Kavain has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na+ and Ca2+ channels.

[2] However, the precise mechanisms underlying the psychotropic, sedative, and anxiolytic actions of kavain and related kavalactones are still debated.

[3] Many studies involved kava extracts from different plant parts and are, therefore, not applicable to kavain itself.

In 2016, kavain was shown to bind at the extrasynaptic α4β2δ GABAA receptor and potentiate GABA efficacy, similarly to barbiturates.

[5] Kavain and analogs remain interesting for drug discovery against a variety of cellular targets, including P-glycoprotein (Pgp), cytochrome P450, and cyclo-oxygenase (COX) enzymes among others.