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Metabotropic glutamate (mGlu) receptors are expressed in key regions of the cortex and the thalamus and are known to regulate spike and wave discharges (SWDs), the electroclinical hallmarks of absence seizures. Recent preclinical studies have highlighted the therapeutic potential of selective group I and III mGlu receptor subtype allosteric modulators, which can suppress pathological SWDs. Of particular interest are positive allosteric modulators (PAMs) for mGlu5 receptors, as they currently show the most promise as novel anti-absence epilepsy drugs. The rational design of novel selective positive and negative allosteric mGlu modulators, especially for the mGlu5 receptor, has been made possible following the recent crystallographic structure determination of group I mGlu receptors. Our current knowledge of the role of different mGlu receptor subtypes in absence epilepsy is outlined in this article. [Abstract copyright: Copyright © 2018. Published by Elsevier Ltd.]

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Autor(es)

Ngomba, Richard Teke -  van Luijtelaar, Gilles - 

Id.: 71193345

Idioma: inglés  - 

Versión: 1.0

Estado: Final

Tipo:  application/pdf - 

Palabras claveB200 Pharmacology, Toxicology and Pharmacy - 

Tipo de recurso: Article  -  PeerReviewed  - 

Tipo de Interactividad: Expositivo

Nivel de Interactividad: muy bajo

Audiencia: Estudiante  -  Profesor  -  Autor  - 

Estructura: Atomic

Coste: no

Copyright: sí

Formatos:  application/pdf - 

Requerimientos técnicos:  Browser: Any - 

Relación: [References] http://eprints.lincoln.ac.uk/31432/
[References] 10.1016/j.coph.2018.01.012

Fecha de contribución: 11-abr-2018

Contacto:

Localización:
* Ngomba, Richard Teke and van Luijtelaar, Gilles (2018) Metabotropic glutamate receptors as drug targets for the treatment of absence epilepsy. Current Opinion in Pharmacology, 38 . pp. 43-50. ISSN 1471-4892

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