gabaa receptor

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

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

Dopamine hydrochloride (ASL279), a naturally occurring catecholamine formed by decarboxylation of dihydroxyphenylalanine and a precursor of norepinephrine and epinephrine, binds to alpha-1- and beta-1- adrenergic receptors.

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.

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.

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. 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.

(-)-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.

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

Rosmanol has antioxidant activity, it can activate the antioxidant response element. Rosmanol has biphasic modulation of GABAA receptors, demonstrates CNS activity in mouse models of antinociception, antidepressant and anxiolysis. Rosmanol potently induce

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.

Picrotoxinin is a blocker of chloride channel and a noncompetitive antagonist of GABAA with an IC50 of 1.15 μM for α1β2γ2L GABAA. Picrotoxinin shows convulsant properties.

Tetrahydrocortisol (Tetrahydrohydrocortisone) is a metabolite of neurosteroids and cortisol, a GABAA receptor antagonist, and also capable of lowering intraocular pressure.

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.

Wogonoside (Wogonin 7-O-glucuronide) acts as a positive allosteric modulator of the benzodiazepine site of the GABAA receptor.

Tetrahydrodeoxycorticosterone(Tetrahydro-11-deoxycorticosterone) is a potent GABAA receptor orthosteric modulator (PAM) with neuroprotective activity that selectively inhibits neurosteroid-mediated enhancement of GABA-induced currents at the GABAA receptor, and can be used in the study of neurological disorders.

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.

Muscimol hydrochloride is the salt form of Muscimol, the main psychoactive component of Amanita muscaria, a potent and selective GABAA receptor agonist and partial GABAC receptor agonist, with no activity on GABAB receptors. It is commonly used in central neuroscience research, with analgesic, anxiolytic and neuroprotective effects, with the advantage of being able to cross the blood-brain barrier and can be taken orally.

Withasomniferolide B, a withanolide, can be obtained through isolation from a methanol extract of Withania somnifera roots, which acts as a positive activator of the GABA(A) receptor [1].

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

Withasomniferolide A, a withanolide extracted from the roots of Withania somnifera, has been identified as a positive activator of the GABAA receptor, isolated using a methanol extract [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.