Acrivastine is a histamine H1 receptor antagonist with a Ki value of 10 nM in COS-7 cells expressing the human receptor.1 In vivo, acrivastine (1 mg/kg) completely inhibits response to histamine in guinea pigs.2 Formulations containing acrivastine have been used for the treatment of seasonal allergies and hay fever.
1.Wieland, K., Laak, A.M., Smit, M.J., et al.Mutational analysis of the antagonist-binding site of the histamine H1 receptorJ. Biol. Chem.274(42)29994-30000(1999) 2.Hoshiko, K., Chapman, I.D., and Morley, J.Histamine(H1) antagonists and airway hyperreactivity in the guinea-pigAgents Actions Suppl.34323-333(1991)