|
|
| | CIPROXIFAN Basic information |
| Product Name: | CIPROXIFAN | | Synonyms: | Ciproxifan Moleate;FUB 359 Maleate;FUB359 Maleate;FUB-359 Maleate;Ciproxifan maleate, >=98%;Cyclopropyl (4-[3-(1H-imidazol-4-yl)propyloxy]phenyl) ketone maleate salt;(4-(3-(1H-Imidazol-5-yl)propoxy)phenyl)(cyclopropyl)methanone maleate;CIPROXIFAN | | CAS: | 184025-19-2 | | MF: | C16H18N2O2.C4H4O4 | | MW: | 386.402 | | EINECS: | | | Product Categories: | Inhibitors | | Mol File: | 184025-19-2.mol |  |
| | CIPROXIFAN Chemical Properties |
| storage temp. | Store at -20°C | | solubility | DMSO: soluble32mg/mL | | form | powder | | color | white to beige | | 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- | | InChIKey | RLQFKEYRALXXEJ-BTJKTKAUSA-N | | SMILES | OC(=O)\C=C/C(O)=O.O=C(C1CC1)c2ccc(OCCCc3c[nH]cn3)cc2 |
| Hazard Codes | Xn | | Risk Statements | 22-36/37/38-43 | | Safety Statements | 26-36/37/39 | | WGK Germany | 3 | | Storage Class | 11 - Combustible Solids | | Hazard Classifications | Acute Tox. 4 Oral
Eye Irrit. 2
Skin Irrit. 2
Skin Sens. 1
STOT SE 3 |
| | CIPROXIFAN Usage And Synthesis |
| Description | Ciproxifan is a histamine H3 receptor antagonist (Ki = 0.5 nM for inhibition of histamine release in rat synaptosomal preparations). 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 . 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. | | Uses | Ciproxifan is a potent histamine H3 receptor antagonist which affects histamine levels in the brain. It may be used in treatments for sleep and neurological disorders. | | Biochem/physiol Actions | Potent, selective H3 histamine receptor antagonist. | | in vivo | Ciproxifan (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 (3 mg/kg, i.p.) improves the accuracy of responding in the five-choice task in rats only when the stimulus duration is 0.25 sec instead of 0.50 sec[1].
Ciproxifan (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 (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 (1 mg/kg; a single p.o.) exhibits oral bioavailability (F=62%) and maximal concentration (Cmax=420 nM) in mice[1]. | | IC 50 | H3 receptor: 9.2 nM (IC50) | | References | [1] X LIGNEAU. Neurochemical and behavioral effects of ciproxifan, a potent histamine H3-receptor antagonist.[J]. Journal of Pharmacology and Experimental Therapeutics, 1998, 287 2: 658-666.
|
| | CIPROXIFAN Preparation Products And Raw materials |
|