clozapine has been researched along with piperidine* in 3 studies
3 other study(ies) available for clozapine and piperidine
| Article | Year |
|---|---|
Discovery of aryl-piperidine derivatives as potential antipsychotic agents using molecular hybridization strategy.
Schizophrenia is a chronic, disabling mental disorder that affects about one percent of world's population. Drugs acting on multiple targets have been demonstrated to provide superior efficacy in schizophrenia than agents acting on single target. In this study, based on FW01, a selective potent 5-HT Topics: Animals; Antipsychotic Agents; Dose-Response Relationship, Drug; Drug Discovery; HEK293 Cells; Humans; Mice; Mice, Inbred ICR; Models, Molecular; Molecular Structure; Piperidines; Receptor, Serotonin, 5-HT1A; Receptors, Dopamine D2; Serotonin Antagonists; Structure-Activity Relationship | 2020 |
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 |
4-N-linked-heterocyclic piperidine derivatives with high affinity and selectivity for human dopamine D4 receptors.
The syntheses of a number of different N-linked heterocyclic pyrazole replacements based on the structure 1 are described (compounds 3-12) as hD4 ligands. After further optimisation the best compound identified was 13 which has high affinity for hD4 (5.2 nM) and >300-fold selectivity for hD4 receptors over hD2 and hD3 receptors. Topics: Animals; CHO Cells; Clozapine; Cricetinae; Humans; Kinetics; Piperidines; Receptors, Dopamine D2; Receptors, Dopamine D4; Serotonin Antagonists | 1999 |