Overview—Flavonoids: A New Family of Benzodiazepine Receptor Ligands View Full Text


Ontology type: schema:ScholarlyArticle     


Article Info

DATE

1997-04

AUTHORS

Jorge H. Medina, Haydee Viola, Claudia Wolfman, Mariel Marder, Cristina Wasowski, Daniel Calvo, Alejandro C. Paladini

ABSTRACT

Benzodiazepines (BDZs) are the most widely prescribed class of psychoactive drugs in current therapeutic use, despite the important unwanted side-effects that they produce such as sedation, myorelaxation, ataxia, amnesia, ethanol and barbiturate potentiation and tolerance. Searching for safer BDZ-receptor (BDZ-R) ligands we have recently demonstrated the existence of a new family of ligands which have a flavonoid structure. First isolated from plants used as tranquilizers in folkloric medicine, some natural flavonoids have shown to possess a selective and relatively mild affinity for BDZ-Rs and a pharmacological profile compatible with a partial agonistic action. In a logical extension of this discovery various synthetic derivatives of those compounds, such as 6,3′-dinitroflavone were found to have a very potent anxiolytic effect not associated with myorelaxant, amnestic or sedative actions. This dinitro compound, in particular, exhibits a high affinity for the BDZ-Rs (Ki = 12–30 nM). Due to their selective pharmacological profile and low intrinsic efficacy at the BDZ-Rs, flavonoid derivatives, such as those described, could represent an improved therapeutic tool in the treatment of anxiety. In addition, several flavone derivatives may provide important leads for the development of potent and selective BDZ-Rs ligands. More... »

PAGES

419-425

Identifiers

URI

http://scigraph.springernature.com/pub.10.1023/a:1027303609517

DOI

http://dx.doi.org/10.1023/a:1027303609517

DIMENSIONS

https://app.dimensions.ai/details/publication/pub.1000348618

PUBMED

https://www.ncbi.nlm.nih.gov/pubmed/9130252


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