Article date: July 1994
By: L. Gallico, A. Borghi, C. Dalla Rosa, R. Ceserani, S. Tognella, in Volume 112, Issue 3, pages 795-800
The antitussive effects of moguisteine have been compared with codeine in several experimental models of cough in guinea‐pigs and dogs.
Moguisteine and codeine dose‐dependently (respective ED50 values are given in parentheses) inhibited cough induced in guinea‐pigs by 7.5% citric acid aerosol (25.2 and 29.2 mg kg−1, p.o.), by 30 μm capsaicin aerosol (19.3 and 15.2 mg kg−1, p.o.), by mechanical stimulation (22.9 and 26.4 mg kg−1, p.o.) and by tracheal electrical stimulation (12.5 and 13.9 mg kg−1, p.o.).
Moguisteine was effective against cough induced by tracheal electrical stimulation in dogs (ED50 17.2 mg kg−1, p.o.); codeine was not tested because of its emetic effect.
After repeated dosing (12–15 days), moguisteine did not induce tolerance in either guinea‐pigs or dogs.
Moguisteine did not interact with opiate receptors, since it did not show affinity for [3H]‐naloxone binding sites and furthermore naloxone (5mg kg−1, s.c.) did not antagonize its antitussive effects.
Moguisteine had no antitussive effect after i.c.v. administration (20 μg), whilst codeine (2–10 μg) and dextromethorphan (2.5–20 μg) were highly effective.
Our findings demonstrate that moguisteine is a novel peripherally acting non‐narcotic antitussive agent, the mode of action of which remains to be elucidated fully.
The antitussive effects of moguisteine have been compared with codeine in several experimental models of cough in guinea‐pigs and dogs.
Moguisteine and codeine dose‐dependently (respective ED50 values are given in parentheses) inhibited cough induced in guinea‐pigs by 7.5% citric acid aerosol (25.2 and 29.2 mg kg−1, p.o.), by 30 μm capsaicin aerosol (19.3 and 15.2 mg kg−1, p.o.), by mechanical stimulation (22.9 and 26.4 mg kg−1, p.o.) and by tracheal electrical stimulation (12.5 and 13.9 mg kg−1, p.o.).
Moguisteine was effective against cough induced by tracheal electrical stimulation in dogs (ED50 17.2 mg kg−1, p.o.); codeine was not tested because of its emetic effect.
After repeated dosing (12–15 days), moguisteine did not induce tolerance in either guinea‐pigs or dogs.
Moguisteine did not interact with opiate receptors, since it did not show affinity for [3H]‐naloxone binding sites and furthermore naloxone (5mg kg−1, s.c.) did not antagonize its antitussive effects.
Moguisteine had no antitussive effect after i.c.v. administration (20 μg), whilst codeine (2–10 μg) and dextromethorphan (2.5–20 μg) were highly effective.
Our findings demonstrate that moguisteine is a novel peripherally acting non‐narcotic antitussive agent, the mode of action of which remains to be elucidated fully.
DOI: 10.1111/j.1476-5381.1994.tb13149.x
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