Rapid communicationClozapine has sub-micromolar affinity for 5-HT1A receptors in human brain tissue
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Cited by (65)
3D-QSAR studies of D<inf>3</inf>R antagonists and 5-HT<inf>1A</inf>R agonists
2019, Journal of Molecular Graphics and ModellingCitation Excerpt :The targets of 5HT1AR are N-methyl-d-aspartate (NMDA) receptor channels. Both of them affect cognitive functions by modulating the excitability of cortical neurons [8]. Three-dimensional quantitative structure-activity relationship (3D-QSAR) method, such as comparative molecular field analysis (CoMFA) [9], is an effective way to find small molecules that have certain promoted or inhibitory functions.
Serotonin in antipsychotic drugs action
2015, Behavioural Brain ResearchSynthesis and structure-activity relationship studies in serotonin 5-HT<inf>1A</inf> receptor agonists based on fused pyrrolidone scaffolds
2013, European Journal of Medicinal ChemistrySerotonin 1A receptor gene, schizophrenia and bipolar disorder: An association study and meta-analysis
2011, Psychiatry ResearchCitation Excerpt :Mason and Reynolds reported that one of the major pharmacological therapeutic targets of clozapine is 5-HT1A receptors on cortical glutamatergic neurons (Mason and Reynolds, 1992). These authors suggested that clozapine binding to 5-HT1A receptors may contribute to the mechanism of the unique efficacy of clozapine in schizophrenic patients (Mason and Reynolds, 1992). Recent pharmacogenetics studies reported that a SNP (C-1019G: rs6295) in the promoter region of the 5-HT1A receptor gene (HTR1A), which regulates HTR1A transcription (Lemonde et al., 2003; Le Francois et al., 2008), is associated with improved response in negative symptoms with antipsychotics such as risperidone (Reynolds et al., 2006; Wang et al., 2008; Mossner et al., 2009).
Serotonin 1A receptor gene is associated with Japanese methamphetamine-induced psychosis patients
2010, NeuropharmacologyCitation Excerpt :Stimulation of 5-HT1A receptors has been known to reduce the negative symptoms and cognitive dysfunction of schizophrenia (Meltzer et al., 2003; Meltzer and Sumiyoshi, 2008; Sumiyoshi et al., 2001, 2007). Mason and Reynolds (1992) reported that one of the major pharmacological therapeutic targets of clozapine is 5-HT1A receptors on cortical glutamatergic neurons. Several postmortem studies reported increased 5-HT1A receptor in the prefrontal cortex of schizophrenic patients (Burnet et al., 1996; Hashimoto et al., 1993, 1991; Simpson et al., 1996; Sumiyoshi et al., 1996).
Serotonergic approaches in the development of novel antipsychotics
2008, NeuropharmacologyCitation Excerpt :The antipsychotics risperidone, olanzapine and haloperidol have limited affinity for 5-HT1A receptors (Newman-Tancredi et al., 2005, 2007b; McCreary et al., 2007). However, ziprasidone, clozapine, nemonapride and aripiprazole have been described as putative 5-HT1A receptor (partial) agonists when tested in vitro (Mason and Reynolds, 1992; Newman-Tancredi et al., 1996, 1998, 2005; Burris et al., 2002; Jordan et al., 2002; Shapiro et al., 2003; Tadori et al., 2005; Cosi et al., 2006). Whilst this has not always translated into in vivo 5-HT1A agonist effects (Lejeune et al., 1994; Assié et al., 1997, 2005; Jordan et al., 2004; Zocchi et al., 2005; McCreary et al., 2007), some studies do suggest that these antipsychotics do have intrinsic activity at 5-HT1A receptors in vivo (Bartoszyk et al., 1996; Assié et al., 1997; Rollema et al., 1997; Millan et al., 1998; Ichikawa and Meltzer, 1999; Sprouse et al., 1999; Dahan et al., 2006; Bortolozzi, et al., 2007).