Herbal Remedies and Their Possible Effect on the GABAergic System and Sleep

Nutrients. 2021 Feb 6;13(2):530. doi: 10.3390/nu13020530.


Sleep is an essential component of physical and emotional well-being, and lack, or disruption, of sleep due to insomnia is a highly prevalent problem. The interest in complementary and alternative medicines for treating or preventing insomnia has increased recently. Centuries-old herbal treatments, popular for their safety and effectiveness, include valerian, passionflower, lemon balm, lavender, and Californian poppy. These herbal medicines have been shown to reduce sleep latency and increase subjective and objective measures of sleep quality. Research into their molecular components revealed that their sedative and sleep-promoting properties rely on interactions with various neurotransmitter systems in the brain. Gamma-aminobutyric acid (GABA) is an inhibitory neurotransmitter that plays a major role in controlling different vigilance states. GABA receptors are the targets of many pharmacological treatments for insomnia, such as benzodiazepines. Here, we perform a systematic analysis of studies assessing the mechanisms of action of various herbal medicines on different subtypes of GABA receptors in the context of sleep control. Currently available evidence suggests that herbal extracts may exert some of their hypnotic and anxiolytic activity through interacting with GABA receptors and modulating GABAergic signaling in the brain, but their mechanism of action in the treatment of insomnia is not completely understood.

Keywords: GABA receptors; gamma-aminobutyric acid; herbal medicine; insomnia; sleep.

Publication types

  • Systematic Review

MeSH terms

  • Brain / metabolism
  • Humans
  • Phytotherapy / methods*
  • Receptors, GABA / drug effects*
  • Sleep / drug effects*
  • Sleep Initiation and Maintenance Disorders / drug therapy*
  • Sleep Initiation and Maintenance Disorders / metabolism
  • Sleep Wake Disorders / drug therapy*
  • Sleep Wake Disorders / metabolism


  • Receptors, GABA

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