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Differential Regulation of Rat 5-HT2A and 5-HT2C Receptors after Chronic Treatment with Clozapine, Chlorpromazine and Three Putative Atypical Antipsychotic Drugs
TLDR
This study characterized the interaction of chlorpromazine (CPZ) and three putative atypical antipsychotic drugs, risperidone (RIS), amperozide (AMP), and ORG 5222 (ORG), and found that 5-HT2A and 5- HT2C receptors are differentially regulated after chronic treatment with CLOZ, CPZ, RIS, AMP, and OrG. Expand
Interactions of selective serotonin reuptake inhibitors with the serotonin 5-HT2C receptor
TLDR
Evidence is provided that fluoxETine, norfluoxetine and citalopram, along with many other antidepressant compounds, interact directly with the 5-HT2C receptor. Expand
Sertindole is a serotonin 5-HT2c inverse agonist and decreases agonist but not antagonist binding to 5-HT2c receptors after chronic treatment
TLDR
The preferential downregulation of 5-HT2C receptor agonist (G-protein-coupled) sites by chronic administration seemed to differentiate sertindole from clozapine at these dose regimens, suggesting that the 5- HT2c receptor downregulation during repeated dosing may contribute to therapeutic efficacy and/or side effects of sERTindole treatment. Expand
Serotonin 5-HT2C receptor-mediated phosphoinositide hydrolysis in rat choroid plexus after fluoxetine and citalopram treatments.
TLDR
It is suggested that sensitisation of 5-HT2C receptor-mediated intracellular signal transduction may play a role in the effects of citalopram, and may explain some of the pharmacodynamic differences seen with these drugs, especially upon repeated administration. Expand
Chronic Citalopram and Fluoxetine Treatments Upregulate 5-HT2C Receptors in the Rat Choroid Plexus
TLDR
The results show that chronic citalopram and fluoxetine treatments induce an increase of choroid plexus 5-HT2C receptor density, but the effect is more marked with citalsopram. Expand
Dopamine D2 receptor gene expression in rat lines selected for differences in voluntary alcohol consumption.
TLDR
The baseline differences in D1 or D2 receptors binding and D2 receptor gene expression between AA and ANA rat lines are marginal, and are not likely to play a role in the genetic background of the differential alcohol drinking behavior of these rat lines. Expand
Combined treatment with citalopram and buspirone: effects on serotonin 5-HT2A and 5-HT2C receptors in the rat brain.
TLDR
It is suggested that downregulation of brain 5- HT2A receptors and possibly of 5-HT2C receptor agonist sites is involved in the beneficial clinical effects of buspirone-SSRI augmentation treatment. Expand
Deramciclane, a putative anxiolytic drug, is a serotonin 5-HT2C receptor inverse agonist but fails to induce 5-HT2C receptor down-regulation
TLDR
Data indicate that deramciclane is a 5- HT2C receptor inverse agonist and occupies 5-HT2C receptors during treatment, and that chronic treatment with deramCiclane does not lead to5-HT 2C receptor down-regulation. Expand
Differential effects of fluoxetine and citalopram treatments on serotonin 5-HT(2C) receptor occupancy in rat brain.
TLDR
Ex vivo receptor occupancy measurements provide evidence that direct occupancy of 5-HT(2C) receptors may contribute to the mechanism of action of fluoxetine, and demonstrate pharmacodynamic differences between fluoxettine and citalopram at the level of5-HT-2C receptors. Expand
5-HT1C receptor-mediated phosphoinositide hydrolysis in the rat choroid plexus after chronic treatment with clozapine.
TLDR
Quantitative 5-HT1C receptor autoradiography indicated that chronic clozapine treatment decreased, in a dose-related manner,5-HT 1C receptor binding sites labeled by antagonist and agonist radioligands, which strengthens the possibility that 5- HT1C receptors may contribute to some of the atypical effects of clozAPine. Expand
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