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Bamirastine inhibits ligand binding to recombinant human histamine H1 receptors (rhH1R) with an IC50 value of 17.3 nM.

Bamirastine (TAK-427) reduces specific binding of [3H] pyrilamine to recombinant human H1 receptors (rhH1R) is seen in a concentration- dependent manner with an IC50 value of 17.3 nM. The Ki value is calculated to be 7.35 nM. The affinity of Bamirastine is found to be as high as that of azelastine, 2 times lower than that of Epinastine, 8 times lower than that of ketotifen and 3 times higher than that of Terfenadine[1].

Bamirastine (TAK-427) inhibits histamine induced skin reactions in guinea pigs and mice with an ID50 value of 0.884 and 0.450 mg/kg, p.o., respectively; significant inhibition associated with 10 mg/kg of Bamirastine is still observed 24 h after dosing in guinea pigs. Even at 300 mg/kg, Bamirastine does not affect pentobarbital-induced sleeping time in mice. Bamirastine significantly inhibits passive cutaneous anaphylaxis (PCA) in mice and guinea pigs, and also inhibits antigen-induced ISRs in guinea pigs[1].

[1]. Fukuda S, et al. Characteristics of the antihistamine effect of TAK-427, a novel imidazopyridazine derivative. Inflamm Res. 2003 May;52(5):206-14.

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