Pharmacology of GYKI-41 099 (chlorpropanol, Tobanum) a new potent beta-adrenergic antagonist.
The compound GYKI-41 099, as a beta-adrenergic antagonist, is 3-8 times more potent than propranolol in vitro and in vivo. Its antiarrhythmic effectiveness surpasses that of propranolol and pindolol inhibiting the ouabain arrhythmia in dogs and cats. GYKI-41 900 has a negligible cardiodepressant activity; it is not cardioselective. The compound shows a rapid and long lasting effect. There was a prolonged elimination of the radioactivity after the injection of 14C-41 099 to rats and dogs. The half life of the unlabeled substance in humans was more than 10 hours.
D000319:Adrenergic beta-Antagonists / Q000378:metabolism / Q000494:pharmacology*; D000779:Anesthetics, Local; D000818:Animals; D001145:Arrhythmias, Cardiac / Q000188:drug therapy; D002415:Cats; D004285:Dogs; D005227:Fatty Acids / Q000378:metabolism; D005260:Female; D006168:Guinea Pigs; D006339:Heart Rate / Q000187:drug effects; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D011412:Propanolamines; D013045:Species Specificity
D000319:Adrenergic beta-Antagonists; D000779:Anesthetics, Local; D005227:Fatty Acids; D011412:Propanolamines; C025725:tobanum