Chemical-Pharmaceutical Investigations Center (NIQFAR)/CCS, University of Itajaí Valey, Itajaí/SC, Brazil.
Pharmacol Rep. 2012;64(6):1419-26. doi: 10.1016/s1734-1140(12)70939-8.
Kavalactones are pharmacologically active compounds present in preparations of the root trunk of Piper methysticum Forst, known as kava. This work describes the analgesic activity of some synthesized analogues of synthetic kavain, which is the main component of kava.
The essays were initially performed against the writhing test in mice, and the most promising compound was analyzed using other classical models of nociception, including formalin-, capsaicin-, glutamate-induced nociception, the hot plate test, and measurement of motor performance.
The results indicated that compound 6-(4-fluorophenyl)-4-methoxy-5,6-dihydropyran-2-one (2d) exerts potent and dose-dependent analgesic activity, inhibiting abdominal constrictions caused by acetic acid in mice, and being more active than some reference drugs. It also presented activity in the other models of pain, with the exception of the hot plate test and the measurement of motor performance.
Although compound 2d exerts antinociceptive activity, the mechanism of action remains uncertain, but it does not involve the opioid system and does not appear to be associated with non-specific effects such as changes in locomotor activity or motor coordination.
卡瓦内酯是存在于 Piper methysticum Forst 根干制剂中的具有药理活性的化合物，被称为卡瓦。这项工作描述了一些合成卡瓦因类似物的镇痛活性，卡瓦因是卡瓦的主要成分。
最初在小鼠的扭体试验中进行了这些研究，对最有前途的化合物进行了其他经典疼痛模型的分析，包括福尔马林、辣椒素、谷氨酸诱导的疼痛、热板试验和运动性能测量。
结果表明，化合物 6-(4-氟苯基)-4-甲氧基-5,6-二氢-2H-吡喃-2-酮（2d）具有强大且剂量依赖性的镇痛活性，抑制了小鼠因乙酸引起的腹部收缩，比一些参考药物更有效。它在其他疼痛模型中也表现出活性，除了热板试验和运动性能测量。
尽管化合物 2d 具有抗伤害活性，但作用机制尚不确定，但它不涉及阿片样物质系统，也似乎与非特异性效应无关，如运动活动或运动协调的改变。
