Pharmacological and toxicological studies of an original xanthine derivative with bronchodilatating activity.
The article studies the pharmacological properties and the toxicity of the original theophylline derivative G112: 7-/2-bis-/2-hydroxy-ethyl/-aminoethyl/-1,3-dimethylxanthine tartarate, synthesized by Y. Gagaouzov and P. Peykov. Considerable bronchorelaxing activity, measurable with novphylline, has been found in experiments in vivo, as well as in isolated tracheal preparations contracted by various spasmogens. In equimolar concentrations the compound has a weaker inhibitory effect on the phosphodiesterase in the lungs and the brain, compared with theophylline, and it almost does not activate the myocardiac phosphorylase "a" and the lipolysis. A weak and brief hypotensive effect has been established, moderate diuretic action and excitatory effect on the central nervous system, similar to that of novphylline. The compound has considerably lower toxicity than novphylline and it does not lead to changes in the body weight and in the basic haematological and biochemical parameters after treatment of rats for three months.
D000109:Acetylcholine / Q000494:pharmacology; D000628:Aminophylline / Q000031:analogs & derivatives* / Q000494:pharmacology* / Q000633:toxicity; D000818:Animals; D001980:Bronchi / Q000187:drug effects / Q000502:physiology; D001993:Bronchodilator Agents / Q000494:pharmacology* / Q000633:toxicity; D002415:Cats; D004231:Diuresis / Q000187:drug effects; D006168:Guinea Pigs; D006439:Hemodynamics / Q000187:drug effects; D007082:Ileum / Q000187:drug effects; D066298:In Vitro Techniques; D051379:Mice; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects / Q000502:physiology; D011817:Rabbits; D051381:Rats; D013806:Theophylline / Q000494:pharmacology; D014132:Trachea / Q000187:drug effects / Q000502:physiology
D001993:Bronchodilator Agents; D000628:Aminophylline; C045451:7-(2-bis(2-hydroxyethyl)aminoethyl)theophylline; D013806:Theophylline; D000109:Acetylcholine