Design and synthesis of nitrogen-containing benzoheterocyclic derivatives and their antipsychotic activities.
- Author:
Shao-Ping PENG
1
;
Lei-Ping YU
;
Jian-Qi LI
Author Information
1. Shanghai Institute of Pharmaceutical Industry, Shanghai 200437, China.
- Publication Type:Journal Article
- MeSH:
Animals;
Antipsychotic Agents;
chemical synthesis;
pharmacology;
Dopamine Agonists;
chemical synthesis;
pharmacology;
Drug Design;
Isoquinolines;
chemical synthesis;
pharmacology;
Mice;
Receptors, Dopamine D2;
Structure-Activity Relationship
- From:
Acta Pharmaceutica Sinica
2009;44(9):994-1001
- CountryChina
- Language:Chinese
-
Abstract:
A series of nitrogen-containing benzoheterocyclic derivatives were synthesized and tested for their antipsychotic activities. Their structures were confirmed by 1H NMR and HR-MS. Preliminary in vitro pharmacological trials showed that most of the target compounds have high affinity with D2 and 5-HT(2A) receptors. Among the tested compounds, 20 exhibited the highest affinity and D2 partial agonist activity. In vivo studies showed 20 has potent antipsychotic activities on apomorphine mice model, which is a chance to find a better precursor of D2 partial agonist for further optimization.
