MOLECULAR PHARMACOLOGICAL STUDIES ON DRUG-RECEPTOR COMPLEXES SYSTEM IN DRUG ACTION

摘要

References(6) Cited-By(1) By Fourneau and others (1) in 1944, it has been reported that F2268, which is one of 1, 3-dioxolane derivatives, is a potent cholinergic agent. According to them, cholinergic activity of these analogues decreases gradually as making along the length of 2-alkyl chain in these structures. From the analysis for dose-response curves of these derivatives, Ariëns and his co-workers (2, 3) have shown that in the case of hydrogen, methyl and ethyl radicals at the 2-position of dioxolane structure, each of these derivatives has almost a cholinergic activity, while in the case of propyl radical it shifts more or less to anticholinergic property, what is called “partial agonist”, and then the hexyl radical changes completely it into anticholinergic activity. On the other hand, the analogus compound (anacoline), which has diphenyl radicals at 2-position of dioxolane structure and piperidinium radical in place of trimethyl ammonium radical in these analogus structures, has been synthesized (4), and its anticholinergic and antihistaminic properties have been observed (5). The purpose of this study is to design the structure with a potent atropine-like activity by means of researching out of the full antagonist of compounds containing 1, 3-dioxolane moiety.