[Beta-adrenoblocking activity and other pharmacological properties of 2-(3-amino-2-hydroxypropoxy)phenyoxymethyl isoxazole derivatives].
Some derivatives of 2-(3-amino-2-hydroxypropoxy)phenoxymethyl isoxazole possess beta- and alpha-adrenoblocking activity. 3-Methyl-4-chlor-5-(3-isopropylamino-2-hydroxypropoxy)phenoxymethyl isoxazole hydrochloride (compound OF-4452) is the most active of the compounds studied. As to the beta-adrenoblocking activity, this compound given in vivo and in vitro compares very favourably with propranolol, oxprenolol and labetalol, in particular; as regards the alpha-adrenoblocking action, it is not inferior to the latter drug. Compound OF-4452 has a partial agonist activity and nonspecific membrane-stabilizing action. It displays antifibrillatory and antiarrhythmic activity as well.
Iuzhakov
S D
SD
Zaĭtseva
K A
KA
Dorodnikova
E V
EV
Mashkovskiĭ
M D
MD
D000317:Adrenergic alpha-Antagonists / Q000494:pharmacology* / Q000633:toxicity; D000319:Adrenergic beta-Antagonists / Q000494:pharmacology* / Q000633:toxicity; D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000494:pharmacology / Q000633:toxicity; D002415:Cats; D004347:Drug Interactions; D005260:Female; D006168:Guinea Pigs; D006339:Heart Rate / Q000187:drug effects; D066298:In Vitro Techniques; D007555:Isoxazoles / Q000494:pharmacology*; D007928:Lethal Dose 50; D008297:Male; D009200:Myocardial Contraction / Q000187:drug effects; D010080:Oxazoles / Q000494:pharmacology*; D050198:Phenoxypropanolamines; D051381:Rats
D000317:Adrenergic alpha-Antagonists; D000319:Adrenergic beta-Antagonists; D000889:Anti-Arrhythmia Agents; D007555:Isoxazoles; D010080:Oxazoles; D050198:Phenoxypropanolamines; C046593:OF 4452
Beta-adrenoblokiruiushchaia aktivnost' i drugie farmakologicheskie svoĭstva proizvodnykh 2-(3-amino-2-oksipropoksi)fenoksimetilizoksazola.