dizocilpine-maleate has been researched along with piperidine* in 1 studies
1 other study(ies) available for dizocilpine-maleate and piperidine
| Article | Year |
|---|---|
Synthesis and evaluation of a series of piperidine-2,6-dione-piperazine (piperidine) derivatives as multireceptor atypical antipsychotics.
In this paper, we report the discovery and the synthesis of novel, potential antipsychotic piperidine-2,6-dione derivatives combining potent dopamine D(2) , D(3) and serotonin 5-HT(1A) , 5-HT(2A) , 5-HT(2C) receptor properties. We describe the structure-activity relationships that led us to the promising derivative: 1-(4-(4-(6-fluorobenzo[d]isoxazol-3-yl)piperidin-1-yl)butyl)-4-(4-chlorophenyl)-piperidine-2,6-dione 5. The unique pharmacological features of compound 5 are a high affinity for dopamine D(2) , D(3) and serotonin 5-HT(1A) , 5-HT(2A) , 5-HT(2C) receptors, together with a low affinity for the H(1) receptor (to reduce the risk of obesity under chronic treatment). In a behavioral model predictive of positive symptoms, compound 5 inhibited apomorphine-induced climbing behavior and MK-801-induced hyperactivity with no extrapyramidal symptoms liability in mice. In particular, compound 5 was more potent than clozapine. Topics: Animals; Antipsychotic Agents; Apomorphine; Behavior, Animal; Clozapine; Disease Models, Animal; Dizocilpine Maleate; Mice; Piperidines; Rats; Rats, Sprague-Dawley; Receptors, Dopamine; Receptors, Histamine H1; Receptors, Serotonin; Structure-Activity Relationship | 2012 |