Central Cholinergic Agents. III. Synthesis of 2-Alkoxy-2,8-diazaspiro[4.5]decane-1,3-diones as Muscarinic Agonists

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概要

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• 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 CO_2-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.

• 公益社団法人日本薬学会の論文
• 1992-05-25

著者

• 石原 雄二

  Chemistry Research Laboratories

• 後藤 義一

  Chemistry Research Laboratories

• 後藤 義一

  Pharmaceutical Research Laboratories I Pharmaceutical Research Division Takeda Chemical Industries L

• 宮本 政臣

  Pharmaceutical Research Laboratories I Pharmaceutical Research Division Takeda Chemical Industries L

• 行正 秀文

  Chemistry Research Laboratories Research And Development Division Takeda Chemical Industries Ltd.

• 石原 雄二

  Pharmaceutical Research Laboratories I Pharmaceutical Research Division Takeda Chemical Industries L

• 宮本 政臣

  Biology Research Laboratories, Research and Development Division, Takeda Chemical Industries, Ltd.,

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