GABA Receptor Activator

Anticonvulsant agent 9 (compound 4f) is an α1β2γ2 GABAA receptors activator. Anticonvulsant agent 9 activatesα1β2γ2 GABAA receptors with an EC₅₀ of 1.24 μM. Anticonvulsant agent 9 inhibits the inactivation of Nav1.2 channels. Anticonvulsant agent 9 exhibits significant anticonvulsant activities.

Dulozafone (F1933) shows anticonvulsant activity and can be used for epilepsy research.

Nav1.2-IN-4 is a blood-brain barrier-penetrant Na_V1.2 inhibitor (IC₅₀ = 31.21 μM). Nav1.2-IN-4 preferentially blocks the inactivated state of the neuronal voltage-gated sodium channel Na_V1.2, inhibiting persistent and resurgent sodium currents associated with epileptogenesis. Nav1.2-IN-4 restores the GABA-glutamate balance by enhancing GABA and reducing glutamate. Nav1.2-IN-4 reduces oxidative stress in brain tissue by increasing GSH and decreasing MDA. Nav1.2-IN-4 protects mice against MES-induced tonic hindlimb extensor seizures and attenuates hippocampal neuronal degeneration in the PTZ kindling model. Nav1.2-IN-4 can be used for research on epilepsy.

Kavain (Standard) is the analytical standard of Kavain. This product is intended for research and analytical applications. Kavain is a class of kavalactone isolated from Piper methysticum, which has anxiolytic properties in animals and humans. Kavain positively modulated γ-Aminobutyric acid type A (GABAA) receptor.

Flupirtine (Standard) (D 9998 (Standard)) is the analytical standard of Flupirtine (HY-17001A). This product is intended for research and analytical applications. Flupirtine is an orally active, blood-brain barrier-crossing non-opioid analgesic and neuroprotective agent. Flupirtine is a neuronal potassium channel opener (Kv7 activator), a NMDA receptor antagonist and a GABA receptor activator. Flupirtine stabilizes blood-brain-barrier integrity, reduces oxidative stress and brain leukocyte infiltration, enhances angioneurogenesis, suppresses calcium influx, stabilizes neuronal resting membrane potential, and counteracts focal cerebral ischemia. Flupirtine exhibits analgesic, muscle relaxant properties, protects neurons from excitotoxic, ischemic, or cytokine-mediated death. Flupirtine functions as a non-opioid analgesic without antipyretic or antiphlogistic properties, shows no relevant affinity to opiate receptor. Flupirtine can be used for the research of focal cerebral ischemia, pain, Alzheimer’s disease, or multiple sclerosis.

Propofol (Standard) is the analytical standard of Propofol. This product is intended for research and analytical applications. Propofol potently and directly activates GABA_A receptor and inhibits glutamate receptor mediated excitatory synaptic transmission. Propofol has antinociceptive properties and is used for sedation and hypnotic.

U-89843A (PNU-89843) is a GABAA receptors positive allosteric modulator (PAM). U-89843A enhances GABA-induced Cl^- currents in the α1β2γ2, α3β2γ2 and α6β2γ2 subtypes. U-89843A shows antioxidant and sedative effects.

Valerenic acid (Standard) is the analytical standard of Valerenic acid. This product is intended for research and analytical applications. 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.

IUN-00433 (Compound 36) is a selective positive allosteric modulator of α4β1δ-type GABA_A receptors, with an EC₅₀ of 0.060 μM. IUN-00433 is applicable to research related to neurological disorders.

Anticonvulsant agent 11 (Compound 8b) is an anticonvulsant agent. Anticonvulsant agent 11 exerts neuroprotective effects by enhancing cell viability and reducing ROS levels. Anticonvulsant agent 11 induces the expression of GABA_A α1, resulting in neuronal hyperpolarization. Anticonvulsant agent 11 increases the number of neurite-bearing cells and the length of neurites. Anticonvulsant agent 11 exhibits dose-dependent anticonvulsant effects in mice. Anticonvulsant agent 11 can be used for the research of epilepsy.

GeX-2 is a truncated analogue of αO-conotoxin. GeX-2 activates GABA_B receptor. GeX-2 inhibits α9α10 nAChR and Ca_V2.2 channels. GeX-2 alleviates pain in the rat model of chronic constriction injury.

U-89843A (PNU-89843) hydrochloride is a GABAA receptors positive allosteric modulator (PAM). U-89843A hydrochloride enhances GABA-induced Cl^- currents in the α1β2γ2, α3β2γ2 and α6β2γ2 subtypes. U-89843A hydrochloride shows antioxidant and sedative effects.

2-Ethyl-3-methylpyrazine is a GABA_A receptor potentiator, Antibacterial agent and Antifungal agent, with a K_p of 1.14 mM for GABA_A. 2-Ethyl-3-methylpyrazine forms via the Maillard reaction in sunflower seeds and also exists in the crust of wheat bread. 2-Ethyl-3-methylpyrazine regulates mood or states of consciousness via central GABA_A receptors. 2-Ethyl-3-methylpyrazine inhibits the growth of Ralstonia solanacearum and Magnaporthe oryzae. 2-Ethyl-3-methylpyrazine acts as an anxiolytic. 2-Ethyl-3-methylpyrazine is one of the sources of cocoa aroma, imparting nutty, corn-like, burnt, cereal, roasted and earthy flavors to foods. 2-Ethyl-3-methylpyrazine can be used in studies related to anxiety disorders and plant bacterial, fungal and oomycete infections.

Methionine (Standard) is the analytical standard of Methionine. This product is intended for research and analytical applications. Methionine (MRX-1024; D-Methionine) is an effective chemoprotective agent which can also inhibit the neuronal activity through GABAA receptor activation.

Flupirtine (D 9998) hydrochloride is an orally active, blood-brain barrier-crossing non-opioid analgesic and neuroprotective agent. Flupirtine hydrochloride is a neuronal potassium channel opener (Kv7 activator), a NMDA receptor antagonist and a GABA receptor activator. Flupirtine hydrochloride stabilizes blood-brain-barrier integrity, reduces oxidative stress and brain leukocyte infiltration, enhances angioneurogenesis, suppresses calcium influx, stabilizes neuronal resting membrane potential, and counteracts focal cerebral ischemia. Flupirtine hydrochloride exhibits analgesic, muscle relaxant properties, protects neurons from excitotoxic, ischemic, or cytokine-mediated death. Flupirtine hydrochloride functions as a non-opioid analgesic without antipyretic or antiphlogistic properties, shows no relevant affinity to opiate receptor. Flupirtine hydrochloride can be used for the research of focal cerebral ischemia, pain, Alzheimer’s disease, or multiple sclerosis.

Flupirtine-d₆ (D 9998-d₆) hydrochloride is the deuterium labeled Flupirtine hydrochloride (HY-W709349). Flupirtine hydrochloride is an orally active, blood-brain barrier-crossing non-opioid analgesic and neuroprotective agent. Flupirtine hydrochloride is a neuronal potassium channel opener (Kv7 activator), a NMDA receptor antagonist and a GABA receptor activator. Flupirtine hydrochloride stabilizes blood-brain-barrier integrity, reduces oxidative stress and brain leukocyte infiltration, enhances angioneurogenesis, suppresses calcium influx, stabilizes neuronal resting membrane potential, and counteracts focal cerebral ischemia. Flupirtine hydrochloride exhibits analgesic, muscle relaxant properties, protects neurons from excitotoxic, ischemic, or cytokine-mediated death. Flupirtine hydrochloride functions as a non-opioid analgesic without antipyretic or antiphlogistic properties, shows no relevant affinity to opiate receptor. Flupirtine hydrochloride can be used for the research of focal cerebral ischemia, pain, Alzheimer’s disease, or multiple sclerosis.

Pregabalin arenacarbil is a proagent of Pregabalin.Pregabalin is an analog of gamma-aminobutyric acid (GABA) for the research of post herpetic neuralgia, peripheral diabetic neuropathy,fibromyalgia and epilepsy.

Topiramate D12 (Standard) is the analytical standard of Topiramate D12. This product is intended for research and analytical applications. 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.

Flupirtine-d₄ (D 9998-d₄) hydrochloride is the deuterium labeled Flupirtine hydrochloride (HY-W709349). Flupirtine hydrochloride is an orally active, blood-brain barrier-crossing non-opioid analgesic and neuroprotective agent. Flupirtine hydrochloride is a neuronal potassium channel opener (Kv7 activator), a NMDA receptor antagonist and a GABA receptor activator. Flupirtine hydrochloride stabilizes blood-brain-barrier integrity, reduces oxidative stress and brain leukocyte infiltration, enhances angioneurogenesis, suppresses calcium influx, stabilizes neuronal resting membrane potential, and counteracts focal cerebral ischemia. Flupirtine hydrochloride exhibits analgesic, muscle relaxant properties, protects neurons from excitotoxic, ischemic, or cytokine-mediated death. Flupirtine hydrochloride functions as a non-opioid analgesic without antipyretic or antiphlogistic properties, shows no relevant affinity to opiate receptor. Flupirtine hydrochloride can be used for the research of focal cerebral ischemia, pain, Alzheimer’s disease, or multiple sclerosis.

Emamectin B1a (L-656,748) is a semisynthetic derivative of avermectin B1a that binds to GABA receptors (Ki=17.6 nM in rat brain membranes) and enhances GABA responses. Emamectin B1a acitivates GABAA receptors α1β1γ2, α1β2γ2, and α1β3γ2 with IC₅₀s of 57, 210, and 49.8 nM, respectively. Emamectin B1a also binds to glycine receptors, inhibiting glycine receptors with an IC₅₀=218 nM in rat spinal cord. Emamectin B1a (1.067 ng/mL) caused 90% mortality of S. exigua larvae in foliar spray bioassays and topical application, making it more toxic than avermectin B1.