Experimental studies on the antitussive properties of the new xanthine derivative 1H-purine-2,6-dione, 3,7-dihydro-3-methyl-7[(5-methyl-1,2,4-oxadiazol-3-yl)methyl]. 1st communication: in vivo demonstration of the effects on animal models of cough and of mucociliary clearance.
CH-13584 (formerly: KHL-8425, 1H-purine-2,6-dione, 3,7-dihydro-3-methyl-7[(5-methyl-1,2,4-oxadiazol-3-yl)methyl], CAS 115779-20-9) is a new xanthine derivative synthesized with the purpose to develop a highly safe compound against several pulmonary disorders, especially for the treatment of acute and chronic cough. CH-13584 showed acute and chronic antitussive activity on citric acid spray-evoked cough model in guinea-pig. CH-13584 was also effective on capsaicine spray and mechanical irritation-induced cough in guinea-pig and rabbit, respectively. The effectivity of CH-13584 on antitussive tests reached and in some cases even exceeded the effectivity of the reference compounds. The compound increased the mucociliary clearance at lower doses than bromhexine.
Mikus
E G
EG
Laboratory for Respiratory Pharmacology of Research & Development Directorate, Chinoin Pharmaceutical and Chemical Works Ltd. Co., Budapest, Hungary.
Révész
J
J
Minker
E
E
Korbonits
D
D
Saano
V
V
Pascal
M
M
Arányi
P
P
D000818:Animals; D000996:Antitussive Agents / Q000494:pharmacology*; D002211:Capsaicin; D019343:Citric Acid / Q000378:metabolism; D003371:Cough / Q000139:chemically induced / Q000517:prevention & control*; D005260:Female; D006168:Guinea Pigs; D066298:In Vitro Techniques; D008297:Male; D009079:Mucociliary Clearance / Q000187:drug effects*; D010069:Oxadiazoles / Q000494:pharmacology*; D010812:Physical Stimulation; D011687:Purines / Q000494:pharmacology*; D011817:Rabbits
D000996:Antitussive Agents; D010069:Oxadiazoles; D011687:Purines; D019343:Citric Acid; C106302:1H-purine-2,6-dione, 3,7-dihydro-3-methyl-7-((5-methyl-1,2,4-oxadiazol-3-yl)methyl)-; D002211:Capsaicin