[Search for new beta-adrenoblockaders among derivatives of (3-amino-2-hydroxypropoxy) phenoxymethyl isoxazole].
In experiments on anesthetized rats it was found that some derivatives of 2-(3-isopropylamino-2-hydroxypropoxy) phenoxymethyl isoxazole possess marked beta-adrenoblocking activity associated with alpha-adrenoblocking properties. The most active compound is 3-methyl-4-chloro-5-(3-isopropylamino-2-hydroxypropoxy) phenoxymethyl isoxazole hydrochloride (compound II) which by its beta-adrenoblocking activity is superior to propranolol, oxprenolol and especially labetalol. By its alpha-adrenoblocking activity the compound does not differ significantly from labetalol but it is inferior to phentolamine. Compound II has partial agonistic activity, exerts nonspecific membrane-stabilizing action and exhibits antifibrillatory and antiarrhythmic activity.
D000319:Adrenergic beta-Antagonists / Q000494:pharmacology* / Q000627:therapeutic use / Q000633:toxicity; D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000494:pharmacology / Q000627:therapeutic use / Q000633:toxicity; D001145:Arrhythmias, Cardiac / Q000188:drug therapy; D002415:Cats; D004305:Dose-Response Relationship, Drug; D004353:Drug Evaluation, Preclinical; D006168:Guinea Pigs; D006339:Heart Rate / Q000187:drug effects; D007555:Isoxazoles / Q000494:pharmacology* / Q000627:therapeutic use / Q000633:toxicity; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D009200:Myocardial Contraction / Q000187:drug effects; D010080:Oxazoles / Q000494:pharmacology*; D051381:Rats; D013329:Structure-Activity Relationship
D000319:Adrenergic beta-Antagonists; D000889:Anti-Arrhythmia Agents; D007555:Isoxazoles; D010080:Oxazoles; C057905:(3-amino-2-oxypropoxy)phenoxymethylisoxazole
Poiski novykh beta-adrenoblokatorov v riadu proizvodnykh (3-amino-2-oksipropoksi) fenoksimetilizoksazola.