The selective 5-HT6 receptor antagonist Ro 04-6790 attenuates psychotomimetic effects of the NMDA receptor antagonist MK-801

Pitsikas, Nikolaos; Zisopoulou, Styliani; Pappas, Ioannis S.; Sakellaridis, Nikolaos

doi:10.1016/j.bbr.2007.11.010

Cited by 16 publications

(9 citation statements)

References 34 publications

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“…It has been shown that N-methyl D-aspartate NMDA receptor antagonists result into stereotypic movement disorder (32,33), while sulindac increases the NR1 and NR2B NMDA receptor subunits in aged Fischer 344 rats (34). NMDA receptors are vital for brain function and these receptors are central to many of the activity-dependent changes occurring in synaptic strength and connectivity (35).…”

Section: Discussionmentioning

confidence: 99%

Sulindac attenuates valproic acid-induced oxidative stress levels in primary cultured cortical neurons and ameliorates repetitive/stereotypic-like movement disorders in Wistar rats prenatally exposed to valproic acid

Zhang

Cailing

Yuan

et al. 2014

International Journal of Molecular Medicine

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Accumulating evidence suggests that anti-inflammatory agents and antioxidants have neuroprotective properties and may be beneficial in the treatment of neurodevelopental disorders, such as autism. In the present study, the possible neuroprotective properties of sulindac, a non-steroidal anti-inflammatory drug (NSAID), were investigated in vitro using cultured cortical neurons with valproic acid (VPA)-induced neurotoxicity, as well as in vivo through the behavioral analysis of rats prenatally exposed to VPA as a model of autism. VPA induced 4-hydroxynonenal (4-HNE) expression, reactive oxygen species (ROS) generation and decreased cell viability in primary cultured cortical neurons established from timed-pregnant (embryonic day 18) Wistar rat pups. However, co-incubation of the neurons with VPA and sulindac reduced oxidative stress and increased cell viability. The rats were administered an intraperitoneal injection with one of the following: VPA, sulindac, VPA and sulindac, or physiological saline, and their offspring were subjected to the open field test. During the test trials, repetitive/stereotypic-like movements for each rat were recorded and analyzed. The results revealed that treatment with both sulindac and VPA reduced the VPA-induced repetitive/stereotypic-like activity and the sulindac and VPA-treated animals responded better in the open field test compared to the VPA-treated animals. The results from the present study demonstrate that the antioxidant properties of sulindac may prove to be beneficial in the treatment of autism, suggesting that the upregulation of the Wnt/β-catenin signaling pathway disrupts oxidative homeostasis and facilitates susceptibility to autism.

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Section: Discussionmentioning

confidence: 99%

Sulindac attenuates valproic acid-induced oxidative stress levels in primary cultured cortical neurons and ameliorates repetitive/stereotypic-like movement disorders in Wistar rats prenatally exposed to valproic acid

Zhang

Cailing

Yuan

et al. 2014

International Journal of Molecular Medicine

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“…Recent interest in the 5-HT 6 receptor in relation to the action of APDs has been based, in part, on the finding that some APDs, including atypical APDs like clozapine, olanzapine, and sertindole, are relatively potent 5-HT 6 receptor antagonists (Monsma et al 1993;Roth et al 1994;Kohen et al 1996;Arnt and Skarsfeldt 1998;Boess et al 1998). A selective 5-HT 6 antagonist, Ro 04-6790, attenuated the acute MK-801-induced deficit in NOR in rats (Pitsikas et al 2008). King et al (2009) examined the impact of regional 5-HT depletion on the cognitive enhancing effect of Ro 04-6790 in the NOR task.…”

Section: The Effect Of 5-ht 2a Receptor Agents On Nor Deficits Inducementioning

confidence: 98%

The role of serotonin in the NMDA receptor antagonist models of psychosis and cognitive impairment

2011

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“…There is considerable evidence that 5‐HT 6 receptor antagonists play a role in improving cognition in animal models of schizophrenia . The selective 5‐HT 6 receptor antagonists attenuated the NMDA receptor antagonists‐induced deficits in NOR . The 5‐HT 6 receptor antagonists have been shown to increase acetylcholine efflux in the cortex and to potentiate both haloperidol‐ and risperidone‐induced dopamine release in the prefrontal cortex or the hippocampus …”

Section: Binding Profile and Neurotransmitter Regulationsmentioning

confidence: 99%

“…12,47 The selective 5-HT6 receptor antagonists attenuated the NMDA receptor antagonists-induced deficits in NOR. 48,49 The 5-HT6 receptor antagonists have been shown to increase acetylcholine efflux in the cortex 50 and to potentiate both haloperidol-and risperidone-induced dopamine release in the prefrontal cortex or the hippocampus. 51 5-HT7 receptor 5-HT7 receptors are involved in the control of circadian rhythms, sleep, pain, and cognitive processes, including learning and memory.…”

Section: -Ht6 Receptormentioning

confidence: 99%

Psychopharmacology of atypical antipsychotic drugs: From the receptor binding profile to neuroprotection and neurogenesis

Kusumi

Boku

Takahashi

2014

Psychiatry Clin Neurosci

143

128

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The original definition of atypical antipsychotic drugs (APD) was drugs that are effective against positive symptoms in schizophrenia with no or little extrapyramidal symptoms (EPS). However, atypical APD have been reported to be more effective for cognitive dysfunction and negative symptoms in schizophrenia than typical APD, which expands the definition of 'atypicality'. This article provides a critical review of the pharmacology of atypical APD, especially from the viewpoint of receptor binding profiles and neurotransmitter regulations as well as neuroprotection and neurogenesis. A variety of serotonin (5-HT) receptors, such as 5-HT2A/2C, 5-HT1A, 5-HT6 and 5-HT7 receptors, may contribute to the mechanisms of action of 'atypicality'. The dopaminergic modulations, including a low affinity for dopamine D2 receptors and a partial D2 receptor agonistic action, and glutamatergic regulations may also be involved in the pharmacological backgrounds of 'atypicality'. Atypical APD, but not typical APD, may facilitate cortical neuroprotection and hippocampal neurogenesis, which might be a part of the action mechanisms of atypical APD. The facilitation of cortical neuroprotection and hippocampal neurogenesis induced by atypical APD might be mediated by an increase in the Ser9 phosphorylation of glycogen synthase kinase-3β (GSK-3β). The stimulation of 5-HT1A receptors and/or the blockade of 5-HT2 receptors, which is characteristic of atypical APD, might increase Ser9 phosphorylation of GSK-3β. Moreover, atypical APD increase brain-derived neurotrophic factor (BDNF) levels. BDNF increases Ser9 phosphorylation of GSK-3β and has neuroprotective and neurogenic effects, as in the case of atypical APD. These findings suggest that GSK-3β might play a role in the action mechanisms of atypical APD, in both the 5-HT-dependent and BDNF-dependent mechanisms.Key words: atypicality, brain-derived neurotrophic factor, dopamine, glycogen synthase kinase-3β, serotonin.A TYPICAL ANTIPSYCHOTIC DRUGS (APD) or second-generation antipsychotics have been chiefly used for the treatment of schizophrenia. Typical APD or first-generation antipsychotics often produce extrapyramidal side-effects, including parkinsonism and tardive dyskinesia, which are thought to be a consequence of dopamine D2 receptor blockade in the nigrostriatal dopamine system. 1 On the other hand, atypical APD have a limited tendency to provoke catalepsy in rodents and to produce extrapy-

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The selective 5-HT6 receptor antagonist Ro 04-6790 attenuates psychotomimetic effects of the NMDA receptor antagonist MK-801

Cited by 16 publications

References 34 publications

Sulindac attenuates valproic acid-induced oxidative stress levels in primary cultured cortical neurons and ameliorates repetitive/stereotypic-like movement disorders in Wistar rats prenatally exposed to valproic acid

Sulindac attenuates valproic acid-induced oxidative stress levels in primary cultured cortical neurons and ameliorates repetitive/stereotypic-like movement disorders in Wistar rats prenatally exposed to valproic acid

The role of serotonin in the NMDA receptor antagonist models of psychosis and cognitive impairment

Psychopharmacology of atypical antipsychotic drugs: From the receptor binding profile to neuroprotection and neurogenesis

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