Showing papers on "Antitussive Agent published in 2011"
TL;DR: The present results suggest that naringin is not a central antitussive drug and naring in does not exert its peripheral antitussives effect through either the sensory neuropeptides system or the modulation of ATP-sensitive K (+) channels.
Abstract: The mechanism of action of naringin has been investigated in different models of experimentally induced cough in guinea pigs. In contrast to codeine phosphate (6 mg/kg, intravenous administration [i. v.]), naringin (15, 30, and 60 mg/kg, i. v.) had no central antitussive effect on cough elicited by electrical stimulation of the superior laryngeal nerve. Naringin (0.5, 1.0, and 2.0 µmol) could not prevent the cough reflex induced by stimulation of the trachea after intracerebroventricular injection (i. c. v.), while codeine phosphate (0.5 µmol) was highly effective. Further characterizing the peripheral mechanism of naringin, we found that its effect (50 mg/kg, i. v.) was not affected by the depletion of sensory neuropeptides, whereas levodropropizine (10 mg/kg, i. v.) lost its capacity to prevent cough in the capsaicin-desensitized guinea pig. Furthermore, pretreatment with glibenclamide (10 mg/kg, intraperitoneal [i. p.]) significantly reduced the antitussive effect of pinacidil (5 mg/kg, subcutaneous [s. c.]), but could not antagonize the antitussive effect of naringin (30 mg/kg, s. c.). Our present results suggest that naringin is not a central antitussive drug. And naringin does not exert its peripheral antitussive effect through either the sensory neuropeptides system or the modulation of ATP-sensitive K (+) channels.
50 citations
TL;DR: Peroral administration of this pectic arabinogalactan inhibited the number of coughs induced by citric acid in guinea pigs and slightly decreased the values of specific airway resistance.
37 citations
TL;DR: Three new indole alkaloids, named kopsihainins A-C, and two known compounds, kopsinine and methyl demethoxycarbonylchanofruticosinate, were isolated from the stems of Kopsia hainanensis and exhibited significant antitussive activity in a citric acid induced guinea pig cough model.
Abstract: Three new indole alkaloids, named kopsihainins A-C (1-3), and two known compounds, kopsinine (4) and methyl demethoxycarbonylchanofruticosinate (5), were isolated from the stems of Kopsia hainanensis. Their structures were determined using extensive spectroscopic methods. The two main constituents 4 and 5 exhibited significant antitussive activity in a citric acid induced guinea pig cough model. The antitussive effect of 4 was demonstrated to interact with the δ-opioid receptor. This is the first report of antitussive effects of aspidofractinine type and chanofruticosinate type alkaloids.
37 citations
TL;DR: Several derivatives had approximately the same potency as codeine when given subcutaneously to guinea‐pigs; one of these, dicholine glycyrrhetinic acid hydrogen succinate, exhibited the same degree of activity after oral administration.
Abstract: The antitussive activity of 18β-glycyrrhetinic acid has been investigated using chemical stimulation in the unanaesthetised guinea-pig and electrical stimulation in the lightly anaesthetised cat. Derivatives of glycyrrhetinic acid were active in both types of experiment indicating a central antitussive effect. Several derivatives had approximately the same potency as codeine when given subcutaneously to guinea-pigs; one of these, dicholine glycyrrhetinic acid hydrogen succinate, exhibited the same degree of activity after oral administration
25 citations
TL;DR: The preparation is described of some dialkylaminoethoxyethyl esters (X) of diethylphenylacetic acid and of some corresponding esters of l‐phenylcycfopentane‐l‐carboxylic acid and 4‐phenyltetrahydropyran‐4‐carboxesic acid to reveal the most potent antitussive agent of the present series.
Abstract: The preparation is described of some dialkylaminoethoxyethyl esters (X) of diethylphenylacetic acid and of some corresponding esters of l-phenylcycfopentane-l-carboxylic acid and 4-phenyltetrahydropyran-4-carboxylic acid. These were required for biological study which revealed that the diethylaminoethoxyethyl ester (X; R = R' = Et) of diethylphenylacetic acid (Oxeladin) was the most potent antitussive agent of the present series.
5 citations