Ultra-short-acting .beta.-adrenergic receptor blocking agents. 2. (Aryloxy)propanolamines containing esters on the aryl function

Several short-acting beta-adrenergic receptor blocking agents have been prepared by incorporating ester functions into the aryl portion of certain (aryloxy)propanolamine systems. In particular, methyl 3-[4-[2-hydroxy-3-(isopropylamino)propoxy]phenyl]propionate hydrochloride (ASL-8052) was found to b...

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Veröffentlicht in:	Journal of medicinal chemistry 1982-12, Vol.25 (12), p.1408-1412
Hauptverfasser:	Erhardt, Paul W, Woo, Chi M, Anderson, William G, Gorczynski, Richard J
Format:	Artikel
Sprache:	eng
Schlagworte:	Adrenergic beta-Antagonists - chemical synthesis Animals Blood Pressure - drug effects Chemical Phenomena Chemistry Dogs Guinea Pigs In Vitro Techniques Muscle, Smooth - drug effects Muscle, Smooth, Vascular - drug effects Propanolamines - chemical synthesis Propanolamines - pharmacology Structure-Activity Relationship Time Factors
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Beschreibung
Zusammenfassung:	Several short-acting beta-adrenergic receptor blocking agents have been prepared by incorporating ester functions into the aryl portion of certain (aryloxy)propanolamine systems. In particular, methyl 3-[4-[2-hydroxy-3-(isopropylamino)propoxy]phenyl]propionate hydrochloride (ASL-8052) was found to be a moderately potent, cardioselective compound with a short duration of action when determined in in vivo canine models.
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm00354a003