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ChemicalBook--->CAS DataBase List--->1246911-67-0

1246911-67-0

1246911-67-0 Structure

1246911-67-0 Structure
IdentificationBack Directory
[Name]

Fenspiride-d5
[CAS]

1246911-67-0
[Synonyms]

[Molecular Formula]

C15H20N2O2
[MOL File]

1246911-67-0.mol
[Molecular Weight]

260.34
Chemical PropertiesBack Directory
[storage temp. ]

-20°C
[solubility ]

DMSO: soluble,Methanol: soluble
[form ]

A solid
Hazard InformationBack Directory
[Uses]

Fenspiride-d5 is the deuterium labeled Fenspiride. Fenspiride, an orally active non-steroidal antiinflammatory agent, is an antagonist of H1-histamine receptor. Fenspiride inhibites phosphodiesterase 3 (PDE3), phosphodiesterase 4 (PDE4) and phosphodiesterase 5 (PDE5) activities with -log IC50 values of 3.44, 4.16 and approximately 3.8, respectively. Fenspiride can be used for the research of respiratory diseases[1][2][3].
[Biological Activity]

Fenspiride-d5 is intended for use as an internal standard for the quantification of fenspiride by GC- or LC-MS. Fenspiride is an antagonist of histamine H1 receptors and a non-steroidal anti-inflammatory drug (NSAID).1,2 It inhibits histamine-induced contraction of isolated guinea pig trachea but not histamine-induced inotropy of isolated guinea pig heart. It also inhibits phosphodiesterase 4 (PDE4), PDE5, and PDE3 (IC50s = 69, ~158, and 363 μM, respectively, in isolated human bronchi derived from patients with lung cancer).3 It is selective for these phosphodiesterases over PDE1 and PDE2, where it provides less than 25% inhibition. Fenspiride potentiates the airway relaxant effects of isoproterenol and sodium nitroprusside indicating an effect on cAMP and cGMP phosphodiesterases, respectively. Aerosolized fenspiride (1 mg/ml) reverses bronchoconstriction induced by capsaicin and, when used at aerosolized concentrations ranging from 1-10 mg/ml, reduces cough induced by citric acid in a guinea pig model of cough.2
[IC 50]

H1 Receptor
[References]

1.Rognoni, F., Marchini, F., Piacenza, G., et al.Effect of 8-N-phenethyl-1-oxa-2-oxo-3,8-diazaspiro(4,5)decane hydrochloride (decaspiride) on histamine receptorsBoll. Chim. Farm.117(7)397-401(1978) 2.Laude, E.A., Bee, D., Crambes, O., et al.Antitussive and antibronchoconstriction actions of fenspiride in guinea-pigsEur. Respir. J.8(10)1699-1704(1995) 3.Cortijo, J., Naline, E., Ortiz, J.L., et al.Effects of fenspiride on human bronchial cyclic nucleotide phosphodiesterase isoenzymes: Functional and biochemical studyEur. J. Pharmacol.341(1)79-86(1998)
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