Antitussive Agent

About: Antitussive Agent is a research topic. Over the lifetime, 380 publications have been published within this topic receiving 5776 citations.

The antitussive effect of cromakalim in rats is not associated with adenosine triphosphate sensitive K+ channels.

Abstract: The effects of cromakalim, a K+ channel opener, on the capsaicin-induced cough reflex in rats were studied. I.P. administration of cromakalim in doses of 0.1 to 1.0 mg/kg decreased the number of induced coughs in a dose- dependent manner. Neither glibenclamide, an adenosine triphosphate-sensitive K+ channel blocker, nor tetraethylammonium, a blocker of other types of K+ channels, affected the antitussive effect of cromakalim. However, the antitussive effect of cromakalim was antagonized by methysergide, a 5-HT antagonist. Although Bay K 8644, a dihydropyridine Ca2+ channel activator, had a marked cough-depressant effect, it had no effect on the antitussive effect of cromakalim. These results suggest that the antitussive effect of cromakalim is primarily mediated by activation of the serotonergic system through the inhibition of voltage-dependent Ca2+ channels, and not through the activation of K+ channels.

N-(2-pyrrolidinoethyl) amides - with antitussive activity

Abstract: New N-(2-pyrrolidinoethyl)amides of formula (I) and their acid-addn salts (where RCO is an acyl residue derived from phenylacetic, alpha-phenyl-alpha-ethylacetic, diphenylacetic, benzilic, alpha-alkoxy-alpha, alpha-diphenylacetic, or phenothiazine-10-carboxylic acid) Cpds (I) are antitussive agents, some with an activity superior to codeine and with low toxicity (eg LD50 = 560-750 mg/kg, po, mouse) A typical cpd is N-(2-pyrrolidinoethyl)-alpha-phenyl-alpha-ethylacetamide In an example, this is prepd in hydrochloride form by reacting alpha-phenyl-alpha-ethylacetyl chloride with 2-pyrrolidinoethylamine

[Possible role of sigma-receptors in the regulation of cough reflex, gastrointestinal and retinal function]

Abstract: This paper provides an overview of our current understanding of the role of sigma-receptors in the regulation of cough, gastrointestinal and retinal function. Systemic administration of N-(+)-allylnormetazocine ((+)SKF-10,047), 1,2-di-(2-toyl)guanidine (DTG) or pentazocine markedly reduced the number of coughs in a dose-dependent manner. The antitussive effect of these sigma-receptor ligands was significantly reduced by pretreatment with haloperidol or rimcazol, a specific antagonist of sigma-receptors. Antitussive effects of dextromethorphan and noscapine were significantly and dose-dependently reduced by pretreatment with rimcazole. However, rimcazole did not have a significant effect on the antitussive effect of morphine. These results suggest that haloperidol-sensitive sigma-receptors may be involved in the antitussive mechanism of non-narcotic antitussive drugs. Selective sigma-receptor ligands such as (+)SKF-10,047, DTG and (+)pentazocine elicit a potent protection against gastric and duodenal ulcers. Ulcerprotective activity of sigma-receptor ligands may be related to their stimulating effect on bicarbonate secretion through interaction with sigma-receptors in the gastrointestinal mucosa. Activation of sigma-receptors in retina protect retinal cells against glutamate-induced neurotoxicity. It is possible that sigma-receptor ligands may be useful as therapeutic drugs against retinal disease with ischemia-induced neuronal cell death such as retinal artery occlusion, diabetes mellitus or glaucoma.