A histamine H3 receptor antagonist
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Ciproxifan (maleate)

Item No. 29513

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
cyclopropyl[4-[3-(1H-imidazol-4-yl)propoxy]phenyl]-methanone (2Z)-2-butenedioate
CAS Number
184025-19-2
Synonyms
  • FUB-359
Molecular Formula
C16H18N2O2 • C4H4O4
Formula Weight
386.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: soluble
λmax
213, 272 nm
SMILES
O=C(C1CC1)C2=CC=C(OCCCC3=CN=CN3)C=C2.OC(/C=C\C(O)=O)=O
InChi Code
InChI=1S/C16H18N2O2.C4H4O4/c19-16(12-3-4-12)13-5-7-15(8-6-13)20-9-1-2-14-10-17-11-18-14;5-3(6)1-2-4(7)8/h5-8,10-12H,1-4,9H2,(H,17,18);1-2H,(H,5,6)(H,7,8)/b;2-1-
InChi Key
RLQFKEYRALXXEJ-BTJKTKAUSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $37

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    5 mg

    $132

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    10 mg

    $246

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    25 mg

    $479

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    Product Description

    Ciproxifan is a histamine H3 receptor antagonist (Ki = 0.5 nM for inhibition of histamine release in rat synaptosomal preparations).1 It is selective for histamine H3 over histamine H1 and H2, M3 muscarinic, and α1D- and β1-adrenergic receptors (Kis = 3.15-25 µM), as well as the serotonin (5-HT) receptor subtypes 5-HT1B, 5-HT2A, 5-HT3, and 5-HT4 (Kis = 1.58-15 µM) in radioligand binding assays. Ciproxifan (3-300 nM) inhibits relaxation in precontracted isolated guinea pig ileal longitudinal muscle induced by R-(–)-α-methylhistamine (Item No. 25601). In vivo, ciproxifan reduces R-(–)-α-methylhistamine-induced water consumption in rats (ED50 = 0.09 mg/kg). It increases wake episode duration and latency to fall asleep in rats when administered at a dose of 2 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ligneau, X., Lin, J., Vanni-Mercier, G., et al. Neurochemical and behavioral effects of ciproxifan, a potent histamine H3-receptor antagonist. J. Pharmacol. Exp. Ther. 287(2), 658-666 (1998).