(+)-Kavain

(+)-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 GABA_A receptor and potentiate GABA efficacy^[2]. (+)-Kavain is used as a treatment for inflammatory diseases, its anti-inflammatory action has been widely studied^[4]. IC50 & Target: Na⁺, Ca²⁺ channel^[1].
α4β2δ GABA_A receptor^[2]. In Vitro: (+)-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].