Table 1.

Flavonols with relevant GABAergic effects.

Flavonol
Compound	Properties	Reference
Quercetin (5,7,3′,4′-tetrahydroxy)	Quercetin acts as a negative allosteric GABAAR modulator with antipsychotic activity. These results justify further therapeutic development of the excitatory-inhibitory imbalance disorders.	[69]
	Quercetin antagonistic actions on GABAAρ₁Rs are mediated through a redox-independent allosteric mechanism.	[70]
	GABAAα5R could be a mechanism for reducing seizure severity (at anticonvulsive doses) or even be used a marker of seizure severity.	[71]
	Quercetin and its glycosides (rutin and isoquercitrin) are partially responsible for the anxiolytic and sedative-like effect of Tilia americana var. mexicana through the GABA/BZD and serotoninergic 5-HT1A receptors.	[72]
Fisetin (7,3′,4′-trihydroxy)	Treatment with fisentin can delay or correct neuropathic hyperalgesia and allodynia in mice with type 1 diabetes. The analgesia caused by fisetin may be linked with its antioxidant activity. Spinal GABAARs are likely rendered as downstream targets.	[73]
Myricetin (3,5,7,3′,4′,5′-pentahydroxy)	Myricetin enhances GABAAR activity via the calcium channel/Ca2+/calmodulin-dependent protein kinase II dependent mechanism, which is distinctively different from that of most existing BZD-binding site agonists of GABAAR.	[74]
Viscosine (5,7,4′-trihydroxy-3,6-dimethoxy)	The anxiolytic and anticonvulsant actions of viscosine are likely mediated via its positive allosteric modulatory action at different GABAAR subtypes.	[75]
Glycosides
Rutin (quercetin 3-O-rutinoside)	The anxiolytic-like effect involves GABAergic neurotransmission without implication of BZD receptors.	[76]
Rutin (quercetin 3-O-rutinoside) Isoquercitrin (quercetin-3-O-glucoside)	Leaves of Tilia americana var. mexicana have anxiolytic and sedative-like effects and its flavonoids, quercetin, rutin and isoquercitrin, are partially responsible due to the involvement of GABA/BZD and serotoninergic 5-HT1A receptors.	[72]