May 1, 1976

Adrenergic sulfonanilides. 4. Centrally active beta-adrenergic agonists

Journal of Medicinal Chemistry
D L TempleL E Allen

Abstract

The central nervous system (CNS) activities of a number of soterenol analogs have been investigated, and several of these compounds possessed potent morphine antagonistic and anorexiant properties. The CNS activity of these compounds was enhanced by certain lipophilic [e.g., 1,1-dimethyl-2-phenethyl (43) or cyclopropyl (40 and 44)] nitrogen substituents; however, minor structural changes on either the aromatic or side-chain moieties drastically reduced central activity. Toxicity in this series was related to the inherent alpha-adrenergic stimulating component (direct or indirect).

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Mentioned in this Paper

Reaction Time
Structure-Activity Relationship
Quinones
Morphine Measurement
Analog
Trachea
Smooth Muscle
Aniline Compounds
Adrenergic beta-Agonists
Adrenergic beta-Agonists [MoA]

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