Pharmacological evaluation of new alkylesters of 4-[(2-hydroxy-3-alkylamino)propoxy]phenylcarbamic acids with beta-adrenolytic properties.
The basic relationship between the chemical structure and pharmacological activities of new alkylesters of 4-[(2-hydroxy-3-alkylamino)propoxy]phenylcarbamic acids were evaluated. The efficiency of compounds was compared with those of metipranolol and practolol, respectively. The majority of 4-substituted derivatives of aryloxypropanolamines have shown antiisoprenaline (beta-adrenolytic) and local anesthetic (membrane stabilizing) activities. The values of LD50 and/or partition coefficients have not differed significantly when compared with those of standard metipranolol.
Racanská
E
E
Department of Pharmacology and Toxicology, Faculty of Pharmacy, Komenský University, Bratislava, CSFR.
Csöllei
J
J
Svec
P
P
D000319:Adrenergic beta-Antagonists / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000777:Anesthetics / Q000138:chemical synthesis; D000818:Animals; D002219:Carbamates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D002682:Chinchilla; D004305:Dose-Response Relationship, Drug; D004983:Ethanolamines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D005260:Female; D006168:Guinea Pigs; D006321:Heart / Q000187:drug effects; D006339:Heart Rate / Q000187:drug effects; D066298:In Vitro Techniques; D007545:Isoproterenol / Q000494:pharmacology; D007928:Lethal Dose 50; D008297:Male; D014290:Metipranolol / Q000494:pharmacology; D051379:Mice; D008970:Molecular Weight; D009130:Muscle, Smooth / Q000187:drug effects; D011217:Practolol / Q000494:pharmacology; D011817:Rabbits; D051381:Rats; D011919:Rats, Inbred Strains; D012995:Solubility
D000319:Adrenergic beta-Antagonists; D000777:Anesthetics; D002219:Carbamates; D004983:Ethanolamines; D007545:Isoproterenol; D011217:Practolol; D014290:Metipranolol