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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
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