DL-Menthol ((±)-Menthol) is a racemic mixture of the monoterpene alcohols (–)-menthol and (+)-menthod, which have been found in Cannabis. (–)-Menthol is more common than (+)-menthol in nature and exhibits analgesic, antibacterial, and anticancer properties, as well as inhibits cholinesterase.2 (+)-Menthol inhibits the growth of F. verticillioides (MIC: 1.5 mM) but, unlike (–)-menthol, does not exhibit analgesic, antibacterial, anticancer, or cholinesterase inhibitory activities.

3,4,5-Trimethoxycinnamic acid (O-Methylsinapic acid) (TMCA) is one of the constituents of Polygalae Radix and may exert anti-seizure activity by acting at the GABAA/BZ receptor complex.

Amentoflavone (3',8''-Biapigenin), as a potent inhibitor of CYP3A4 and CYP2C9, can interact with many other medications. CYP3A4 and CYP2C9 are proteins used for drug metabolism in the body. Amentoflavone also is an inhibitor of human cathepsin B. It has antimalarial activity in trials significant affinities towards the Delta-1, kappa opioid receptors (as an antagonist) and binds to benzodiazepine receptors. Amentoflavone may be a potential lead for a new type of anti-inflammatory agents having the dual inhibitory activity of group II phospholipase A2 and cyclooxygenase. Amentoflavone and quercetin differentially exerted suppression of PGE2 biosynthesis via downregulation of COX-2/iNOS expression.

Cholesterol Myristate (Cholesteryl Myristate) is a natural steroid found in traditional Chinese medicine that interacts with various ion channels, including the GABAA receptor, nicotinic acetylcholine receptor, and the inward-rectifier potassium ion channel.

Arecaidine hydrochloride may have carcinogenesis.

Songorine (Napellonine) shows favorable anti-tumor activity in preliminary pharmacological verification trials including cell proliferation and molecular docking assays.

L-DABA (L-2,4-Diaminobutyric acid) is an inhibitor of GABA transaminase (IC50 > 500 μM).

Ginkgolide A (BN-52020) is a highly active PAF antagonist cage molecule that is isolated from the leaves of the Ginkgo biloba tree. Shows potential in a wide variety of inflammatory and immunological disorders.

Kavain, a compound extracted from the Kava plant, Piper methysticum, is found to be involved in TNF-α expression in human and mouse cells via regulation of transcriptional factors such as NF-kB and LITAF.

6,2'-Dihydroxyflavone is a novel antagonist of GABAA receptor.

Bicuculline ((+)-Bicuculline) is a light-sensitive competitive antagonist of GABAA receptors. It was originally identified in 1932 in plant alkaloid extracts and has been isolated from Dicentra cucullaria, Adlumia fungosa, Fumariaceae, and several Corydalis species.

(+)-Kavain ((R)-KAWAIN) is one of the six major kavalactones found in the Piper methysticum (kava) plant; reversible inhibitor of MAO-B.

(-)-Securinine (Securinine) is plant-derived alkaloid and also a GABAA receptor antagonist.

γ-Aminobutyric acid (4-Aminobutyric acid) is the most common inhibitory neurotransmitter in the central nervous system.

alpha-Asarone (trans-Asarone) is a psychoactive compound with antidepressant-like activity in mice.

Jujuboside A is a glycoside extracted from Semen Ziziphi Spinosae, having neurophysiological inhibitory effects, used as a potential therapeutic agent for the treatment of Alzheimer s disease.

4-Acetamidobutanoic acid (4-ACETAMIDOBUTYRIC ACID) can be found in blood, feces, and urine, as well as in human prostate tissue. 4-Acetamidobutanoic acid exists in all eukaryotes, ranging from yeast to humans. 4-Acetamidobutanoic acid is a GABA derivative, a product of the urea cycle and the metabolism of amino groups, and the product of NAD-linked aldehyde dehydrogenase (EC 1.2.1.3) (KEGG).

Dihydroergotoxine mesylate (Ergoloid mesylates) is mainly used to improve symptoms and physical symptoms of mental degeneration related to aging.

Cirsimaritin exhibits antibacterial, anti-inflammation, anti-tumor, antioxidant properties and renal protection. Cirsimaritin binds weakly to the benzodiazepine site on GABAA receptors.

Thiocolchicoside (Thiocolchicine 2-glucoside analog) (Muscoril, Myoril, Neoflax) is a muscle relaxant with anti-inflammatory and analgesic effects. It acts as a competitive GABAA receptor antagonist and also glycine receptor antagonist with similar potency and nicotinic acetylcholine receptors to a much lesser extent. It has powerful convulsant activity and should not be used in seizure-prone individuals.

Guvacine hydrochloride is an inhibits of GABA uptake (IC50 : 10 μM)

Bemegride (3-Ethyl-3-methylglutarimide), a central nervous system stimulant, serves as an antidote for barbiturate poisoning.

Ginsenoside Rc (Panaxoside Rc) is one of the ginsenosides from Panax ginseng, inhibits the expression of TNF-α and IL-1β.

(-)-α-Pinene ((1S)-(-)-Alpha-Pinene) enhances the quantity of NREMS without affecting the intensity of NREMS by prolonging GABAergic synaptic transmission, acting as a partial modulator of GABAA-BZD receptors and directly binding to the BZD binding site of GABAA receptor.

(2S)-6-Prenylnaringenin (6-Prenylnaringenin) is an isomer of the potent phytoestrogen, 8-prenylnaringenin. (2S)-6-Prenylnaringenin is the most potent compound in the forebrain and acts as a positive allosteric modulator of GABAA at the α+β binding site.

(E)-3,4,5-Trimethoxycinnamic acid (O-Methylsinapic acid) is a natural product from the roots and rhizomes of Notopterygium incisum.

α-Thujone is an inhibitor of ACh with an IC50 value of 24.7μM.

2'-O-Methylisoliquiritigenin, a compound synthesized by enzymes specifically induced in NR.2'-O-Methylisoliquiritigenin, isolated from the Arachis species, up-regulates 5-HT, NE, DA and GABA pathways, but does not put a very significant effect on ne NE pathway.

6-Methylflavone is an activator of α1β2γ2L and α1β2 GABAA receptors.

1. p-Hydroxybenzaldehyde (p-Oxybenzaldehyde) shows an inhibitory effect on the GABA transaminase to contribute to an antiepileptic and anticonvulsive activity, and its inhibitory activity was higher than that of valproic acid, a known anticonvulsant.

1. Pulegone ((+)-Pulegone) has cytotoxicity followed by regenerative cell proliferation is the MOA for Pulegone-induced urothelial tumors in female rats. 2. Pulegone induces a verapamil-sensitive psychostimulant effect that appears to independ on the opening of L-type calcium channels. 3. Pulegone has negative reinforcing properties and seems to possess anxiolytic-like actions unrelated to the benzodiazepine site of the γ-aminobutyric acid type A (GABAA) receptor.

Miltirone is a CYPs inhibitor, it has been characterized as a low-affinity ligand for central benzodiazepine receptors.