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.

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.

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.

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.

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.

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.

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].

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

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

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

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

Arecaidine hydrobromide is the salt form of Arecaidine, a pyridine alkaloid with potent GABA uptake inhibitory properties that acts as a substrate for H+-coupled amino acid transporter protein 1 (PAT1, SLC36A1) to competitively inhibit the uptake of L-proline.

Cicutoxin is a convulsant compound. It inhibits Na+ and K+ channels and suppresses the γ-aminobutyric acid pathway. As a potent GABA antagonist, Cicutoxin induces recurrent seizures and exhibits cholinergic activity. Its primary targets are the brain and skeletal muscles. Cicutoxin can be isolated from [Cicuta maculata] and [Cicuta douglasii].

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.

(-)-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.

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.

Penicillin G sodium(Benzylpenicillin sodium) salt is a penicillin derivative commonly used in the form of its sodium or potassium salts in the treatment of a variety of infections. It is effective against most gram-positive bacteria and against gram-negative cocci. It has also been used as an experimental convulsant because of its actions on GAMMA-AMINOBUTYRIC ACID mediated synaptic transmission.

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.

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.

β-Alanine (3-Aminopropanoic acid) is a naturally occurring beta amino acid formed in vivo by the degradation of dihydrouracil and carnosine. It acts as a neurotransmitter by activating glycine and GABA receptors.

(+)-BORNEOL (d-Borneol) is a natural bicyclic monoterpene used for analgesia and anesthesia in traditional Chinese medicine; enhances GABA receptor activity with an EC50 of 248 μM.

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.

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.