[Design and synthesis of nitrogen-containing benzoheterocyclic derivatives and their antipsychotic activities].
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.
Peng
Shao-Ping
SP
Shanghai Institute of Pharmaceutical Industry, Shanghai 200437, China.
Yu
Lei-Ping
LP
Li
Jian-Qi
JQ
D000818:Animals; D014150:Antipsychotic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D018491:Dopamine Agonists / Q000138:chemical synthesis* / Q000494:pharmacology*; D015195:Drug Design; D007546:Isoquinolines / Q000138:chemical synthesis / Q000494:pharmacology; D051379:Mice; D017448:Receptors, Dopamine D2; D013329:Structure-Activity Relationship
D014150:Antipsychotic Agents; D018491:Dopamine Agonists; D007546:Isoquinolines; D017448:Receptors, Dopamine D2