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GABAAreceptor agent 6 (compound 2027) is a potent γ-GABAAR antagonist with an Ki of 0.56 µM. GABAAreceptor agent 6 shows γ-GABAAR antagonist activity with low cellular membrane permeability .
GABAAreceptor agonist 2 (compound 4c) is a potent GABAAreceptor agonist. GABAAreceptor agonist 2 shows anti-depression activities in classical mouse models of depression of FST and TST. GABAAreceptor agonist 2 binds at the GABA binding site of GABAAreceptor in order to produce GABAergic effects. GABAAreceptor agonist 2 has the potential for the research of depression .
GABAAreceptor agonist 1 (compound 3e) is a potent GABAAreceptor agonist. GABAAreceptor agonist 1 shows anti-depression activities in classical mouse models of depression of FST and TST. GABAAreceptor agonist 1 binds at the GABA binding site of GABAAreceptor in order to produce GABAergic effects. GABAAreceptor agonist 1 has the potential for the research of depression .
GABAAreceptor agent 8 (compoud 5e) is a potent GABAAreceptor positive modulator. GABAAreceptor agent 8 shows anticonvulsant activity in vitro and in vivo with low neurotoxicity. GABAAreceptor agent 8 has the potential for the research of epilepsy .
GABAAreceptor agent 7 (compoud 5c) is a potent GABAAreceptor positive modulator. GABAAreceptor agent 7 shows anticonvulsant activity in vitro and in vivo with low neurotoxicity. GABAAreceptor agent 7 has the potential for the research of epilepsy .
GABAAreceptor agent 4 (compound 1e) is a potent γ-GABAAR antagonist with an Ki of 0.18 µM. GABAAreceptor agent 4 efficiently rescues inhibition of T cell proliferation. GABAAreceptor agent 4 has the immunomodulatory potential .
GABAAreceptor agent 2 TFA is a potent and high-affinity GABAAreceptor antagonist with an IC50 of 24 nM (human α1β2γ2 GABAA-expressing tsA201 cells) and a Ki of 28 nM (rat GABAAreceptors). GABAAreceptor agent 2 TFA is inactive against four human GABA transporters (hGAT-1, hBGT-1, hGAT-2, and hGAT-3) .
GABAAreceptor agent 5 (compound 018) is a potent γ-GABAAR antagonist with an Ki of 0.020 µM. GABAAreceptor agent 5 shows γ-GABAAR antagonist activity with low cellular membrane permeability .
GABAAreceptor modulator-2 (Compound 20) is selective, orally active α5-GABAAR negative allosteric modulator (NAM) with a Ki of 4.1 nM. GABAAreceptor modulator-2 shows high-metabolic stability and good CNS safety .
SB-205384 is a GABAAreceptor modulator. The primary effect of SB-205384 on GABAA-activated currents is a prolonged response decay half-life upon removal of the agonist .
3-Hydroxyphenazepam is an active metabolite of Cinazepam. Cinazepam is a GABAAreceptor agonist. 3-Hydroxyphenazepam can inhibit synaptosomal transporter-mediated [ 3H]GABA uptake .
Withasomniferolide B is a withanolide. Withasomniferolide B can be isolated from a GABAAreceptor positive activator methanol extract of the roots of Withania somnifera .
Basmisanil (RG1662) is a highly selective orally active α subunit-containing GABAAreceptors (GABAAα5) negative allosteric modulator (NAMs). Basmisanil can inhibit GABAA-α5 with a Ki value of 5 nM and IC50 value of 8 nM, respectively. Basmisanil can be used for the research of multiple cognitive and psychiatric disorders .
Picrotin is an active compound, also is one of the composition of picrotoxin (an antagonist of GABAAreceptors (GABAARs) and glycine receptors (GlyRs)). Picrotin has sensitivity for GlyRs/b> with IC50 values range from 5.2 μM to 106 μM. Picrotin can be used for the research of neurotransmission .
DMCM hydrochloride is a nonselective full inverse agonist of benzodiazepine. DMCM shows bnding afinity at human recombinant GABAA αxβ3γ2 receptor subtypes with Kis of 10 nM, 13 nM, 7.5 nM, 2.2 nM for α1, α2, α3, and α5 receptors, respectively .
Songorine is a diterpenoid alkaloid isolated from the genus Aconitum. Songorine is a GABAAreceptor antagonist in rat brain and has anti cancer, antiarrhythmic and anti-inflammatory activities. Songorine has the potential for the treatment of Epithelial ovarian cancer (EOC) .
Panadiplon (FG 10571; PNU 78875), a benzodiazepine receptor, is a 5GABAA partial agonist. Panadiplon exhibits selectivity for 5GABAAreceptors versus 1GABAAreceptors .
Picrotoxinin, a potent convulsant, is a chloride channel blocker. Picrotoxinin is a noncompetitive GABAAreceptor antagonist, which negatively modulates the action of GABA on GABAAreceptors. Picrotoxinin inhibits α1β2γ2LGABAAreceptor with an IC50 of 1.15 μM .
U93631 is a GABAAreceptor ligand of novel chemical structure with IC50 of 100 nM,and has been shown to induce a rapid, time-dependent decay of GABA-induced whole-cell Cl-currents in recombinant GABAAreceptors.
SL651498 is a full agonist of α2 and α3 GABAAreceptors, and a partial agonist of α1 and α5 GABAAreceptors. SL651498 shows anxiolytic and anticonvulsant activities .
NS11394 is an orally active and unique subtype-selective GABAA positive allosteric receptor (PAM), with a Ki of ~0.5 nM. NS11394 shows a selectivity profile in the order of GABAA-5 > α3 > α2 > α1-containing receptors. NS11394 has anxiolytic and anti-inflammatory properties .
HZ166 is a GABAAreceptor subtype-selective benzodiazepine site agonist with preferential activity at α2- and α3-GABAAreceptors. HZ166 shows anti-hyperalgesic effects . HZ166 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
MmTx2 toxin is a GABAAreceptor modulator that enhances GABAAreceptor sensitivity to agonists. MmTx2 toxin can be obtained from venom of coral snake. MmTx2 toxin can be used in the study of neurological diseases such as epilepsy, schizophrenia and chronic pain .
MRK-898 is an orally active GABA(A) receptor modulator. MRK-898 binds to α1, α2, α3 or α5 subunit of GABA(A) receptor with Ki values of 1.2 nM, 1.0 nM, 0.73 nM, and 0.50 nM, respectively. However, α1-containing GABA(A) receptors are identified as the "sedative" and α2- and/or α3-containing receptors as the "anxiolytic" subtype(s) .
MRK-016 is a selective, orally bioavailable inverse agonist of GABAA α5 receptor, with an EC50 of 3 nM for GABAA α5, and Kis of 0.83, 0.85, 0.77 and 1.4 nM for human GABAA α1β3γ2, GABAA α2β3γ2, GABAA α3β3γ2, and GABAA α5β3γ2, respectively; MRK-016 also readily penetrates the CNS.
Valerenic acid ((-)-Valerenic Acid), a sesquiterpenoid, is an orally active positive allosteric modulator of GABAAreceptors. Valerenic acid is also a partial agonist of the 5-HT5areceptor. Valerenic acid mediates anxiolytic activity via GABAAreceptors containing the β3 subunit. Valerenic acid also exhibits potent antioxidant properties .
Lotilaner is a parasiticide, acts as a potent non-competitive antagonist of insects GABACl receptors, with an IC50 of 23.84 nM for Drosophila melanogasterGABAreceptor. No effect on a dog GABAAreceptor .
Etbicyphat (Trimethylopropane phosphate) is a potent GABA(A) receptors competitive antagonist. Etbicyphat induces epileptiform activities in hippocampal CA1 neurons, and binds to the GABA(A)-benzodiazepine receptors .
Propofol potently and directly activates GABAAreceptor and inhibits glutamate receptor mediated excitatory synaptic transmission. Propofol has antinociceptive properties and is used for sedation and hypnotic .
Bis(7)-tacrine dihydrochloride is a dimeric AChE inhibitor derived from tacrine. Bis(7)-tacrine dihydrochloride prevents glutamate-induced neuronal apoptosis by blocking NMDA receptors. Bis(7)-tacrine dihydrochloride is a potent GABAAreceptor antagonist. Bis(7)-tacrine dihydrochloride has the potential for the research of Alzheimer's disease .
Propofol-d18 is the deuterium labeled Propofol. Propofol potently and directly activates GABAAreceptor and inhibits glutamate receptor mediated excitatory synaptic transmission[1].
Valnoctamide (Valmethamide), a derivative of valproate, suppresses benzodiazepine-refractory status epilepticus. Valnoctamide (Valmethamide) acts directly on GABAAreceptors .
Tetrahydrodeoxycorticosterone, an neurosteroid, is a potent positive allosteric modulator (PAM) of GABAAreceptor. Tetrahydrodeoxycorticosterone has potent neuroinhibitory properties .
Cholesterol myristate is a natural steroid present in traditional Chinese medicine. Cholesterol myristate binds to several ion channels such as the nicotinic acetylcholine receptor, GABAAreceptor, and the inward-rectifier potassium ion channel.
Dihydroergotoxine mesylate is a complex of closely related alkaloid salts; Binds with high affinity to the GABAAreceptor Cl- channel, producing an allosteric interaction with the benzodiazepine site.
Valnoctamide-d5 is the deuterium labeled Valnoctamide. Valnoctamide (Valmethamide), a derivative of valproate, suppresses benzodiazepine-refractory status epilepticus. Valnoctamide (Valmethamide) acts directly on GABAAreceptors[1][2].
Loreclezole, an antiepileptic compound, is a selective GABAAreceptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit containing receptors .
Loreclezole hydrochloride, an antiepileptic compound, is a selective GABAAreceptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit containing receptors .
Methionine (MRX-1024; D-Methionine) is an effective chemoprotective agent which can also inhibit the neuronal activity through GABAAreceptor activation.
Propofol-d17 is the deuterium labeled Propofol. Propofol potently and directly activates GABAAreceptor and inhibits glutamate receptor mediated excitatory synaptic transmission. Propofol has antinociceptive properties[1].
3α,21-Dihydroxy-5α-pregnan-20-one (THDOC), an endogenous neurosteroid, is a positive modulator of GABAAreceptors. 3α,21-Dihydroxy-5α-pregnan-20-one potentiates neuronal response to low concentrations of GABA at α4β1δ GABAAreceptors in vitro.
Etbicyphat- 13C3 is the 13C labeled Etbicyphat (HY-139145). Etbicyphat is a potent GABA(A) receptors competitive antagonist. Etbicyphat induces epileptiform activities in hippocampal CA1 neurons, and binds to the GABA(A)-benzodiazepine receptors[1][2].
Lorediplon is a novel non-benzodiazepine drug acting as a GABAAreceptor modulator, differentially active at the alpha1-subunit, associated with promoting sleep.
Adipiplon (NG2-73) is a selective GABAAreceptor positive allosteric modulator. Adipiplon is particularly useful in the research of a variety of central nervous system (CNS) disorders.
ZAPA sulfate is an agonist at low affinity GABAA-receptors. ZAPA sulfate induces membrane hyperpolarization of the Ascaris muscle cell with an EC50 of 10.3 μM .
γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain, binding to the ionotropic GABAreceptors(GABAAreceptors) and metabotropic receptors (GABABreceptors. γ-Aminobutyric acid shows calming effect by blocking specific signals of central nervous system .
TCS1105 is a benzodiazepine ligand with agonist for α2-subunit containing GABAAreceptors and antagonist for α1-subunit containing GABAAreceptors. TCS1105 reduces anxiety-like behavior in mice. TCS1105 enhances offensive behavior and social dominance. TCS1105 blocks Sema3A induced AGC (axonal growth cones) collapse in a concentration-dependent fashion .
γ-Aminobutyric acid-d2 is the deuterium labeled γ-Aminobutyric acid. γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain[1][2], binding to the ionotropic GABAreceptors (GABAAreceptors) and metabotropic receptors (GABAB receptors)[2].
γ-Aminobutyric acid-d6 is the deuterium labeled γ-Aminobutyric acid. γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain[1][2], binding to the ionotropic GABAreceptors (GABAAreceptors) and metabotropic receptors (GABAB receptors)[2].
Thiocolchicoside is a competitive γ-aminobutyric acid type A (GABAA)receptor antagonist and glycine receptor agonist in the central nervous system. Thiocolchicoside is a semisynthetic sulfur derivative of colchicoside. Thiocolchicoside is a muscle relaxant and has anti-inflammatory, and analgesic properties .
THIP (Gaboxadol) is a selective extrasynaptic GABAAreceptors (eGABARs) agonist (with blood-brain barrier permeability), shows an EC50 value of 13 µM for δ-GABAAR. THIP induces strong tense GABAA-mediated currents in layer 2/3 neurons, but shows on effect on miniature IPSCs. THIP can be used in studies of sleep disorders .
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[1][2], binding to the ionotropic GABAreceptors (GABAAreceptors) and metabotropic receptors (GABAB receptors)[2].
p-Hydroxybenzaldehyde is a one of the major components in vanilla aroma, with antagonistic effect on GABAAreceptor of the α1β2γ2S subtype at high concentrations.
(-)-α-Pinene is a monoterpene and shows sleep enhancing property through a direct binding to GABAA-benzodiazepine (BZD) receptors by acting as a partial modulator at the BZD binding site .
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 .
Propofol (Standard) is the analytical standard of Propofol. This product is intended for research and analytical applications. Propofol potently and directly activates GABAAreceptor and inhibits glutamate receptor mediated excitatory synaptic transmission. Propofol has antinociceptive properties and is used for sedation and hypnotic .
γ-Aminobutyric acid-4,4-d2 is the deuterium labeled γ-Aminobutyric acid. γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain[1][2], binding to the ionotropic GABAreceptors (GABAAreceptors) and metabotropic receptors (GABAB receptors)[2].
Propanidid (Sombrevin; Fabantol) is a γ-aminobutyric acid type A (GABAA)receptor agonist and a short-acting non-barbiturate general anesthetic agent. Propanidid can decrease the arterial pressure .
6-(4-Methoxyphenyl)pyridazin-3-amine is an aminopyridazine derivative, and can be used for the synthesis of SR 95103. SR 95103 is a selective and competitive GABA-Areceptor antagonist .
(-)-Bicuculline methobromide (l-Bicuculline methobromide) is a potent GABAAreceptor antagonist. (-)-Bicuculline methobromide blocks afterhyperpolarizations (AHPs) mediated by Ca 2+-activated K + channels in various types of neurons .
(-)-Bicuculline methochloride (l-Bicuculline methochloride) is a potent GABAAreceptor antagonist. (-)-Bicuculline methochloride blocks afterhyperpolarizations (AHPs) mediated by Ca 2+-activated K + channels in various types of neurons .
SJM-3 is a positive allosteric modulator of different isoforms of the GABAAreceptor. SJM-3 binds at the high-affinity benzodiazepine binding site at the α+/γ- subunit interface .
Tetrahydrodeoxycorticosterone-d3 is the deuterium labeled Tetrahydrodeoxycorticosterone. Tetrahydrodeoxycorticosterone, an neurosteroid, is a potent positive allosteric modulator (PAM) of GABAAreceptor. Tetrahydrodeoxycorticosterone has potent neuroinhibitory properties[1][2][3].
FG 7142 (ZK 39106; LSU-65), a non-selectively benzodiazepine inverse agonist, has high affinity for the α1 subunit-containing GABAAreceptor (Ki=91 nM). FG 7142 (ZK 39106; LSU-65) also modulates GABA-induced chloride flux at GABAAreceptors expressing the α1 subunit (EC50= 137 nM). FG 7142 (ZK 39106; LSU-65) can increase tyrosine hydroxylation and cause upregulation of β-adrenoceptors in mouse cerebral cortex .
Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity . Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the GABAAreceptor than its enantiomer form .
Methionine-d3 is the deuterium labeled Methionine. Methionine (MRX-1024; D-Methionine) is an effective chemoprotective agent which can also inhibit the neuronal activity through GABAAreceptor activation.
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 GABAAreceptor activation.
TPMPA, a hybrid of isoguvacine and 3-APMPA, is the first selective antagonist for a GABACreceptor (KB = 2.1 μM), but not to interact with GABAA (KB = 320 μM) or GABABreceptors (EC50 = 500 μM). TPMPA has the potential for the research of suppressing orientation selectivity in ganglion cells .
5-Methoxyflavone, belonged to Flavonoid family, is a DNA polymerase-beta inhibitor and neuroprotective agent against beta-amyloid toxicity. possess central nervous system (CNS) depressant effect mediated through the ionotropic GABAAreceptors.
γ-Aminobutyric acid (Standard) is the analytical standard of γ-Aminobutyric acid. This product is intended for research and analytical applications. γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain, binding to the ionotropic GABAreceptors(GABAAreceptors) and metabotropic receptors (GABABreceptors. γ-Aminobutyric acid shows calming effect by blocking specific signals of central nervous system .
TACA (trans-4-Aminocrotonic acid) is a potent agonist of GABAA and GABACreceptors (KD= 0.6 μM). TACA also is GABA uptake inhibitor and substrate for GABA-T. TACA produces late biphasic responses in the MPG neurons .
Lesogaberan (AZD-3355) is a potent and selective GABABreceptor agonist with an EC50 of 8.6 nM for human recombinant GABABreceptors. The affinity (Kis) of Lesogaberan for rat GABAB and GABAAreceptors, as measured by displacement of [ 3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action .
Lesogaberan (AZD-3355) hydrochloride is a potent and selective GABABreceptor agonist with an EC50 of 8.6 nM for human recombinant GABABreceptor. The affinity (Kis) of Lesogaberan hydrochloride for rat GABAB and GABAAreceptors, 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 .
p-Hydroxybenzaldehyde-d4 is the deuterium labeled p-Hydroxybenzaldehyde. p-Hydroxybenzaldehyde is a one of the major components in Dendrocalamus asper bamboo shoots, with antagonistic effect on GABAAreceptor of the α1β2γ2S subtype at high concentrations.
p-Hydroxybenzaldehyde- 13C is the 13C-labeled p-Hydroxybenzaldehyde. p-Hydroxybenzaldehyde is a one of the major components in Dendrocalamus asper bamboo shoots, with antagonistic effect on GABAAreceptor of the α1β2γ2S subtype at high concentrations.
Pivagabine (CXB 722) is a hydrophobic 4-aminobutyric acid derivative with neuromodulatory activity. Pivagabine penetrates the blood-brain barrier in rats. Pivagabine antagonizes the effects of foot shock on both GABAAreceptor function and corticotropin-releasing factor (CRF) concentrations in rat brain .
Lesogaberan (AZD-3355) napadisylate is a potent and selective GABABreceptor agonist with an EC50 of 8.6 nM for human recombinant GABABreceptors. The affinity (Kis) of Lesogaberan napadisylate for rat GABAB and GABAAreceptors, as measured by displacement of [ 3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan napadisylate inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action .
Etifoxine hydrochloride, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAAreceptors. Etifoxine hydrochloride reveals anxiolytic and anticonvulsant properties in rodents .
Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAAreceptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents .
Etiocholanolone-d5 is the deuterium labeled Etiocholanolone. Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity[1]. Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the GABAAreceptor than its enantiomer form[2].
p-Hydroxybenzaldehyde-d5 is the deuterium labeled p-Hydroxybenzaldehyde[1]. p-Hydroxybenzaldehyde is a one of the major components in vanilla aroma, with antagonistic effect on GABAAreceptor of the α1β2γ2S subtype at high concentrations[2].
SCS (Salicylidene salicylhydrazide) is a potent, allosteric and selective inhibitor of β1-containing GABAAreceptors with an IC50 of 32 nM against α2β1γ1θ by VIPR measurement. SCS is also a chelator of metal ions .
AA29504 is a ethyl carbamate with γ-aminobutyric acid (GABAA(HY-L120)receptor activity. AA29504 inhibits the delivery of the neurotransmitter gamma-aminobutyric acid in the central nervous system. AA29504 can be used to research anxiety, insomnia and other neuropsychiatric diseases .
Abecarnil (ZK 112119) is a ligand or a partial agonist for benzodiazepine (BZ) receptor. Abecarnil possesses anxiolytic and anticonvulsant properties. Abecarnil can act as a positive allosteric modulator of GABAAreceptor. Abecarnil inhibits the binding of the BZ [3H]lormetazepam to rat cerebral cortex membranes, with an IC50 of 0.82 nM. Abecarnil can be used for epilepsy research .
Furosemide is a potent and orally active inhibitor of Na +/K +/2Cl - (NKCC) cotransporter, NKCC1 and NKCC2 . Furosemide is also a GABAA receptors antagonist and displays 100-fold selectivity for α6-containing receptors than α1-containing receptors. Furosemide acts as a loop diuretic and used for the study of congestive heart failure, hypertension and edema .
Furosemide sodium is a potent and orally active inhibitor of Na +/K +/2Cl - (NKCC) cotransporter, NKCC1 and NKCC2 . Furosemide sodium is also a GABAA receptors antagonist and displays 100-fold selectivity for α6-containing receptors than α1-containing receptors. Furosemide sodium acts as a loop diuretic and used for the study of congestive heart failure, hypertension and edema .
DS2 is a selective positive allosteric modulator of δ-GABAAreceptor. DS2 selectively potentiates GABA responses mediated by α4β3δ receptor. DS2 does not enhance activity at α4β3γ2 and α1β3γ2 receptors. DS2 relieves pain and has the potential for sleep disorders research .
Etiocholanolone-d2 is the deuterium labeled Etiocholanolone. Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity[1]. Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the GABAAreceptor than its enantiomer form[2][3].
Bicuculline methobromide is a selective GABAAReceptor antagonist with an IC50 value of 3 μM. Bicuculline methobromide induces clonic tonic convulsions in mammals and can also be used to block Ca 2+ activated potassium channels. Bicuculline methobromide can be used in studies of epilepsy and other related psychiatric disorders .
3α,21-Dihydroxy-5α-pregnan-20-one-d3 is the deuterium labeled 3α,21-Dihydroxy-5α-pregnan-20-one. 3α,21-Dihydroxy-5α-pregnan-20-one (THDOC), an endogenous neurosteroid, is a positive modulator of GABAAreceptors. 3α,21-Dihydroxy-5α-pregnan-20-one potentiates neuronal response to low concentrations of GABA at α4β1δ GABAAreceptors in vitro.
3-Methyl-GABA is a potent GABA aminotransferase activator. 3-Methyl-GABA can fit the binding pocket of GABAAreceptor (GABAaR). 3-Methyl-GABA can activate L-glutamic acid decarboxylase (GAD). 3-Methyl-GABA has anticonvulsant activity .
Humulone (α-Lupulic acid), a prenylated phloroglucinol derivative, is a potent cyclooxygenase-2 (COX-2) inhibitor. Humulone acts as a positive modulator of GABAAreceptor at low micromolar concentrations. Humulone is an inhibitor of bone resorption. Humulone possesses antioxidant, anti-angiogenic and apoptosis-inducing properties .
Bicuculline ((+)-Bicuculline) is A competing neurotransmitter GABAAreceptor antagonist (IC50=2 μM). Bicuculline also blocks Ca 2+ activating potassium (SK) channels and subsequently blocks slow post-hyperpolarization (slow AHP). Bicuculline has anticonvulsant activity. Bicuculline can be used to induce seizures in mice .
Bicuculline ((+)-Bicuculline; d-Bicuculline) methochloride is a selective GABAAreceptor antagonist with an IC50 value of 3 μM. Bicuculline methochloride induces clonic tonic convulsions in mammals and can also be used to block Ca 2+ activated potassium channels. Bicuculline methochloride can be used in studies of epilepsy and other related psychiatric disorders .
2'MeO6MF is a brain-penetrant positive allosteric modulator at α2β1γ2L and all α1-containing GABAAreceptors. 2'MeO6MF also can directly activate α2β2/3 and α2β2/3γ2L GABAAreceptors. 2'MeO6MF has anxiolytic and psychomotor stabilizing properties. 2'MeO6MF offers neuroprotection and improved functional recovery and dampens the stroke-induced inflammatory response .
Etifoxine-d5 is the deuterium labeled Etifoxine. Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAAreceptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents[1][2][3].
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 GABAAreceptor, but shows no effect on the amounts of α-, β-subunits .
MRK-623 (Compound 14k) is an orally active, high-affinity GABAAreceptor agonist, with the Ki values of 0.85 nM, 3.7 nM, 4.0 nM, and 0.53 nM for α1, α2, α3, and α5, respectively. MRK-623 shows anxiolytic effect .
Furosemide-d5 is the deuterium labeled Furosemide. Furosemide is a potent and orally active inhibitor of Na+/K+/2Cl- (NKCC) cotransporter, NKCC1 and NKCC2[1]. Furosemide is also a GABAA receptors antagonist and displays 100-fold selectivity for α6-containing receptors than α1-containing receptors. Furosemide acts as a loop diuretic and used for the study of congestive heart failure, hypertension and edema[2].
Furosemide (Standard) is the analytical standard of Furosemide. This product is intended for research and analytical applications. Furosemide is a potent and orally active inhibitor of Na +/K +/2Cl -?(NKCC) cotransporter, NKCC1 and NKCC2 .?Furosemide is also a GABAA?receptors antagonist and displays 100-fold selectivity for?α6-containing receptors than?α1-containing receptors. Furosemide acts as a loop diuretic and used for the study of congestive heart failure, hypertension and edema .
6-Hydroxyflavanone is a compound that can be isolated from the Muntingia calabura leaves. 6-Hydroxyflavanone targets cyclooxygenase-2 (COX-2), 5-lipoxygenase (5-LOX), and opioid and GABA-Areceptors that has anti-inflammatory and anti-neuropathic pain potential. 6-Hydroxyflavanone can be used for the research of diabetes .
MIDD0301 (GL-II-93) is an orally effective, anti-asthmatic positive allosteric modulator of GABAAreceptor. MIDD0301 had no significant adverse immune reactions at repeated doses and was better than Prednisone (HY-B0214). MIDD0301 relaxes histamine contractions in guinea pig and human tracheal smooth muscle for the study of bronchial systolic diseases .
AZD7325 is a potent and orally active partial selective PAM of GABAAα2 and Aα3 receptor (Ki=0.3 and 1.3 nM, respectively), and has less antagonistic efficacy at the Aα1 and Aα5 receptor subtypes . AZD7325 is a moderate CYP1A2 and a potent CYP3A4 inducer in vitro . AZD7325 has the potential for the investigation of anxiety and dravet syndrome . PAM: positive allosteric modulator.
TPA-023B is a high-affinity and orally active GABAAreceptorα2/α3 subtype (Kis of 0.73 nM/2 nM) partial agonist and a α1 subtype (Ki of 1.8 nM) antagonist. TPA-023B has non-sedating anxiolytic-like properties .
Bicuculline methiodide is a potent GABA(A) receptors blocker. Bicuculline methiodide alters membrane properties and firing pattern. Bicuculline methiodide reduces the Apamin-sensitive afterhyperpolarization, while Apamin is a toxin isolated from bee venom to block small conductance Ca 2+ -activated K + channels. Bicuculline methiodide facilitates burst firing via blocking apamin-sensitive Ca 2+ -activated K + current .
Gaboxadol hydrochloride (Lu 02-030 hydrochloride) is a potent agonist of the GABAAreceptor and an antagonist of GABACreceptors (IC50=25 μM). Gaboxadol hydrochloride displays a partial agonist efficacy on subunit α1β2γ2 with an ED50 value of 143 µM, a full agonist efficacy at α5 subunit (ED50=28-129 µM) and a superagonist efficacy at α4β3δ (ED50=6 µM). Gaboxadol hydrochloride is a non-opioid agent .
Tracazolate (ICI 136753) hydrochloride is a potent GABAAreceptor modulator. Tracazolate hydrochloride has selectivity for β3 and potentiates α1β1γ2s (EC50=13.2 μM), α1β3γ2 (EC50=1.5 μM). Tracazolate hydrochloride has the potency (EC50) determined by the nature of the third subunit (γ1-3, δ, ε) within the receptor complex. Tracazolate hydrochloride possesses anxiolytic and anticonvulsant activity .
Ro15-4513, imidazobenzodiazepinone derivative, is a partial inverse agonist of benzodiazepine receptor (BZR) . Ro15-4513 is a potent ethanol antagonist . Ro15-4513 has anti-anxiety effect . Ro15-4513 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
(+)-Kavain, a main kavalactone extracted from Piper methysticum, has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na + and Ca 2+ channels . (+)-Kavain is shown to bind at the α4β2δ GABAAreceptor and potentiate GABA efficacy . (+)-Kavain is used as a treatment for inflammatory diseases, its anti-inflammatory action has been widely studied .
CLP257 is a selective K +-Cl − cotransporter KCC2 activator with an EC50 of 616 nM. CLP257 is inactive against NKCC1, GABAAreceptors, KCC1, KCC3 or KCC4. CLP257 restores impaired Cl − transport in neurons with diminished KCC2 activity. CLP257 alleviates hypersensitivity in rats with neuropathic pain. CLP257 modulates plasmalemmal KCC2 protein turnover post-translationally .
Etazolate hydrochloride (SQ 20009) is an orally active, selective inhibitor of type 4 phosphodiesterase (PDE4) with an IC50 of 2 μM. Etazolate hydrochloride is a γ-aminobutyric acid A (GABAA)receptor regulator. Etazolate hydrochloride is an α-secretase activator and induced the production of soluble amyloid precursor protein (sAPPα). Etazolate hydrochloride, a pyrazolopyridine class derivative, increases cAMP levels. Etazolate hydrochloride has anxiolyticlike, antidepressant-like and anti-inflammatory effects .
Flindokalner (BMS-204352) is a potassium channel modulator. Flindokalner is a positive modulator of all neuronal Kv7 channel subtypes expressed in HEK293 cells. Flindokalner is also a large conductance calcium-activated K channel (BKca) positive modulator. Flindokalner shows a negative modulatory activity at Kv7.1 channels (Ki=3.7 μM), and acts as a negative modulator of GABAAreceptors. Flindokalner shows anxiolytic efficacy in vivo .
TP003 is a non-selective benzodiazepine site agonist with EC50s of 20.3, 10.6, 3.24, 5.64 nM for α1β2γ2, α2β3γ2, α3β3γ2, α5β2γ2, respectively. TP003 induces anxiolysis via α2GABAAreceptors .
PF-06372865 is an orally active, α2/α3/α5 subtype-selective GABAA positive allosteric modulator (PAM). PF-06372865 is a high affinity ligand at GABAAreceptors containing α1/α2/α3/α5 subunits (Kis of 2.9 nM, 21 nM, 134 nM for α2, α1 PAM, α2 PAM, respectively), with low affinity for α4/α6 subunits. PF-06372865 can across the blood-brain barrier (BBB). PF-06372865 has anxiolytic activity and has the potential for epilepsy .
LP-922761 is a potent, selective and orally active adapter protein-2 associated kinase 1 (AAK1) inhibitor with IC50s of 4.8 nM and 7.6 nM in enzyme and cell assays, respectively. LP-922761 also inhibits BMP-2-inducible protein kinase (BIKE) with an IC50 of 24 nM. LP-922761 exhibits no significant activity at cyclin G-associated kinase (GAK), opioid, adrenergic α2 or GABAareceptors .
LP-922761 hydrate is a potent, selective and orally active adapter protein-2 associated kinase 1 (AAK1) inhibitor with IC50s of 4.8 nM and 7.6 nM in enzyme and cell assays, respectively. LP-922761 hydrate also inhibits BMP-2-inducible protein kinase (BIKE) with an IC50 of 24 nM. LP-922761 hydrate shows less activity at cyclin G-associated kinase (GAK), opioid, adrenergic α2 or GABAareceptors .
(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 GABAA/BZreceptor agonist. (E)-3,4,5-Trimethoxycinnamic exhibits favourable binding affinity to 5-HT2C and 5-HT1Areceptor, 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 .
Cipepofol (Ciprofol), a novel 2,6-disubstituted phenol derivative, is a positive allosteric modulator and direct agonist of the GABAAreceptor. Cipepofol can cause the central nerve inhibition and promote sleep based on the structural modification of Propofol (HY-B0649). Cipepofol can activate the sirtuin1 (Sirt1)/Nrf2 pathway. Cipepofol protects the heart against Isoproterenol (ISO; HY-B0468)-induced myocardial infarction by reducing cardiac oxidative stress, inflammatory response and cardiomyocyte apoptosis .
L-838417 is a selective partial agonist at the α2, α3 and α5 subtypes of the GABAAreceptor and an antagonist at the α1, with binding Ki values of 0.79 nM, 0.67 nM, 1.67 nM, 267 nM, 2.25 nM and 2183 nM for α1β3γ2, α2β3γ2, α3β3γ2, α4β3γ2, α5β3γ2 and α6β3γ2 .
GABAreceptors are a class of receptors that respond to the neurotransmitter gamma-aminobutyric acid (GABA), the chief inhibitory neurotransmitter in the vertebrate central nervous system. There are two classes of GABAreceptors: GABAA and GABAB. GABAAreceptors are ligand-gated ion channels (also known as ionotropic receptors), whereas GABAB receptors are G protein-coupled receptors (also known asmetabotropic receptors). GABAreceptors are significant drug targets in the treatment of neuropsychiatric disorders such as epilepsy, insomnia, and anxiety, as well as in anesthesia in surgical operations.
MCE offers a unique collection of 139 GABAreceptors inhibitors and activators, which is an efficient tool for neuropsychiatric disorders drugs discovery.
Cholesterol myristate is a natural steroid present in traditional Chinese medicine. Cholesterol myristate binds to several ion channels such as the nicotinic acetylcholine receptor, GABAAreceptor, and the inward-rectifier potassium ion channel.
MmTx2 toxin is a GABAAreceptor modulator that enhances GABAAreceptor sensitivity to agonists. MmTx2 toxin can be obtained from venom of coral snake. MmTx2 toxin can be used in the study of neurological diseases such as epilepsy, schizophrenia and chronic pain .
Picrotin is an active compound, also is one of the composition of picrotoxin (an antagonist of GABAAreceptors (GABAARs) and glycine receptors (GlyRs)). Picrotin has sensitivity for GlyRs/b> with IC50 values range from 5.2 μM to 106 μM. Picrotin can be used for the research of neurotransmission .
Songorine is a diterpenoid alkaloid isolated from the genus Aconitum. Songorine is a GABAAreceptor antagonist in rat brain and has anti cancer, antiarrhythmic and anti-inflammatory activities. Songorine has the potential for the treatment of Epithelial ovarian cancer (EOC) .
Withasomniferolide B is a withanolide. Withasomniferolide B can be isolated from a GABAAreceptor positive activator methanol extract of the roots of Withania somnifera .
Propofol potently and directly activates GABAAreceptor and inhibits glutamate receptor mediated excitatory synaptic transmission. Propofol has antinociceptive properties and is used for sedation and hypnotic .
Tetrahydrodeoxycorticosterone, an neurosteroid, is a potent positive allosteric modulator (PAM) of GABAAreceptor. Tetrahydrodeoxycorticosterone has potent neuroinhibitory properties .
Cholesterol myristate is a natural steroid present in traditional Chinese medicine. Cholesterol myristate binds to several ion channels such as the nicotinic acetylcholine receptor, GABAAreceptor, and the inward-rectifier potassium ion channel.
Methionine (MRX-1024; D-Methionine) is an effective chemoprotective agent which can also inhibit the neuronal activity through GABAAreceptor activation.
γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain, binding to the ionotropic GABAreceptors(GABAAreceptors) and metabotropic receptors (GABABreceptors. γ-Aminobutyric acid shows calming effect by blocking specific signals of central nervous system .
p-Hydroxybenzaldehyde is a one of the major components in vanilla aroma, with antagonistic effect on GABAAreceptor of the α1β2γ2S subtype at high concentrations.
(-)-α-Pinene is a monoterpene and shows sleep enhancing property through a direct binding to GABAA-benzodiazepine (BZD) receptors by acting as a partial modulator at the BZD binding site .
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 .
Propofol (Standard) is the analytical standard of Propofol. This product is intended for research and analytical applications. Propofol potently and directly activates GABAAreceptor and inhibits glutamate receptor mediated excitatory synaptic transmission. Propofol has antinociceptive properties and is used for sedation and hypnotic .
Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity . Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the GABAAreceptor than its enantiomer form .
γ-Aminobutyric acid (Standard) is the analytical standard of γ-Aminobutyric acid. This product is intended for research and analytical applications. γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain, binding to the ionotropic GABAreceptors(GABAAreceptors) and metabotropic receptors (GABABreceptors. γ-Aminobutyric acid shows calming effect by blocking specific signals of central nervous system .
Humulone (α-Lupulic acid), a prenylated phloroglucinol derivative, is a potent cyclooxygenase-2 (COX-2) inhibitor. Humulone acts as a positive modulator of GABAAreceptor at low micromolar concentrations. Humulone is an inhibitor of bone resorption. Humulone possesses antioxidant, anti-angiogenic and apoptosis-inducing properties .
Bicuculline ((+)-Bicuculline) is A competing neurotransmitter GABAAreceptor antagonist (IC50=2 μM). Bicuculline also blocks Ca 2+ activating potassium (SK) channels and subsequently blocks slow post-hyperpolarization (slow AHP). Bicuculline has anticonvulsant activity. Bicuculline can be used to induce seizures in mice .
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 GABAAreceptor, but shows no effect on the amounts of α-, β-subunits .
6-Hydroxyflavanone is a compound that can be isolated from the Muntingia calabura leaves. 6-Hydroxyflavanone targets cyclooxygenase-2 (COX-2), 5-lipoxygenase (5-LOX), and opioid and GABA-Areceptors that has anti-inflammatory and anti-neuropathic pain potential. 6-Hydroxyflavanone can be used for the research of diabetes .
GABARAP (gamma-aminobutyric acid receptor-associated protein) is a protein that performs multiple functions within cells. As a ubiquitin-like modifier, it participates in the intracellular transport of GABA(A) receptors and interacts with the cytoskeleton. GABARAP Protein, Human (His, Fc) is the recombinant human-derived GABARAP protein, expressed by E. coli , with N-His, C-hFc labeled tag. The total length of GABARAP Protein, Human (His, Fc) is 117 a.a., with molecular weight of ~50 kDa.
GABRB2 protein is an important component of heteropentameric GABA receptors that form ligand-gated chloride channels. It plays a crucial role in establishing functional inhibitory GABAergic synapses, contributing to synaptic depression. GABRB2 Protein, Human (His) is the recombinant human-derived GABRB2 protein, expressed by E. coli , with N-His labeled tag. The total length of GABRB2 Protein, Human (His) is 219 a.a., with molecular weight of ~29.3 kDa.
GABARAP Protein is essential for regulating ubiquitination and degradation of TIAM1, a guanyl-nucleotide exchange factor (GEF) involved in RAC1 activation and downstream signaling. The D6/7 E3 ubiquitin ligase complex, where GABARAP is a key component, contributes to diverse biological processes, including cytoskeletal organization, cell migration, proliferation, and apoptosis. GABARAP Protein, Human (His-MBP) is the recombinant human-derived GABARAP protein, expressed by E. coli , with N-His, N-MBP labeled tag. The total length of GABARAP Protein, Human (His-MBP) is 117 a.a., with molecular weight of 49-58 kDa.
GABARAP (gamma-aminobutyric acid receptor-associated protein) is a protein that performs multiple functions within cells. As a ubiquitin-like modifier, it participates in the intracellular transport of GABA(A) receptors and interacts with the cytoskeleton. GABARAP Protein, Human (GST) is the recombinant human-derived GABARAP protein, expressed by E. coli , with N-GST labeled tag. The total length of GABARAP Protein, Human (GST) is 117 a.a., with molecular weight of ~37.0 kDa.
GABARAPL1/GEC-1 is a multifunctional ubiquitin-like modifier that contributes to cell surface expression of kappa-type opioid receptors and contributes to autophagy, shaping autophagosome vacuoles. Unlike LC3, which is involved in phagophore elongation, the GABARAP/GATE-16 subfamily plays a crucial role in late autophagosome maturation. GABARAPL1/GEC-1 Protein, Human (His) is the recombinant human-derived GABARAPL1/GEC-1 protein, expressed by E. coli , with N-6*His labeled tag. The total length of GABARAPL1/GEC-1 Protein, Human (His) is 117 a.a., with molecular weight of ~20.0 kDa.
Propofol-d18 is the deuterium labeled Propofol. Propofol potently and directly activates GABAAreceptor and inhibits glutamate receptor mediated excitatory synaptic transmission[1].
Valnoctamide-d5 is the deuterium labeled Valnoctamide. Valnoctamide (Valmethamide), a derivative of valproate, suppresses benzodiazepine-refractory status epilepticus. Valnoctamide (Valmethamide) acts directly on GABAAreceptors[1][2].
Propofol-d17 is the deuterium labeled Propofol. Propofol potently and directly activates GABAAreceptor and inhibits glutamate receptor mediated excitatory synaptic transmission. Propofol has antinociceptive properties[1].
Etbicyphat- 13C3 is the 13C labeled Etbicyphat (HY-139145). Etbicyphat is a potent GABA(A) receptors competitive antagonist. Etbicyphat induces epileptiform activities in hippocampal CA1 neurons, and binds to the GABA(A)-benzodiazepine receptors[1][2].
γ-Aminobutyric acid-d2 is the deuterium labeled γ-Aminobutyric acid. γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain[1][2], binding to the ionotropic GABAreceptors (GABAAreceptors) and metabotropic receptors (GABAB receptors)[2].
γ-Aminobutyric acid-d6 is the deuterium labeled γ-Aminobutyric acid. γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain[1][2], binding to the ionotropic GABAreceptors (GABAAreceptors) and metabotropic receptors (GABAB receptors)[2].
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[1][2], binding to the ionotropic GABAreceptors (GABAAreceptors) and metabotropic receptors (GABAB receptors)[2].
γ-Aminobutyric acid-4,4-d2 is the deuterium labeled γ-Aminobutyric acid. γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain[1][2], binding to the ionotropic GABAreceptors (GABAAreceptors) and metabotropic receptors (GABAB receptors)[2].
Tetrahydrodeoxycorticosterone-d3 is the deuterium labeled Tetrahydrodeoxycorticosterone. Tetrahydrodeoxycorticosterone, an neurosteroid, is a potent positive allosteric modulator (PAM) of GABAAreceptor. Tetrahydrodeoxycorticosterone has potent neuroinhibitory properties[1][2][3].
Methionine-d3 is the deuterium labeled Methionine. Methionine (MRX-1024; D-Methionine) is an effective chemoprotective agent which can also inhibit the neuronal activity through GABAAreceptor activation.
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 GABAAreceptor activation.
p-Hydroxybenzaldehyde-d4 is the deuterium labeled p-Hydroxybenzaldehyde. p-Hydroxybenzaldehyde is a one of the major components in Dendrocalamus asper bamboo shoots, with antagonistic effect on GABAAreceptor of the α1β2γ2S subtype at high concentrations.
p-Hydroxybenzaldehyde- 13C is the 13C-labeled p-Hydroxybenzaldehyde. p-Hydroxybenzaldehyde is a one of the major components in Dendrocalamus asper bamboo shoots, with antagonistic effect on GABAAreceptor of the α1β2γ2S subtype at high concentrations.
Etiocholanolone-d5 is the deuterium labeled Etiocholanolone. Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity[1]. Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the GABAAreceptor than its enantiomer form[2].
p-Hydroxybenzaldehyde-d5 is the deuterium labeled p-Hydroxybenzaldehyde[1]. p-Hydroxybenzaldehyde is a one of the major components in vanilla aroma, with antagonistic effect on GABAAreceptor of the α1β2γ2S subtype at high concentrations[2].
Etiocholanolone-d2 is the deuterium labeled Etiocholanolone. Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity[1]. Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the GABAAreceptor than its enantiomer form[2][3].
3α,21-Dihydroxy-5α-pregnan-20-one-d3 is the deuterium labeled 3α,21-Dihydroxy-5α-pregnan-20-one. 3α,21-Dihydroxy-5α-pregnan-20-one (THDOC), an endogenous neurosteroid, is a positive modulator of GABAAreceptors. 3α,21-Dihydroxy-5α-pregnan-20-one potentiates neuronal response to low concentrations of GABA at α4β1δ GABAAreceptors in vitro.
Etifoxine-d5 is the deuterium labeled Etifoxine. Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAAreceptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents[1][2][3].
Furosemide-d5 is the deuterium labeled Furosemide. Furosemide is a potent and orally active inhibitor of Na+/K+/2Cl- (NKCC) cotransporter, NKCC1 and NKCC2[1]. Furosemide is also a GABAA receptors antagonist and displays 100-fold selectivity for α6-containing receptors than α1-containing receptors. Furosemide acts as a loop diuretic and used for the study of congestive heart failure, hypertension and edema[2].
Ro15-4513, imidazobenzodiazepinone derivative, is a partial inverse agonist of benzodiazepine receptor (BZR) . Ro15-4513 is a potent ethanol antagonist . Ro15-4513 has anti-anxiety effect . Ro15-4513 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
HZ166 is a GABAAreceptor subtype-selective benzodiazepine site agonist with preferential activity at α2- and α3-GABAAreceptors. HZ166 shows anti-hyperalgesic effects . HZ166 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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