Ambroxol-d5 is intended for use as an internal standard for the quantification of ambroxol by GC- or LC-MS. Ambroxol is an expectorant and active metabolite of bromhexine. It decreases short-circuit currents in electrically stimulated isolated canine tracheal epithelial cells when applied submucosally. Ambroxol decreases IL-13-induced production of mucin 5AC (MUC5AC) in primary human airway epithelial cells and inhibits IL-13-induced decreases in the mucociliary transport rate of endogenous particles in the same cells. Ambroxol increases phenol red secretion, a marker of expectorant activity, in mice when administered at doses of 30, 60, or 120 mg/kg. Formulations containing ambroxol have been used in the treatment of acute or chronic respiratory conditions.
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......