gabareceptor

Valproic Acid (2-Propylpentanoic Acid) is an HDAC inhibitor that inhibits HDAC1 activity, induces HDAC2 degradation, and is orally active. Valproic Acid can be used in epilepsy and bipolar disorder research.

Urethane (Ethylurethane) was an antineoplastic agent .Now is used for other medicinal purposes.

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

L-Cycloserine ((-)-Cycloserine) irreversibly inhibits GABA pyridoxal 5′-phosphate-dependent aminotransferase in E. coli, as well in the brains of various animals, results in increased levels of gamma-aminobutyric acid (GABA), which is an inhibitory neurotransmitter in vivo.

Tramiprosate (Alzhemed) is an orally active, blood-brain-barrier-crossing, naturally occurring amino acid found in a variety of red seaweeds that binds soluble Aβ and maintains it in a non-protofibrillar form.It is a GABA analog with neuroprotective, anticonvulsant, and antihypertensive activity.

Baicalin (Baicalein 7-O-β-D-glucuronide) is a prolyl endopeptidase inhibitor isolated from scutellaria baicalensis, with antioxidant, anti-tumor, anti-HIV properties.

Glabridin (KB-289522) may serve as an anti-inflammatory agent in diabetes-related vascular dysfunction, through regulating the synthesis and activity of iNOS under high-glucose levels; may possess a therapeutic effect on metabolic disorders( such as diabetes and hyperglycemia), by modulating glucose metabolism through AMPK in skeletal muscle cells. Glabridin may have potential as a chemopreventive agent against liver Y metastasis, by inhibiting the invasion of human HCC cells.

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.

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).

DL-Borneol ((endo)-Borneol) is a small molecule extracted from traditional Chinese medicine (TCM). It is an orally bioadjuvant that improves drug delivery to the brain and is commonly used as an adjuvant ingredient in TCM for the treatment of cardio-cerebral vascular diseases.

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.

(-)-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.

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

Pimpinellin is a natural product that acts as antagonist of proteins with GABA receptor activity.

6-Hydroxyflavanone, extracted from the leaves of Acorus calamus, exhibits anti-inflammatory and anti-neuropathic pain activity by targeting cyclooxygenase-2 (COX-2), 5-lipoxygenase (5-LOX), as well as opioid and GABA-A receptors. 6-Hydroxyflavanone has anti-injury sensory properties in a streptozotocin-induced diabetic neuropathy model. in a streptozotocin-induced diabetic neuropathy model with anti-injury sensory properties.

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

Sanggenon D (Sanggenone D), a small molecule compound from Morus alba Bark, is a GABA(A) receptor modulator with antioxidant and antibacterial activity, inhibits breast cancer cell proliferation, and inhibits the growth of Staphylococcus aureus by modulating the fatty acid biosynthesis system.

5-aminovalerate (or 5-aminopentanoic acid) is a lysine degradation product. It can be produced both endogenously or through bacterial catabolism of lysine. 5-aminovalerate is formed via the following multi-step reaction: L-lysine leads to cadverine leads

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

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

Guvacine hydrobromide, an alkaloid derived from the Areca catechu nut, serves as a potent inhibitor of GABA (GABA uptakp) uptake. It effectively inhibits rat GABA transporter isoforms GAT-1, GAT-2, and GAT-3, with respective IC50 values of 39 μM, 58 μM, and 378 μM [1].

Cannabidivarin (GWP42006) is a potent inhibitor against gamma 2 subunit of GABAA receptors. it may serve as a novel drug with definite control over childhood absence epilepsy.

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

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