Design and synthesis of nitrogen-containing benzoheterocyclic derivatives and their antipsychotic activities / 药学学报
Acta Pharmaceutica Sinica
; (12): 994-1001, 2009.
Article
in Zh
| WPRIM
| ID: wpr-354606
Responsible library:
WPRO
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.
Full text:
1
Index:
WPRIM
Main subject:
Pharmacology
/
Structure-Activity Relationship
/
Antipsychotic Agents
/
Drug Design
/
Receptors, Dopamine D2
/
Dopamine Agonists
/
Isoquinolines
Limits:
Animals
Language:
Zh
Journal:
Acta Pharmaceutica Sinica
Year:
2009
Type:
Article