H3R antagonist 8 is a selective nonimidazole histamine H3 receptor antagonist ( IC 50 = 0.35 μM). H3R antagonist 8 exhibits hERG channel blockade activity ( IC 50 = 0.67 μM). H3R antagonist 8 inhibits seizures by antagonizing H3 receptor. H3R antagonist 8 reduces tonic hind limb extension (THLE) in mice in the maximal electroshock seizure (MES) model ( ED 50 = 20.21 mg/kg) and and shortens pentylenetetrazol (PTZ)-induced total movement distance in AB strain zebrafish larvae. H3R antagonist 8 can be used for the study of epilepsy.
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