Adrenergic sulfonanilides. 4. Centrally active beta-adrenergic agonists.
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).
D000318:Adrenergic beta-Agonists / Q000138:chemical synthesis*; D000700:Analgesics; D000814:Aniline Compounds / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D000818:Animals; D002490:Central Nervous System / Q000187:drug effects*; D004983:Ethanolamines / Q000031:analogs & derivatives; D006168:Guinea Pigs; D066298:In Vitro Techniques; D007928:Lethal Dose 50; D008297:Male; D009020:Morphine / Q000037:antagonists & inhibitors; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects; D011809:Quinones / Q000037:antagonists & inhibitors; D051381:Rats; D011930:Reaction Time / Q000187:drug effects; D012110:Reserpine / Q000037:antagonists & inhibitors; D012669:Seminal Vesicles / Q000187:drug effects; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D014132:Trachea / Q000187:drug effects
D000318:Adrenergic beta-Agonists; D000700:Analgesics; D000814:Aniline Compounds; D004983:Ethanolamines; D011809:Quinones; D013449:Sulfonamides; D009020:Morphine; D012110:Reserpine