1. Methyl eugenol (4-allylveratrole) is a natural constituent of the essential oils of a number of plants widely used in foodstuffs as flavouring agents, in view of the carcinogenic potential of ME, the need to check its presence in food products with effective analytical methods. 2. Methyleugenol has insecticidal properties. 3. Methyleugenol can inhibit the production of nitric oxide and decreased the protein expression of inducible nitric oxide synthase, it down-regulates the production of pro-inflammatory cytokines in the ischemic brain as well as in immunostimulated mixed glial cells; indicates that methyleugenol could be useful for the treatment of ischemia/inflammation-related diseases. 4. Methyleugenol has cytotoxicity and genotoxicity. 5. Intravenous (i.v.) treatment with methyleugenol (ME) in either anesthetized or conscious rats elicits hypotension, an effect that seems related to an active vascular relaxation rather than withdrawal of sympathetic tone. 6. Methyleugenol has antinociceptive effect on the second phase of formalin-induced pain, may be due to the inhibition of N-methyl-d-aspartic acid (NMDA) receptor-mediated hyperalgesia via GABA(A) receptors. 7. Methyleugenol has elaxant and antispasmodic actions on guinea-pig isolated ileum.

Xilmenolone acts as a positive allosteric modulator of the GABA_A receptor [1].

E2730 is a selective and noncompetitive inhibitor of the gamma-aminobutyric acid (GABA) transporter 1 (GAT1) that exhibits oral availability as well as antiepileptic properties. Its inhibition of GAT1 is dependent on the prevailing GABA concentrations and specifically targets GAT1-mediated GABA uptake. Demonstrating in vivo effectiveness, E2730 has been tested at doses ranging from 5-50 mg/kg orally in various models, including the rat amygdala kindling and the mouse corneal kindling models, as well as in drug-resistant psychomotor epilepsy, fragile X syndrome at 2.5-300 mg/kg, and Dravet syndrome at dosages of 10 mg/kg and 20 mg/kg [1].

Arecaidine hydrobromide, a pyridine alkaloid, functions as a potent GABA uptake inhibitor and acts as a substrate for the H+-coupled amino acid transporter 1 (PAT1, SLC36A1), where it competitively inhibits L-proline uptake [1] [2].

Tiagabine hydrochloride (NO050328 hydrochloride) is the hydrochloride salt form of tiagabine, a nipecotic acid derivative with anticonvulsant property. A selective gamma-aminobutyric acid (GABA) reuptake inhibitor.