Valterio C, Kalix P
Arch Int Pharmacodyn Ther. 1982 Feb;255(2):196-203.
Khat leaves, widely used as a stimulant in East Africa and the Arab Peninsula, contain the alkaloid, (-)cathinone. This substance was found to cause in mice an increase of locomotor activity characterized by a dose-effect relationship typical for amphetamine. Furthermore, the effect of (-)cathinone was inhibited by pretreatment of the animals with the neuroleptics haloperidol, spiroperidol, pimozide, flupentixol and butaclamol. Pretreatment with reserpine reduced the effect of (-)cathinone moderately; in reserpinized mice the effect of (-)cathinone was antagonized by the uptake inhibitors mazindol and nomifensine. Together, these observations indicate that the pharmacology of (-)cathinone hypermotility closely parallels that of amphetamine hypermotility. The results suggest that the stimulating properties of khat leaves are due to the presence of an alkaloid with amphetamine-like effects.
巧茶树叶在东非和阿拉伯半岛被广泛用作兴奋剂,它含有生物碱(-)去甲伪麻黄碱。研究发现,这种物质会使小鼠的运动活性增加,其特征是具有苯丙胺典型的剂量效应关系。此外,用抗精神病药物氟哌啶醇、螺哌啶醇、匹莫齐特、氟奋乃静和布他拉莫对动物进行预处理,可抑制(-)去甲伪麻黄碱的作用。用利血平预处理可适度降低(-)去甲伪麻黄碱的作用;在利血平化的小鼠中,(-)去甲伪麻黄碱的作用被摄取抑制剂马吲哚和诺米芬辛拮抗。这些观察结果共同表明,(-)去甲伪麻黄碱导致的运动亢进药理学与苯丙胺导致的运动亢进药理学非常相似。结果表明,巧茶树叶的刺激特性归因于一种具有类似苯丙胺作用的生物碱的存在。