gabar

Primidone (NCI-C56360) is a potent anticonvulsant agent. It is a neuronal voltage-gated sodium channel blocker and has value in the study of epilepsy, essential tremor, and psychiatric disorders.

Urethane (Ethyl carbamate; Ethylurethane) is a byproduct formed during the fermentation process of various foods. As an ethyl ester of carbamic acid, it has the ability to inhibit the growth of bacteria, sea urchin eggs, protozoa, and plant tissues, and is commonly used for establishing lung cancer models.

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.

Gabapentin (Neurontin) is an Anti-epileptic Agent. The physiologic effect of gabapentin is by means of Decreased Central Nervous System Disorganized Electrical Activity.

Halothane (Anestan) is a nonflammable, halogenated, hydrocarbon anesthetic that provides relatively rapid induction with little or no excitement. Analgesia may not be adequate. NITROUS OXIDE is often given concomitantly. Because halothane may not produce sufficient muscle relaxation, supplemental neuromuscular blocking agents may be required.

Baclofen (Lioresal) is a synthetic chlorophenyl-butanoic acid derivative used to treat spasms due to spinal cord damage and multiple sclerosis, muscle-relaxing Baclofen acts as a gamma-aminobutyric acid (GABA) agonist specific for GABA-B receptors. It acts at spinal and supraspinal sites, reducing excitatory transmission.

Flumazenil (Ro 15-1788) antagonizes the benzodiazepine binding site of the gamma-aminobutyric acid (GABA)/benzodiazepine receptor complex in the central nervous system (CNS), thereby preventing the chloride channel opening events and inhibiting neuronal hyperpolarization. As a result, flumazenil reverses benzodiazepine-induced effects including sedation, psychomotor deficits, amnesia, and hypoventilation in a dose-dependent manner. Flumazenil is an imidazobenzodiazepine derivative, effective in reversing benzodiazepine-induced activities.

Bemegride (3-Ethyl-3-methylglutarimide), a central nervous system stimulant, serves as an antidote for barbiturate poisoning.

Pentylenetetrazol is a GABA(A) receptor antagonist, that displays activity as a central nervous system and respiratory stimulant.

Valproic acid sodium salt (Sodium Valproate) is the sodium salt form of valproic acid with anti-epileptic activity. Valproic acid sodium salt is converted into its active form, valproate ion, in blood. Although the mechanism of action remains to be elucidated, Valproic acid sodium salt increases concentrations of gamma-aminobutyric acid (GABA) in the brain, probably due to inhibition of the enzymes responsible for the catabolism of GABA. This potentiates the synaptic actions of GABA. Valproic acid sodium salt may also affect potassium channels, thereby creating a direct membrane-stabilizing effect.

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

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.

Phenibut (Aminophenylbutyric acid) is a central depressant and derivative of the naturally occurring inhibitory neurotransmitter γ-aminobutyric acid (GABA).

Dihydromyricetin (Ampelopsin) is a natural antioxidant flavonoid from Ampelopsis grossedentata. Dihydromyricetin is a potent inhibitor of dihydropyrimidinase with an IC50 of 48 μM. Dihydromyricetin can activate autophagy by inhibiting mTOR signaling.

Gabapentin hydrochloride (Neurontin HCl) is a GABA analogue, used to treat seizures and neuropathic pain.

Oxiracetam (ISF2522), a cyclic derivative of gamma-aminobutyric acid (GABA), is utilized for the treatment of cognitive impairments.

Acamprosate calcium (Campral EC) is a GABA receptor agonist and modulator of glutamatergic systems, used for treating alcohol dependence.

Bicuculline is an alkaloid extracted from Corydalis decumbens, acting as a competitive antagonist of the neurotransmitter GABAA receptor (IC50 = 2 μM). It also blocks Ca2+-activated potassium (SK) channels and inhibits slow afterhyperpolarization (slow AHP). Bicuculline has anticonvulsant effects and is commonly used to establish mouse seizure models.

(R)-baclofen (STX209), a derivative of gamma-aminobutyric acid, is commonly utilized for the treatment of spasticity.

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

Afizagabar (S44819) is a first-in-class, competitive, and selective antagonist at the GABA-binding site of the α5-GABAAR, with an IC50 of 585 nM for α5β2γ2 and a Ki of 66 nM for α5β3γ2. It enhances hippocampal synaptic plasticity and exhibits pro-cognitive efficacy [1].

Broflanilide is metabolized to desmethyl-broflanilide, which is a potent antagonist at the insect resistant-to-dieldrin GABA receptor and inhibits S. litura RDL GABAR (IC50: 1.3 nM).

Losigamone (AO-33), an agonist of the GABA receptor, can be utilized in studies on the treatment of partial seizures.

Nikethamide is a stimulant which mainly influences the respiratory cycle. Widely known by its former sales name of Coramine, it was used in the mid-twentieth century as a medical countermeasure against tranquilizer overtreatments, before the advent of end