beta-Adrenergic blocking agents. alpha- and gamma-methyl(aryloxy)propanolamines.
A series of gamma-methyl- (5) and alpha-methyl(aryloxy)propanolamines (6) were synthesized and evaluated for beta-adrenergic blocking action. The binding constant (KD) was determined for compounds 5a-j on cultured C6-2B astrocytoma cells. Compounds 5a-j and 6a-e were evaluated for beta 1-antagonist action on guinea pig atria and beta 2-antagonist action on guinea pig tracheal strips. Several gamma-methyl(aryloxy)propanolamines showed affinity for beta receptors and a possible preference for beta 2 receptors.
D000319:Adrenergic beta-Antagonists / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology*; D000818:Animals; D006168:Guinea Pigs; D006321:Heart / Q000187:drug effects; D066298:In Vitro Techniques; D011412:Propanolamines / Q000138:chemical synthesis / Q000494:pharmacology*; D011943:Receptors, Adrenergic, beta / Q000378:metabolism; D013329:Structure-Activity Relationship; D014132:Trachea / Q000187:drug effects
D000319:Adrenergic beta-Antagonists; D011412:Propanolamines; D011943:Receptors, Adrenergic, beta