Ciproxifan (Synonyms: FUB-359) |
| Catalog No.GC12924 |
시프록시판(FUB 359)은 9.2 nM의 IC50으로 히스타민 H3 수용체의 강력하고 선택적이며 경구 생체이용 가능한 경쟁적 길항제입니다.
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Cas No.: 184025-18-1
Sample solution is provided at 25 µL, 10mM.
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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.
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