Central cholinergic agents. III. Synthesis of 2-alkoxy-2,8- diazaspiro[4.5]decane-1,3-diones as muscarinic agonists.

doi:10.1248/CPB.40.1177

Paper

Central cholinergic agents. III. Synthesis of 2-alkoxy-2,8- diazaspiro[4.5]decane-1,3-diones as muscarinic agonists.

Published May 25, 1992 · Y. Ishihara, H. Yukimasa, M. Miyamoto

Chemical & pharmaceutical bulletin

Q3 SJR score

7

Citations

0

Influential Citations

Full textSemantic Scholar

Abstract

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.

In Vitro Study

Study Snapshot

2-Methoxy-2,8-diazaspiro[4.5]decane-1,3-dione (1i) is a relatively M1 selective agonist with long duration of action, but may display peripheral effects at low doses.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

Sign up to use Study Snapshot

Consensus is limited without an account. Create an account or sign in to get more searches and use the Study Snapshot.

Create an account

Central cholinergic agents. III. Synthesis of 2-alkoxy-2,8- diazaspiro[4.5]decane-1,3-diones as muscarinic agonists.

Sign up to use Study Snapshot

References

Citations