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

Arzneimittelforschung. 1997 Apr;47(4):395-400.

Abstract

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.

MeSH terms

  • Animals
  • Antitussive Agents / pharmacology*
  • Capsaicin
  • Citric Acid / metabolism
  • Cough / chemically induced
  • Cough / prevention & control*
  • Female
  • Guinea Pigs
  • In Vitro Techniques
  • Male
  • Mucociliary Clearance / drug effects*
  • Oxadiazoles / pharmacology*
  • Physical Stimulation
  • Purines / pharmacology*
  • Rabbits

Substances

  • Antitussive Agents
  • Oxadiazoles
  • Purines
  • Citric Acid
  • 1H-purine-2,6-dione, 3,7-dihydro-3-methyl-7-((5-methyl-1,2,4-oxadiazol-3-yl)methyl)-
  • Capsaicin