| Identification | Back Directory | [Name]
PROXYFAN MALEATE | [CAS]
177708-09-7 | [Synonyms]
PROXYFAN MALEATE
Proxyfan oxalate
1H-Imidazole, 5-[3-(phenylmethoxy)propyl]-
4-[3-(Phenylmethoxy)propyl]-1H-imidazoleoxalate | [Molecular Formula]
C13H16N2O | [MDL Number]
MFCD09038563 | [MOL File]
177708-09-7.mol | [Molecular Weight]
216.28 |
| Chemical Properties | Back Directory | [Boiling point ]
414.5±33.0 °C(Predicted) | [density ]
1.115±0.06 g/cm3(Predicted) | [storage temp. ]
Desiccate at RT | [solubility ]
Soluble to 100 mM in DMSO and to 100 mM in water | [form ]
Powder | [pka]
14.60±0.10(Predicted) |
| Hazard Information | Back Directory | [Uses]
Proxyfan is a potent histamine H3 receptor antagonist with Ki values of 2.9 nM and 2.7 nM for rat and human H3 receptor, respectively. Proxyfan is over 1000-fold more potent at H3 receptors than other histamine receptors[1][2]. | [Biological Activity]
High affinity histamine H 3 receptor ligand (pK i = 8.62) that acts as a protean agonist at recombinant and native receptors. In functional studies, activity ranges from full agonist to inverse agonist depending on system used. Displays partial agonist effects on cAMP inhibition and MAPK activity, neutral antagonist activity on histamine release and partial inverse agonism of [ 3 H]-arachidonic acid release. | [IC 50]
Rat H3LR: 2.9 nM (Ki); Human H3LR: 2.7 nM (Ki) | [References]
[1] X Ligneau, et al. Distinct pharmacology of rat and human histamine H(3) receptors: role of two amino acids in the third transmembrane domain. Br J Pharmacol. 2000 Dec;131(7):1247-50. DOI:10.1038/sj.bjp.0703712
[2] R H Clapp, et al. Proxyfan acts as a neutral antagonist of histamine H3 receptors in the feeding-related hypothalamic ventromedial nucleus. Br J Pharmacol. 2012 Nov;167(5):1099-110. DOI:10.1111/j.1476-5381.2012.02056.x |
|
|