Pharmacological studies of 1-(o-chlorophenyl)-2-tert.-butylaminoethanol (C-78), a new bonchodilator.
The bronchodilating effects and other related pharmacological properties of 1-(o-chlorophenyl)-2-tert.-butylaminoethanol-hydrochloride (C-78) were studied in comparison with those of isoproterenol, salbutamol and clorprenaline. C-78 was found to produce a bronchodilating effect 2--10 times stronger and considerably weaker than clorprenaline and isoproterenol, respectively. However, the bronchodilating effect of C-78 was sustained more than 10 times as long as those of isoproterenol and sulbutamol and, especially on oral administration, it was much more potent. The bronchodilating effect of C-78 seems to be due to excitation of the adrenergic beta-receptor, and was antagonized by propranolol. The positive chronotropic and inotropic effects of C-78 on an isolated atrial preparation were less than 1/1000 as potent as those of isoproterenol. C-78 also decreased the tone of smooth muscle, such as the uterus, but its affinity for the bronchial muscle is much higher than for the uterus. C-78 showed strong anti-anaphylactic action and strongly promoted the tracheal ciliary movement. Anitussive effect was also demonstrated, though this was inferior to that of codeine, however, there was no influence on bronchosecretion.
D000109:Acetylcholine / Q000037:antagonists & inhibitors; D000318:Adrenergic beta-Agonists; D000420:Albuterol / Q000494:pharmacology; D000707:Anaphylaxis; D000818:Animals; D001993:Bronchodilator Agents; D004285:Dogs; D005260:Female; D006168:Guinea Pigs; D006634:Histamine H1 Antagonists; D007545:Isoproterenol / Q000031:analogs & derivatives / Q000494:pharmacology; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D009119:Muscle Contraction / Q000187:drug effects; D009129:Muscle Tonus / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects; D009928:Organ Specificity; D010477:Perfusion; D011312:Pressure; D011817:Rabbits; D051381:Rats; D013726:Terbutaline / Q000031:analogs & derivatives* / Q000494:pharmacology; D014132:Trachea / Q000187:drug effects; D014590:Uterine Contraction / Q000187:drug effects
D000318:Adrenergic beta-Agonists; D001993:Bronchodilator Agents; D006634:Histamine H1 Antagonists; D007545:Isoproterenol; D013726:Terbutaline; D000109:Acetylcholine; D000420:Albuterol