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Dual orexin receptor antagonists - promising agents in the treatment of sleep disorders.
Palasz, Artur; Lapray, Damien; Peyron, Christelle; Rojczyk-Golebiewska, Ewa; Skowronek, Rafal; Markowski, Grzegorz; Czajkowska, Beata; Krzystanek, Marek; Wiaderkiewicz, Ryszard.
Afiliación
  • Palasz A; Department of Histology and Embryology, Medical University of Silesia, Katowice, Poland.
Int J Neuropsychopharmacol ; 17(1): 157-68, 2014 Jan.
Article en En | MEDLINE | ID: mdl-23702225
ABSTRACT
Insomnia is a serious medical and social problem, its prevalence in the general population ranges from 9 to 35% depending on the country and assessment method. Often, patients are subject to inappropriate and therefore dangerous pharmacotherapies that include prolonged administration of hypnotic drugs, benzodiazepines and other GABAA receptor modulators. This usually does not lead to a satisfactory improvement in patients' clinical states and may cause lifelong drug dependence. Brain state transitions require the coordinated activity of numerous neuronal pathways and brain structures. It is thought that orexin-expressing neurons play a crucial role in this process. Due to their interaction with the sleep-wake-regulating neuronal population, they can activate vigilance-promoting regions and prevent unwanted sleep intrusions. Understanding the multiple orexin modulatory effects is crucial in the context of pathogenesis of insomnia and should lead to the development of novel treatments. An important step in this process was the synthesis of dual antagonists of orexin receptors. Crucially, these drugs, as opposed to benzodiazepines, do not change the sleep architecture and have limited side-effects. This new pharmacological approach might be the most appropriate to treat insomnia.
Asunto(s)

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Piperidinas / Pirimidinas / Azepinas / Tiazoles / Triazoles / Benzofuranos / Antagonistas de los Receptores de Orexina / Trastornos del Inicio y del Mantenimiento del Sueño / Isoquinolinas / Acetamidas Tipo de estudio: Risk_factors_studies Límite: Animals / Humans Idioma: En Revista: Int J Neuropsychopharmacol Asunto de la revista: NEUROLOGIA / PSICOFARMACOLOGIA Año: 2014 Tipo del documento: Article País de afiliación: Polonia

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Piperidinas / Pirimidinas / Azepinas / Tiazoles / Triazoles / Benzofuranos / Antagonistas de los Receptores de Orexina / Trastornos del Inicio y del Mantenimiento del Sueño / Isoquinolinas / Acetamidas Tipo de estudio: Risk_factors_studies Límite: Animals / Humans Idioma: En Revista: Int J Neuropsychopharmacol Asunto de la revista: NEUROLOGIA / PSICOFARMACOLOGIA Año: 2014 Tipo del documento: Article País de afiliación: Polonia