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...

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Veröffentlicht in:	Journal of medicinal chemistry 1981-10, Vol.24 (10), p.1211-1214
Hauptverfasser:	Lemke, Thomas L, Cramer, Michael B, Adamski, Stanley W, Pedone, Carolyn A, Brooker, Gary
Format:	Artikel
Sprache:	eng
Schlagworte:	Adrenergic beta-Antagonists - chemical synthesis Adrenergic beta-Antagonists - metabolism Adrenergic beta-Antagonists - pharmacology Animals Guinea Pigs Heart - drug effects In Vitro Techniques Propanolamines - chemical synthesis Propanolamines - pharmacology Receptors, Adrenergic, beta - metabolism Structure-Activity Relationship Trachea - drug effects
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Zusammenfassung:	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.
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm00142a017