Skip to content
2000
Volume 10, Issue 9
  • ISSN: 1381-6128
  • E-ISSN: 1873-4286

Abstract

The enhancement of GABA-mediated synaptic transmission underlies the pharmacotherapy of various neurological diseases. GABAA receptors are thus targets for neuroactive drugs, including classical benzodiazepines, mediating their anxiolytic, hypnotic and anticonvulsant effects via the benzodiazepine site (BZS). Based on findings that low intrinsic efficacy and subtype selectivity can greatly improve the specificity of drugs targeting the BZS, recent research has identified possible drug leads with apparently little side effects. In particular, drug leads of natural sources have been identified as promising candidates. This review describes the advances in the design of effective therapeutics targeting the GABAA receptor, focusing on the more recent research on naturally occurring drug leads. This includes discussion on the isolation of neuroactive alkaloids and flavonoids from herbal medicines and their rational development based on structure-activity relationships studies. Interest in the development of effective therapeutics from natural sources is clear and awaits to be seen whether their medicinal potential can be fulfilled.

Loading

Article metrics loading...

/content/journals/cpd/10.2174/1381612043452767
2004-04-01
2025-02-19
Loading full text...

Full text loading...

/content/journals/cpd/10.2174/1381612043452767
Loading

  • Article Type:
    Review Article
Keyword(s): alkaloids; benzodiazepine; flavonoids; gabaa receptor
This is a required field
Please enter a valid email address
Approval was a Success
Invalid data
An Error Occurred
Approval was partially successful, following selected items could not be processed due to error
Please enter a valid_number test