(+)-Kavain

A kavalactone with diverse biological activities

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5mg

￥537.00

430.00

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10mg

￥750.00

600.00

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Background

Kavain is a kavalactone and the major constituent of the pepper plant kava (P. methysticum) and has diverse biological activities.^1,2,3,4 It is a positive allosteric modulator of α4β2δ subunit-containing GABA_A receptors with EC₅₀ values of 25 and 59 ?M in the presence and absence of 300 ?M kavain, respectively, in Xenopus oocytes expressing human receptors.¹ Kavain reduces growth of WPMY-1 prostate cancer cells (IC₅₀ = 5.2 ?g/ml).² It reduces LPS-induced TNF-α production in primary murine macrophages in a concentration-dependent manner.³ In vivo, kavain (1 mg/animal) reduces hind paw swelling and TNF-α production in wild-type, but not Erk^-/-, mice in a mouse model of collagen-induced arthritis. Kavain also reduces acetic acid-induced abdominal constrictions in mice (ED₅₀= 15.71 mg/kg).⁴

1.Chua, H.C., Christensen, E.T., Hoestgaard-Jensen, K., et al.Kavain, the major constituent of the anxiolytic kava extract, potentiates GABAA receptors: Functional characteristics and molecular mechanismPLoS One11(6)e0157700(2016) 2.Li, X., Liu, Z., Xu, X., et al.Kava components down-regulate expression of AR and AR splice variants and reduce growth in patient-derived prostate cancer xenografts in micePLoS One7(2)e31213(2012) 3.Tang, X., and Amar, S.Kavain Inhibition of LPS-Induced TNF-α via ERK/LITAFToxicol. Res. (Camb).5(1)188-196(2016) 4.Kormann, E.C., de Aguiar Amaral, P., David, M., et al.Kavain analogues as potential analgesic agentsPharmacol. Rep.64(6)1419-1426(2012)