Ciproxifan is a novel and potent antagonist of histamine H3-receptor with a IC50 value of 9.2±1.8nM [1].
Ciproxifan has shown the in-vitro antagonistic action to H3-receptor with a IC50 value of 9.2±1.8nM. In addition, Ciproxifan has been reported to competitively antagonize the (R) α-MeHA induced relaxation of electrically stimulated guinea pig ileum longitudinal muscle. Besides, Ciproxifan has been revealed to have the effect on [125I]iodoproxyfan binding with a Ki value of 0.7±0.2 nM. Apart from these, Ciproxifan has been found to be a selective antagonist with pKi values of 9.3, 4.9, 4.6, 5.5, 5.4, 4.9, <5.0, 4.8, <5.5 and <5.7 for H3, H2, H1, muscarinic M3, adrenergic α1D, β1, serotonin 5-HT1B, 5-HT2A, 5-HT3 and 5-HT4, respectively [1].
References:
[1] Ligneau X1, Lin J, Vanni-Mercier G, Jouvet M, Muir JL, Ganellin CR, Stark H, Elz S, Schunack W, Schwartz J. Neurochemical and behavioral effects of ciproxifan, a potent histamine H3-receptor antagonist. J Pharmacol Exp Ther. 1998 Nov; 287(2):658-66.