Actions of the sympathomimetic bronchodilator, rimiterol (R798), on the cardiovascular, respiratory and skeletal muscle systems of the anaesthetized cat.
1. The actions of rimiterol [erythro(3,4-dihydroxyphenyl, 2-piperidyl methanol hydrobromide)], a new sympathomimetic bronchodilator, have been compared with those of salbutamol and laevoisoprenaline on the heart and lungs, and on contractions of the soleus muscle of cats under chloralose anaesthesia.2. Rimiterol and salbutamol injected intravenously were about equipotent in all tests, and were about 8 times less potent than laevoisoprenaline both in opposing the bronchoconstrictor action of 5-hydroxytryptamine, and in decreasing the tension and degree of fusion of incomplete tetanic contractions of the cat soleus muscle. They were about 19 times less potent than laevoisoprenaline in increasing heart rate.3. The effect on the soleus muscle is considered to be analogous to the muscle tremor that often occurs in man, and the results therefore suggest that systemic administration of bronchodilator doses of rimiterol, like salbutamol, may produce muscle tremor as an unwanted side-effect.4. When equipotent doses to oppose 5-hydroxytryptamine-induced bronchospasm were compared, rimiterol and salbutamol produced less tachycardia than did laevoisoprenaline. In order to match the tachycardia produced by laevoisoprenaline, the doses of rimiterol or salbutamol had to be increased about two and a half times. This safety margin for salbutamol in the cat is considerably less than that reported by others for different species, which suggests that beta(1)- and beta(2)-adrenoceptors may be less clearly differentiated in the cat than they are in other laboratory animals.
D000605:Amino Alcohols / Q000494:pharmacology; D000818:Animals; D001794:Blood Pressure / Q000187:drug effects; D001993:Bronchodilator Agents / Q000494:pharmacology*; D002396:Catechols / Q000494:pharmacology; D002415:Cats; D005260:Female; D006321:Heart / Q000187:drug effects*; D006339:Heart Rate / Q000187:drug effects; D007275:Injections, Intravenous; D007545:Isoproterenol / Q000494:pharmacology; D008168:Lung / Q000187:drug effects*; D008297:Male; D000432:Methanol / Q000494:pharmacology; D009119:Muscle Contraction / Q000187:drug effects; D009132:Muscles / Q000187:drug effects*; D010880:Piperidines / Q000494:pharmacology*; D012702:Serotonin Antagonists; D013268:Stimulation, Chemical
D000605:Amino Alcohols; D001993:Bronchodilator Agents; D002396:Catechols; D010880:Piperidines; D012702:Serotonin Antagonists; C084590:rimiterol; D007545:Isoproterenol; D000432:Methanol