GABA Receptor Activator

DL-Menthol (Racementhol) is an orally active, GABA_aR positive allosteric modulator and UDP-glucuronosyltransferase (UGT) inhibitor that can cross the blood-brain barrier. DL-Menthol binds to GABA_AR and exhibits an allosteric activation effect, enhancing GABA-mediated chloride influx and inhibiting neuronal excitability. DL-Menthol can induce surgical anesthesia in fish and inhibit the metabolic detoxification of tobacco carcinogens by human liver and intestinal UGT enzymes, resulting in reduced NNAL-N-Gluc production.

6'''-Feruloylspinosin is an orally active RORα activator that crosses the blood-brain barrier, with a K_d of 0.308 μM, and is found in natural sources. 6'''-Feruloylspinosin modulates AMPK and mTOR phosphorylation. 6'''-Feruloylspinosin promotes autophagy through the AMPK/mTOR signaling pathway, inhibits GSK3β phosphorylation at Tyr216, and activates the PGC-1α/Nrf2/HO-1 pathway. 6'''-Feruloylspinosin regulates neurotransmitter levels, enhances mRNA expression of GABA_A α1, α5, and GABA_B R1 receptor subunits, increases brain 5-HT and GABA, restores melatonin levels, and ameliorates anxiety-like behaviors. 6'''-Feruloylspinosin regulates oxidative stress homeostasis, inhibits mitochondrial dysfunction, decreases MDA while increasing GSH. 6'''-Feruloylspinosin can be used for research on Alzheimer's disease, acute myocardial infarction, heart failure with insomnia, and insomnia.

Methionine-d₄ is the deuterium labeled Methionine. Methionine (MRX-1024; D-Methionine) is an effective chemoprotective agent which can also inhibit the neuronal activity through GABAA receptor activation.

Dipropofol is a dimeric derivative of Propofol (HY-B0649) with antioxidant and antibacterial activities. Dipropofol terminates free radical chain reactions, scavenges DPPH free radicals and inhibits lipid peroxidation. Dipropofol protects cells from death induced by glutamate, Aβ(25-35) and buthionine sulfoximine, and increases the survival rate of mice exposed to oxygen. Dipropofol selectively activates tonic GABAA currents, hyperpolarizes resting membrane potential, reduces action potential firing, and alleviates the severity of seizures induced by Kainic acid. Dipropofol can be used in the research of Gram-positive bacterial infections, Alzheimer's disease, cerebral ischemia-related neuronal injury, oxygen toxicity and temporal lobe epilepsy.

α-Androstenol (5α-Androst-16-en-3α-ol) is a steroid pheromone that has been found in boar testes and male axillary sweat. α-Androstenol is also a positive allosteric modulator of GABAA receptors, which enhances GABA-activated currents in primary mouse cerebellar granule cells (EC₅₀ of 0.4 μM). α-Androstenol produces anxiolytic-like, antidepressant-like, and anticonvulsant effects in mice. α-Androstenol can be used for the research of seizures.

Propofol-d₁₈ is the deuterium labeled Propofol. Propofol potently and directly activates GABAA receptor and inhibits glutamate receptor mediated excitatory synaptic transmission.

Valerenic acid ((-)-Valerenic Acid), a sesquiterpenoid, is an orally active positive allosteric modulator of GABA_A receptors. Valerenic acid is also a partial agonist of the 5-HT_5a receptor. Valerenic acid mediates anxiolytic activity via GABA_A receptors containing the β3 subunit. Valerenic acid also exhibits potent antioxidant properties.

3-Methyl-GABA is a potent GABA aminotransferase activator. 3-Methyl-GABA can fit the binding pocket of GABA_A receptor (GABAaR). 3-Methyl-GABA can activate L-glutamic acid decarboxylase (GAD). 3-Methyl-GABA has anticonvulsant activity.

N-Arachidonoyl-GABA is one member of a new class of lipoamino acids related to anandamide identified in bovine brain. N-Arachidonoyl-GABA displays analgesic activity.

Etifoxine hydrochloride, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABA_A receptors. Etifoxine hydrochloride reveals anxiolytic and anticonvulsant properties in rodents.

Topiramate (Standard) is the analytical standard of Topiramate. This product is intended for research and analytical applications. Topiramate (McN 4853) is a broad-spectrum antiepileptic agent. Topiramate is a GluR5 receptor antagonist. Topiramate produces its antiepileptic effects through enhancement of GABAergic activity, inhibition of kainate/AMPA receptors, inhibition of voltage-sensitive sodium and calcium channels, increases in potassium conductance, and inhibition of carbonic anhydrase.

3-Carene is an orally active TCA cycle enzyme inhibitor. 3-Carene inhibits succinate dehydrogenase and malate dehydrogenase as well as pyruvate kinase, disrupting energy metabolism. 3-Carene disrupts cell wall and cell membrane integrity, leading to potassium ion leakage, protein leakage, membrane depolarization, ATP depletion, morphological disruption, and cell lysis. 3-Carene interferes with amino acid metabolism, pantothenate and CoA biosynthesis, purine and pyrimidine metabolism, and aminoacyl-tRNA biosynthesis. 3-Carene enhances GABA receptor-mediated synaptic responses. 3-Carene can be used in research on bacterial infections, inflammation, anxiety, and sleep disorders.

FGIN-1-43 is an effective and specific ligand for the mitochondrial diazepam binding inhibitor (DBI) receptor (related to the production of neurosteroids). FGIN 1-43 enhances the transmission of GABA by inducing the production of neurosteroids, which can be used for research on anti-anxiety.

COR659 is a potent and effective GABA_B positive allosteric modulator (PAM). COR659 suppresses alcohol and chocolate self-administration in rats.

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.

Topiramate D12 (McN 4853 D12) is a deuterium labeled Topiramate. Topiramate is a broad-spectrum antiepileptic agent. Topiramate is a GluR5 receptor antagonist. Topiramate produces its antiepileptic effects through enhancement of GABAergic activity, inhibition of kainate/AMPA receptors, inhibition of voltage-sensitive sodium and calcium channels, increases in potassium conductance, and inhibition of carbonic anhydrase.

Propofol-d₁₇ is the deuterium labeled Propofol. Propofol potently and directly activates GABAA receptor and inhibits glutamate receptor mediated excitatory synaptic transmission. Propofol has antinociceptive properties.

alpha-Asarone (Standard) is the analytical standard of alpha-Asarone. This product is intended for research and analytical applications. alpha-Asarone (α-Asarone) is one of the main psychoactive compounds, and possesses an antidepressant-like activity in mice.

Topiramate-13C6 (McN 4853-13C6) is the ¹³C labeled isotope of Topiramate (HY-B0122). Topiramate (McN 4853) is a broad-spectrum antiepileptic agent. Topiramate is a GluR5 receptor antagonist. Topiramate produces its antiepileptic effects through enhancement of GABAergic activity, inhibition of kainate/AMPA receptors, inhibition of voltage-sensitive sodium and calcium channels, increases in potassium conductance, and inhibition of carbonic anhydrase.

Topiramate (McN 4853) lithium is a broad-spectrum antiepileptic agent. Topiramate lithium is a GluR5 receptor antagonist. Topiramate produces its antiepileptic effects through enhancement of GABAergic activity, inhibition of kainate/AMPA receptors, inhibition of voltage-sensitive sodium and calcium channels, increases in potassium conductance, and inhibition of carbonic anhydrase.