Moguisteine

Moguisteine is a peripherally acting antitussive agent.^1,2 It inhibits the citric acid-induced cough reflex in conscious guinea pigs but not the cough reflex induced by electrical stimulation of the afferent superior laryngeal nerve in anesthetized guinea pigs (ED₅₀s = 5.5 and >20 mg/kg, respectively).² Moguisteine (75 and 150 mg/kg, p.o.) prevents bronchoalveolar lavage fluid (BALF) eosinophil and neutrophil infiltration in an ovalbumin-sensitized guinea pig model of allergic airway inflammation.³ It inhibits increases in tracheal and bronchial plasma exudation induced by cigarette smoke in anesthetized guinea pigs when administered at a dose of 30 mg/kg.

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1. Gandolfi, C.A., Di Domenico, R., Spinelli, S., et al. N-acyl-2-substituted-1,3-thiazolidines, a new class of non-narcotic antitussive agents: Studies leading to the discovery of ethyl 2-[(2-methoxyphenoxy)methyl]-beta-oxothiazolidine-3-propanoate. J. Med. Chem. 38(3), 508-525 (1995).

2. Ishii, R., Furuta, M., Hashimoto, M., et al. Effects of moguisteine on the cough reflex induced by afferent electrical stimulation of the superior laryngeal nerve in guinea pigs. Eur. J. Pharmacol. 362(2-3), 207-212 (1998).

3. Gallico, L., Oggioni, N., Dalla Rosa, C., et al. Effects of moguisteine, a peripheral nonnarcotic antitussive agent, on airway inflammation in guinea-pigs in vivo. Eur. Respir. J. 9(3), 478-485 (1996).