| Identification | Back Directory | [Name]
Cyclopropyl[4-[3-(1H-imidazol-5-yl)propoxy]phenyl]methanone hydrochloride | [CAS]
1049741-81-2 | [Synonyms]
Cyclopropyl[4-[3-(1H-imidazol-5-yl)propoxy]phenyl]methanone hydrochloride | [Molecular Formula]
C16H19ClN2O2 | [MDL Number]
MFCD08705321 | [MOL File]
1049741-81-2.mol | [Molecular Weight]
306.787 |
| Chemical Properties | Back Directory | [storage temp. ]
2-8°C | [solubility ]
DMSO: soluble30mg/mL | [form ]
solid | [color ]
off-white | [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 | [InChIKey]
PWAPSKMHZQQTRJ-UHFFFAOYSA-N | [SMILES]
Cl.O=C(C1CC1)c2ccc(OCCCc3c[nH]cn3)cc2 |
| Safety Data | Back Directory | [Hazard Codes ]
Xn | [Risk Statements ]
22 | [WGK Germany ]
3 | [Storage Class]
11 - Combustible Solids | [Hazard Classifications]
Acute Tox. 4 Oral |
| Hazard Information | Back Directory | [Uses]
Ciproxifan Hydrochloride is a novel chemical series of human histamine H3-receptor antagonists. | [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. | [in vivo]
Ciproxifan hydrochloride (1 mg/kg; a single p.o.) increases the t-MeHA level in mouse brain, with an ED50 of 0.14 mg/kg[1].
Ciproxifan hydrochloride (3 mg/kg, i.p.) improves the accuracy of responding in the five-choice task in rats only when the stimulus duration was 0.25 sec instead of 0.50 sec[1].
Ciproxifan hydrochloride (0.15-2 mg/kg; p.o.) induces marked signs of neocortical electroencephalogram activation manifested by enhanced fast-rhythms density and an almost total waking state in cats[1].
Ciproxifan hydrochloride (1 mg/kg; a single i.v.) decreases the H3-receptor ligand concentration in serum in mice, with the half-lives (t1/2) of 13 and 87 min for the distribution and elimination phases in mice, respectively[1].
Ciproxifan hydrochloride (1 mg/kg; a single p.o.) exhibits oral bioavailability (F=62%) and maximal concentration (Cmax=420 nM) in mice[1]. |
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Merck KGaA
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