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Phenolics as GABA-A receptor ligands:an updated review

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Phenolics as GABA-A receptor ligands:an updated review

dc.contributor.author	Ríos Cañavate, José Luis
dc.contributor.author	Schinella, Guillermo
dc.contributor.author	Moragrega Vergara, Inés
dc.date.accessioned	2023-06-20T11:01:07Z
dc.date.available	2023-06-20T11:01:07Z
dc.date.issued	2022
dc.identifier.citation	Ríos Cañavate, José Luis Schinella, Guillermo Moragrega Vergara, Inés 2022 Phenolics as GABA-A receptor ligands:an updated review Molecules 27 1770 1 29
dc.identifier.uri	https://hdl.handle.net/10550/88358
dc.description.abstract	Natural products can act as potential GABA modulators, avoiding the undesirable effects of traditional pharmacology used for the inhibition of the central nervous system such as benzodiazepines (BZD). Phenolics, especially flavonoids and phlorotannins, have been considered as modulators of the BZD-site of GABAA receptors (GABAARs), with sedative, anxiolytic or anticonvulsant effects. However, the wide chemical structural variability of flavonoids shows their potential action at more than one additional binding site on GABAARs, which may act either negatively, positively, by neutralizing GABAARs, or directly as allosteric agonists. Therefore, the aim of the present review is to compile and discuss an update of the role of phenolics, namely as pharmacological targets involving dysfunctions of the GABA system, analyzing both their different compounds and their mechanism as GABAergic modulators. We focus this review on articles written in English since the year 2010 until the present. Of course, although more research would be necessary to fully establish the type specificity of phenolics and their pharmacological activity, the evidence supports their potential as GABAAR modulators, thereby favoring their inclusion in the development of new therapeutic targets based on natural products. Specifically, the data compiled in this review allows for the directing of future research towards ortho-dihydroxy diterpene galdosol, the flavonoids isoliquiritigenin (chalcone), rhusflavone and agathisflavone (biflavonoids), as well as the phlorotannins, dieckol and triphlorethol A. Clinically, flavonoids are the most interesting phenolics due to their potential as anticonvulsant and anxiolytic drugs, and phlorotannins are also of interest as sedative agents.
dc.language.iso	eng
dc.relation.ispartof	Molecules, 2022, vol. 27, num. 1770, p. 1-29
dc.subject	Sistema nerviós central Malalties
dc.subject	Psicobiologia
dc.subject	Psicofarmacologia
dc.title	Phenolics as GABA-A receptor ligands:an updated review
dc.type	journal article
dc.date.updated	2023-06-20T11:01:08Z
dc.identifier.doi	10.3390/molecules27061770
dc.identifier.idgrec	160525
dc.rights.accessRights	open access