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Ciproxifan hydrochloride

Cat. No. M7722

All AbMole products are for research use only, cannot be used for human consumption.

Ciproxifan hydrochloride Structure

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Quality Control & Documentation
Biological Activity

Ciproxifan belongs to a novel chemical series of histamine H3-receptor antagonists. In vitro, it behaved as a competitive antagonist at the H3 autoreceptor controlling 3H histamine release from synaptosomes and displayed similar Ki values (0.5-1.9 nM) at the H3 receptor controlling the electrically-induced contraction of guinea pig ileum or at the brain H3 receptor labeled with 125I-iodoproxyfan. Ciproxifan appears to be an orally bioavailable, extremely potent and selective H3-receptor antagonist whose vigilance- and attention-promoting effects are promising for therapeutic applications in aging disorders.

Chemical Information
Molecular Weight 306.79
Formula C16H18N2O2 · HCl
CAS Number 1049741-81-2
Solubility (25°C) DMSO: 30 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Lucyna Piera, et al. Histamine is involved in the regulation of collagen content in cultured heart myofibroblasts via H 2, H 3 and H 4 histamine receptors

[2] Xiaofei She, et al. A high-throughput screen identifies inhibitors of lung cancer stem cells

[3] Christophe Plisson, et al. 11C-GSK189254: a selective radioligand for in vivo central nervous system imaging of histamine H3 receptors by PET

[4] Siyuan Le, et al. Correlation between ex vivo receptor occupancy and wake-promoting activity of selective H3 receptor antagonists

[5] X Ligneau, et al. BF2.649 [1-{3-[3-(4-Chlorophenyl)propoxy]propyl}piperidine, hydrochloride], a nonimidazole inverse agonist/antagonist at the human histamine H3 receptor: Preclinical pharmacology

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