Leonurine weakly binds to multiple GABA receptor sites including the GABAA receptor.[2][3] However, it shows much higher affinity as a 5-HT3A receptorantagonist.[4] 5-HT3A antagonists have been shown to help prevent nausea and vomiting as well as the negative effects of serotonin in the gastrointestinal tract.[5][6]
Leonurine can regulate a variety of functions including oxidative stress, inflammation, fibrosis, apoptosis, and metabolic disorder.[7][8][9]
Leonurine has demonstrated antidepressant-like action and has been shown to increase levels of serotonin, noradrenaline, and dopamine in chronic mild stress studies on mice and inhibits the production of pro-inflammatory cytokines.[10][11][12]
Leonurine has been investigated as a potential treatment for cardiovascular disorders.[13][14][15][16] It protects against oxidative damage from ischemic stroke and demonstrates neuroprotective activity against focal cerebral ischemia brain injury induced on rats.[17][18][19]
Leonurine protects mice from pneumonia induced by influenza A.[20]
Metabolites of leonurine in rats dosed orally include leonurine-10-O-sulfate (the sulfate conjugate of leonurine), leonurine-10-O-β-D-glucuronide (the glucuronide metabolite of leonurine) and an O-demethylated leonurine analog that has not yet had its structure definitively confirmed.[26]
