Fenspiride-d5 - CAS 1246911-67-0

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) . 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) . 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 aci......

PDE, Histamine Receptor

Immunology/Inflammation, Neuroscience, GPCR/G Protein, Metabolism

1246844

C15H15D5N2O2

265.36

O=C1OC2(CCN(CCC3=C(C(=C(C(=C3[2H])[2H])[2H])[2H])[2H])CC2)CN1

-20°C

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