因此得出结论，4aα,7α,7aα-荆芥内酯是活性成分，具有特定的阿片受体亚型激动活性。
