product name Ciproxifan
Description: Ciproxifan is a highly potent and selective histamine H3-receptor antagonist with IC50 of 9.2 nM, with low apparent affinity at other receptor subtypes. In addition, Ciproxifan has been reported to competitively antagonize the (R) α-MeHA induced relaxation of electrically stimulated guinea pig ileum longitudinal muscle. Besides, Ciproxifan has been revealed to have the effect on [125I]iodoproxyfan binding with a Ki value of 0.7±0.2 nM.
References: J Pharmacol Exp Ther. 1998 Nov;287(2):658-66; Behav Brain Res. 2004 Aug 12;153(1):69-76.
386.4
Formula
C16H18N2O2.C4H4O4
CAS No.
184025-19-2
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 54 mg/mL (139.8 mM)
Water: <1 mg/mL
Ethanol: 54 mg/mL (139.8 mM)
Solubility (In vivo)
Synonyms
FUB 359
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19427510
| In Vitro |
In vitro activity: Ciproxifan inhibits [3H]HA release from synaptosomes with Ki of 0.5 nM. Ciproxifan inhibits the binding of [125I]iodoproxyfan at the brain H3 receptor with Ki of 0.7 nM. Ciproxifan displays high affinity at H3 receptor but shows low apparent affinity at other receptor subtypes as evaluated in functional tests on isolated organs (histamine H1 and H2, muscarinic M3, adrenergic α1D and β1, serotonin 5-HT1B, 5-HT2A, 5-HT3 and 5-HT4). Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Ciproxifan intravenously injected at dose of 1 mg/kg decreases the H3-receptor ligand concentration in serum in Male Swiss mice, with half-times of distribution phase of 13min and elimination phase of 87 min, respectively. Ciproxifan (1 mg/kg, p.o.) rises brain t-MeHA level rapidly in Male Swiss mice, being already significantly increased after 30 min, reaching a plateau between 90 and 180 min and still remaining enhanced after 270 min. Ciproxifan leads to ED50 values of 0.23 mg/kg in cerebral cortex, 0.28 mg/kg in striatum and 0.30 mg/kg in hypothalamus in Male Wistar rats. Ciproxifan (3 mg/kg, i.p.) significantly increases choice accuracy as evaluated in the five-choice task performed using a short stimulus duration. 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. Ciproxifan (10 mg/kg i.p.) enhances prepulse inhibition in the DBA/2 strain mice. Ciproxifan (3 mg/kg i.p.) alleviates hyperactivity and cognitive deficits in the APP Tg2576 mouse model of Alzheimers disease. Ciproxifan (3 mg/kg i.p.) improves accuracy and decreased impulsivity in adult male hooded Lister rats. |
| Animal model | Male Swiss mice |
| Formulation & Dosage | Dissolved in 1% methylcellulose for the oral route, in 0.9% NaCl for i.v. routes; 1 mg/kg; p.o. or i.v. administration |
| References | J Pharmacol Exp Ther. 1998 Nov;287(2):658-66; Behav Brain Res. 2004 Aug 12;153(1):69-76. |
