184025-18-1 Usage
Biological Activity
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.
Check Digit Verification of cas no
The CAS Registry Mumber 184025-18-1 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,8,4,0,2 and 5 respectively; the second part has 2 digits, 1 and 8 respectively.
Calculate Digit Verification of CAS Registry Number 184025-18:
(8*1)+(7*8)+(6*4)+(5*0)+(4*2)+(3*5)+(2*1)+(1*8)=121
121 % 10 = 1
So 184025-18-1 is a valid CAS Registry Number.
InChI:InChI=1/C16H18N2O2/c19-16(12-3-4-12)13-5-7-15(8-6-13)20-9-1-2-14-10-17-11-18-14/h5-8,10-12H,1-4,9H2,(H,17,18)
184025-18-1Relevant articles and documents
Convenient procedures for synthesis of ciproxifan, a histamine H3-receptor antagonist
Stark, Holger
, p. 315 - 316 (2000)
Cyclopropyl 4-(3-(1H-imidazol-4-yl)propyloxy)phenyl methanone (ciproxifan) is a novel reference antagonist for the histamine H3 receptor. Despite the former Mitsunobu reaction the actual key reaction for preparation based on S(N)Ar for acylated fluoroaromatics with an additional cyclization in a one-pot procedure needs no chromatographic purification steps and results in good yields.
Novel histamine H3-receptor antagonists with carbonyl-substituted 4-(3-(phenoxy)propyl)-1H-imidazole structures like ciproxifan and related compounds
Stark,Sadek,Krause,Huls,Ligneau,Ganellin,Arrang,Schwartz,Schunack
, p. 3987 - 3994 (2007/10/03)
Novel histamine H3-receptor antagonists possessing a 4-(3-(phenoxy)propyl)-1H-imidazole structure generally substituted in the para-position of the phenyl ring have been synthesized according to Mitsunobu or S(N)Ar reactions. With in vitro and
