(+)-Kavain是从卡瓦胡椒(Pipermethysticum)中提取的一种主要的卡瓦内酯，具有抗惊厥作用，通过电压依赖性的Na+和Ca2+通道相互作用，减弱血管平滑肌的收缩。Kavain能与α4β2δGABAA受体结合，加强GABA的功效。Kavain是一种治疗炎症疾病的药物，其抗炎作用已被广泛研究。
CAS：500-64-1
分子式：C14H14O3
分子量：230.26
纯度：98%
存储：Store at -20°C

Background:

(+)-Kavain, a main kavalactone extracted from Piper methysticum, has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na+ and Ca2+ channels[1]. (+)-Kavain is shown to bind at the α4β2δ GABAA receptor and potentiate GABA efficacy[2]. (+)-Kavain is used as a treatment for inflammatory diseases, its anti-inflammatory action has been widely studied[4].

(+)-Kavain (10-300 μM) enhances GABA-elicited responses in a concentration-dependent manner. The modulatory effect of Kavain is moderate, with only 170±23% of enhancement measured at 300 μM[2]. (+)-Kavain inhibits TNF-α secretion in cells via suppression of LITAF[4].

[1]. Bradi? I, et al. [Hirschsprung’s disease -- therapy and results]. Acta Chir Iugosl. 1975;22(2):183-95. [2]. Chua HC, et al. Kavain, the Major Constituent of the Anxiolytic Kava Extract, Potentiates GABAA Receptors: Functional Characteristics and Molecular Mechanism. PLoS One. 2016 Jun 22;11(6):e0157700. [3]. G. Boonen, et al. In vivo Effects of the Kavapyrones (+)-Dihydromethysticin and (±)-Kavain on Dopamine, 3,4-Dihydroxyphenylacetic Acid, Serotonin and 5-Hydroxyindoleacetic Acid Levels in Striatal and Cortical Brain Regions. Planta Medica 64 (1998) 507-510. [4]. Tang X, et al. Kavain Inhibition of LPS-Induced TNF-α via ERK/LITAF. Toxicol Res (Camb). 2016 Jan 1;5(1):188-196.