Adrenergic receptor agonists. Benzofuranylethanolamines.
Two hydroxy-substituted benzofuranylethanolamines (9 and 10), analogues of adrenoceptor-active aryloxypropanolamines, were prepared and their beta-adrenoceptor activity was examined. Compound 9 was found to be a beta 1-selective adrenergic agonist with high intrinsic activity. Due to the rigidity of the benzofuranyl moiety of 9, its functional groups cannot be brought into the same spatial positions as those of a phenylethanolamine-type agonist like isoprenaline. This could indicate that adrenergic agonists of the aryloxypropanolamine type and of the phenylethanolamine type are differently bound to the receptor when eliciting the effect.
D000318:Adrenergic beta-Agonists / Q000138:chemical synthesis*; D000818:Animals; D001572:Benzofurans / Q000138:chemical synthesis / Q000494:pharmacology; D002415:Cats; D004983:Ethanolamines / Q000138:chemical synthesis* / Q000494:pharmacology; D005260:Female; D006339:Heart Rate / Q000187:drug effects; D008297:Male; D008968:Molecular Conformation; D013329:Structure-Activity Relationship; D014655:Vascular Resistance / Q000187:drug effects
D000318:Adrenergic beta-Agonists; D001572:Benzofurans; D004983:Ethanolamines