Tricyclic compounds as selective muscarinic receptor antagonists. 3. Structure-selectivity relationships in a series of cardioselective (M2) antimuscarinics

• Published in: Journal of medicinal chemistry Vol. 32; no. 8; pp. 1718 - 1724
• Main Authors: Engel, Wolfhard W, Eberlein, Wolfgang G, Mihm, Gerhard, Hammer, Rudolf, Trummlitz, Guenter
• Format: Journal Article
• Language: English
• Published: United States American Chemical Society 01.08.1989
• Subjects: acetylcholine; Animals; Chemical Phenomena; Chemistry; In Vitro Techniques; Myocardium - metabolism; Parasympatholytics - chemical synthesis; Parasympatholytics - metabolism; Pirenzepine - analogs & derivatives; Pirenzepine - chemical synthesis; Pirenzepine - metabolism; Pirenzepine - pharmacology; Rats; Receptors, Muscarinic - metabolism; Structure-Activity Relationship

On the basis of the cardioselective muscarinic receptor antagonist AF-DX 116 (2), a series of 11-substituted pyridobenzodiazepinones (9-35) was prepared and screened for their binding affinity to muscarinic receptors located in cardiac (M2) and glandular (M3) tissue. The ratio of IC50 values of the...