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Biochem/physiol Actions
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.
H3 histamine receptor antagonist.
Features and Benefits
This compound is featured on the Histamine Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
| Quality Level | 100 |
| assay | ≥98% (HPLC) |
| form | solid |
| storage condition | desiccated,under inert gas |
| color | off-white |
| solubility | DMSO: 30 mg/mL,water, high purity: 30 mg/mL |
| storage temp. | 2-8°C |
| SMILES string | Cl.O=C(C1CC1)c2ccc(OCCCc3c[nH]cn3)cc2 |
| InChI | 1S/C16H18N2O2.ClH/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);1H |
| InChI key | PWAPSKMHZQQTRJ-UHFFFAOYSA-N |
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¥ 1956.41
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