Role OF 5-HT2C receptors in dyskinesia
| Autor: | Anton J.M. Loonen, Ivanova, Svetlana A. |
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| Přispěvatelé: | PharmacoTherapy, -Epidemiology and -Economics, Real World Studies in PharmacoEpidemiology, -Genetics, -Economics and -Therapy (PEGET) |
| Jazyk: | angličtina |
| Rok vydání: | 2016 |
| Předmět: |
side effect
olanzapine ziprasidone protein localization GABAergic transmission haloperidol serotonin 2A receptor aripiprazole pipamperone Tardive dyskinesia binding affinity ventral striatum substantia nigra pars compacta human 5-HT2C receptors protein expression Extrapyramidal system parkinsonism Medium spiny neurons prefrontal cortex risperidone clozapine serotonin 2C receptor dopamine 2 receptor drug receptor binding serotoninergic system article quetiapine nerve cell stimulation receptor blocking dopamine 3 receptor asenapine Inverse agonism substantia nigra pars reticulata drug induced disease sertindole ritanserin paliperidone |
| Zdroj: | International Journal of Pharmacy and Pharmaceutical Sciences, 8(1), 5-10. International Journal of Pharmacy and Pharmaceutical Science University of Groningen |
| ISSN: | 0975-1491 |
| Popis: | By integrating knowledge gained by pharmacogenetic, neuroanatomical and pharmacological studies, a model can be constructed how serotonin (5-HT) affects the vulnerability to induce tardive dyskinesia. From neuroanatomical studies, it can be concluded that 5-HT inhibits the release of dopamine (DA) within the dorsal striatum by affecting 5-HT2C receptors and also within the ventral striatum and prefrontal cortex by affecting 5-HT2A receptors. However, considering the low affinity of DA for its receptors, it is unlikely that the so released DA is able to displace atypical antipsychotics from DA D2 and D3 receptors. 5-HT2C receptors and, to a lesser extent, 5-HT2A receptors, have constitutive activity and therefore, atypical antipsychotics can have inverse agonistic effects. It is hypothesized that decreasing the activity of 5-HT2 receptor carrying medium spiny neurons (MSNs) within the dorsal striatum represents the mechanism showing how atypical antipsychotics have limited ability to cause tardive dyskinesia. |
| Databáze: | OpenAIRE |
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