Conformationally defined adrenergic agents. 4. 1-(Aminomethyl)phthalans: synthesis and pharmacological consequences of the phthalan ring oxygen atom

The synthesis of a series of 1-(aminomethyl)phthalans 1b is reported. The radioligand binding to alpha 1- and alpha 2-receptors and the in vitro pharmacology in alpha 1 (rabbit aorta) and alpha 2 (phenoxybenzamine-pretreated dog saphenous vein) tissues were determined and were compared to the activi...

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Veröffentlicht in:	Journal of medicinal chemistry 1987-01, Vol.30 (1), p.178-184
Hauptverfasser:	DeBernardis, John F, Arendsen, David L, Kyncl, John J, Kerkman, Daniel J
Format:	Artikel
Sprache:	eng
Schlagworte:	Adrenergic alpha-Agonists - chemical synthesis Animals Benzofurans - chemical synthesis Benzofurans - pharmacology Brain - metabolism Dogs Female In Vitro Techniques Indicators and Reagents Kinetics Liver - metabolism Magnetic Resonance Spectroscopy Male Mass Spectrometry Methylamines - chemical synthesis Methylamines - pharmacology Muscle Contraction - drug effects Muscle, Smooth, Vascular - drug effects Muscle, Smooth, Vascular - physiology Rabbits Rats Rats, Inbred Strains Receptors, Adrenergic, alpha - drug effects Receptors, Adrenergic, alpha - metabolism Spectrophotometry, Infrared Structure-Activity Relationship
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