GABA Receptor Agonist

Bifenazate is a carbazate acaricide that control 100% of mites at a concentration of 25 ppm. Bifenazate is a positive allosteric modulator of GABA receptor. Bifenazate is the inhibitor for the mitochondrial electron transport chain complex III.

3α,21-Dihydroxy-5α-pregnan-20-one (THDOC), an endogenous neurosteroid, is a positive modulator of GABA_A receptors. 3α,21-Dihydroxy-5α-pregnan-20-one potentiates neuronal response to low concentrations of GABA at α4β1δ GABA_A receptors in vitro.

Phenibut (β-Phenyl-GABA) hydrochloride is an orally active GABA-B agonist. Phenibut hydrochloride acts as a GABA-mimetic, primarily at GABAB?receptors. Phenibut hydrochloride has anxiolytic and nootropic (cognition enhancing) effects.

(2S)-6-Prenylnaringenin is the most efficient compound in forebrain. (2S)-6-Prenylnaringenin acts as a GABA_A positive allosteric modulator at α+β- binding interface.

Isonipecotic acid is a GABAA receptor partial agonist.

γ-Aminobutyric acid-¹³C₄ is the ¹³C-labeled γ-Aminobutyric acid. γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain, binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors).

3,4,5-Trimethoxycinnamic acid is a phenylpropanoid isolated from the roots of Polygala tenuifolia WILLD, with anti-stress effect, prolonging the sleeping time in animals. 3,4,5-Trimethoxycinnamic acid increases expression of GAD65 and γ-subunit of GABAA receptor, but shows no effect on the amounts of α-, β-subunits.

Lesogaberan (AZD-3355) hydrochloride is a potent and selective GABA_B receptor agonist with an EC₅₀ of 8.6 nM for human recombinant GABA_B receptor. The affinity (K_is) of Lesogaberan hydrochloride for rat GABA_B and GABA_A receptors, as measured by displacement of [³H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan hydrochloride inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action.

Alogabat is a positive allosteric modulator (PAM) and agonist (K_i <100 nM) of the GABAA α5 receptor, targeting the α5β3γ2 subunit with a Ki of 8.7 nM. Alogabat increases the expression level of α5β3γ2 in oocytes (1.97-fold). GABAA has been implicated in cognitive impairment associated with central nervous system (CNS) disorders, brain cancer (including brain tumors such as medulloblastoma), and can be used in the study of mild cognitive impairment (MCI), amnestic MCI (aMCI), age-associated memory impairment (AAMI), age-related cognitive decline (ARCD), dementia, Alzheimer's disease (AD), prodromal AD, post-traumatic stress disorder (PTSD), schizophrenia, bipolar disorder, amyotrophic lateral sclerosis (ALS), cognitive impairment associated with cancer treatment, mental retardation, Parkinson's disease (PD), autism spectrum disorder, fragile X, Rett syndrome, obsessive-compulsive behavior, and substance addiction.

Tetrahydrodeoxycorticosterone, an neurosteroid, is a potent positive allosteric modulator (PAM) of GABA_A receptor. Tetrahydrodeoxycorticosterone has potent neuroinhibitory properties.

MK0343 (MRK-409) is an orally bioavailable GABA_A receptor subtype-selective partial agonist. MK0343 is a non-sedating anxiolytic.

TACA (trans-4-Aminocrotonic acid) is a potent agonist of GABA_A and GABA_C receptors (K_D= 0.6 μM). TACA also is GABA uptake inhibitor and substrate for GABA-T. TACA produces late biphasic responses in the MPG neurons.

FGIN 1-27, an indoleacetamide, is a specific peripheral benzodiazepine receptor (PBR) ligand with a K_i of 5.0 nM. FGIN 1-27 can penetrate the blood brain barrier (BBB). FGIN 1-27 inhibits the onset of Isoniazid-induced convulsions.

GS39783 is a positive allosteric modulator (PAM) of GABA_BR. Positive modulation of the GABA_BR can be used for the research of Nicotine addiction.

Phenibut (β-Phenyl-GABA) is a GABA-B agonist. Phenibut acts as a GABA-mimetic, primarily at GABAB receptors. Phenibut has anxiolytic and nootropic (cognition enhancing) effects.

(E)-3,4,5-Trimethoxycinnamic acid (TMCA) is a cinnamic acid substituted by multi-methoxy groups. (E)-3,4,5-Trimethoxycinnamic acid is an orally active and potent GABA_A/BZ receptor agonist. (E)-3,4,5-Trimethoxycinnamic exhibits favourable binding affinity to 5-HT_2C and 5-HT_1A receptor, with IC₅₀ values of 2.5 and 7.6 μM, respectively. (E)-3,4,5-Trimethoxycinnamic acid shows anticonvulsant and sedative activity. (E)-3,4,5-Trimethoxycinnamic acid can be used for the research of insomnia, headache and epilepsy.

Progabide is a gamma-aminobutyric acid receptor (GABA) agonist.

6-Aminonicotinic acid is an analog of Niacin (HY-B0143) and also a GABA_A receptor agonist with a K_i value of 4.4 μM in rats. 6-Aminonicotinic acid binds to both native and recombinant GABA_A receptors, is metabolized into non-functional pyridine nucleotide analogs to inhibit dehydrogenases, and suppresses the proliferation of T2 bacteriophages. 6-Aminonicotinic acid accumulates in specific bacterial cells in the form of pyridine nucleotide analog metabolites. 6-Aminonicotinic acid can be used in research related to neurological disorders such as anxiety, epilepsy and schizophrenia, and also serves as an intermediate in organic synthesis.

Bretazenil (Ro 16-6028) is a partial agonist at the gamma-aminobutyric acid A (GABA_A) receptor-linked benzodiazepine site. Bretazenil is potent benzodiazepine examined, exhibiting an IC₅₀ (concentration at which half-maximal inhibition of specific [35S]TBPS binding occurs) of 6.1 nM. Bretazenil shows an EC₅₀ of 10 nM for recombinant α1β1γ2. Anticonvulsant effects.

3-Aminopropylphosphonic acid ((3-Aminopropyl)phosphonic acid) is a phosphonic acid analogue of GABA and a GABA_B receptor agonist.