Central Cholinergic Agents. III. Synthesis of 2-Alkoxy-2,8-diazaspiro(4.5)decane-1,3-diones as Muscarinic Agonists
| العنوان: | Central Cholinergic Agents. III. Synthesis of 2-Alkoxy-2,8-diazaspiro(4.5)decane-1,3-diones as Muscarinic Agonists |
|---|---|
| المؤلفون: | Yuji Ishihara, Giichi Goto, Hidehumi Yukimasa, Masaomi Miyamoto |
| المصدر: | Chemical and Pharmaceutical Bulletin. 40:1177-1185 |
| بيانات النشر: | Pharmaceutical Society of Japan, 1992. |
| سنة النشر: | 1992 |
| مصطلحات موضوعية: | Male, Agonist, Stereochemistry, medicine.drug_class, Arecoline, Guinea Pigs, Succinimides, Muscarinic Antagonists, In Vitro Techniques, Muscarinic agonist, Methylatropine, Mice, chemistry.chemical_compound, Piperidines, Drug Discovery, Muscarinic acetylcholine receptor, medicine, Muscarinic Receptor Binding, Animals, Spiro Compounds, Rats, Wistar, Mice, Inbred ICR, Muscarinic antagonist, General Chemistry, General Medicine, Receptors, Muscarinic, Pirenzepine, Rats, Parasympathomimetics, chemistry, Cholinergic, medicine.drug |
| الوصف: | A series of 2-alkoxy-2, 8-diazaspiro[4.5]decane-1, 3-diones and related compounds were synthesized and tested for muscarinic receptor binding affinity using [3H]pirenzepine and [3H]oxotremorine M as ligands. They were also evaluated for agonistic activities in the guinea pig ileum assay. 2-Methoxy-2, 8-diazaspiro[4.5]decane-1, 3-dione (1i) was found to be a relatively M1 selective agonist. It reversed CO2-induced impairment of passive avoidance response with long duration of action, but also displayed peripheral effects at low doses. To minimize these side effects, we proposed the idea of conjugation of 1i with a muscarinic antagonist. The carbamate linked conjugate (1u) of 1i with methylatropine was therefore examined. |
| تدمد: | 1347-5223 0009-2363 |
| الوصول الحر: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9d1f1df375eec497663b6e0c44a2f057Test https://doi.org/10.1248/cpb.40.1177Test |
| حقوق: | OPEN |
| رقم الانضمام: | edsair.doi.dedup.....9d1f1df375eec497663b6e0c44a2f057 |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 13475223 00092363 |
|---|