GABA Receptor
Inhibitory Selectivity
Isoform-specific Inhibitors
GABA Receptor Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S2996New |
L-DAB HBRL-DAB HBR (L-Dab Hydrobromide, L-2,4-Diaminobutyric acid hydrobromide) is an inhibitor of GABA (Gamma-aminobutyric acid) transaminase with IC50 of >500 μM. L-DAB HBR exhibits antitumor activity. |
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| S5194New |
Furosemide sodiumFurosemide (Frusemide) sodium is a potent and orally active inhibitor of Na-K-Cl cotransporter (NKCC). Furosemide sodium is a subtype-selective antagonist of gamma-aminobutyric acid type A (GABAA) receptor. |
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| S4494New |
MethionineMethionine (MRX-1024, D-Methionine) is an activitor of GABAA receptor that modulates neuronal activity. |
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| S4423New |
Emamectin BenzoateEmamectin Benzoate (EMB, MK-244) activates gamma-amino butyric acid (GABA) transporter. Emamectin Benzoate induces of reactive oxygen species (ROS)-mediated DNA damage and apoptosis. |
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| S4772 |
alpha-AsaroneAlpha (α)-asarone (trans-Asarone) is one of the main pharmacologically active compounds present in Acorus calamus Linn (Acoraceae), Acorus tatarinowii Schott (Acoraceae), and Acorus gramineus Solander. It has anticonvulsant, neuroprotective, anxiolytic and nootropic effects. |
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| S7071 |
(+)-Bicuculline(+)-Bicuculline (d-Bicuculline) is a competitive antagonist of GABAA receptors with IC50 of 2 μM, also blocks Ca(2+)-activated potassium channels. |
-Bicuculline-S707101X0320161109.gif)
-Bicuculline-S707101X0320161109.gif)
Effects of antagonists on the anti-hyperalgesic effects of sinomenine in CCI rats. * P<0.05 as compared to vehicle control group (N=8 per group). The GABAA receptor antagonist bicuculline but not the opioid receptor antagonist naltrexone nor the 5-HT1A receptor antagonist WAY100635 blocked the antinociceptive effects of 40 mg/kg sinomenine. |
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| S0303 |
CGP52432CGP52432 is a potent and selective antagonist of GABAB autoreceptor with IC50 of 0.085 μM. |
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| S2026 |
Ginkgolide AGinkgolide A (BN52020) is an extract from in Ginkgo biloba and a g-aminobutyric acid (GABA) antagonist with a Ki of 14.5 μM. |
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| S6100New |
PicrotoxinPicrotoxin (Picrotin, Cocculin, Cocculus, NSC 403139), a plant alkaloid, is a non-competitive antagonist of neuronal GABA and glycine receptors. |
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| S6008 |
p-Hydroxybenzaldehydep-Hydroxybenzaldehyde (4-Hydroxybenzaldehyde, 4-Formylphenol, p-Formylphenol), which can be found in the orchids Gastrodia elata, Galeola faberi and vanilla, is a hydroxybenzaldehyde that reacts with NAD+ and H2O to produce 4-hydroxybenzoate, NADH, and 2 protons. p-Hydroxybenzaldehyde at 101.7 μM can significantly reduce the GABA-induced chloride current of GABAA receptors(α1β2γ2S subtype) expressed. |
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| S9065 |
SongorineSongorine, a ubiquitous alkaloid in the genus Aconitum, is a novel antagonist of the GABAA receptor in rat brain and has antiarrhythmic, antinociceptive, anti-inflammatory, regenerative and CNS-modulating properties. |
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| S6094 |
Imidazole-4(5)-acetic Acid HydrochlorideImidazole-4(5)-acetic Acid Hydrochloride is a competitive antagonist at GABAC receptors. |
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| S9176 |
PimpinellinPimpinellin is a furocoumarin that acts as antagonist of proteins with GABA receptor activity. |
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| S3634 |
6-Hydroxyflavone (6-HF)6-Hydroxyflavone, a naturally occurring flavonoid, binds to GABAA receptors with moderate affinity and acts as a partial agonist of GABAA receptors. |
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| S4724New |
Etomidate hydrochlorideEtomidate (Amidate, R 16659) hydrochloride is a general anesthetic that produces its effects by enhancing GABA(A) receptor activity. |
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| S3786 |
GlabridinGlabridin (Q-100692, KB-289522, LS-176045), one of the active phytochemicals in licorice extract, binds to and activates the ligand binding domain of PPARγ, as well as the full length receptor. It is also a GABAA receptor positive modulator promoting fatty acid oxidation and improving learning and memory. |
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| S2399 |
DihydromyricetinDihydromyricetin (Ampelopsin, Ampeloptin) is a natural antioxidant flavonoid from Ampelopsis grossedentata. |
ADH and ALDH expressions in 40% ethanol loaded mice for three hours. Group 1, 500 lM taraxerone; Group 2, 1 mM taraxerone; Group 3, 3 mM DHM (positive control); Group 4, DMSO (control); Group 5, saline. Taraxerone and DHM were dissolved in DMSO, and all treated samples (ethanol, taraxerone, DHM, DMSO, and saline) were administered orally (5 mL/kg body weight). The same letters denote significant differences at p < 0.05, and the error bar represents standard deviation. |
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| S5612 |
Isonipecotic acidIsonipecotic acid (4-Piperidinecarboxylic acid, 4-Carboxypiperidine, Hexahydroisonicotinic acid) is a heterocyclic compound that mainly acts as a GABAA receptor partial agonist. |
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| S9409 |
KavainKavain, the main kavalactone found mostly in the roots of the kava plant, has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na+ and Ca2+ channels. Kavain positively modulated γ-Aminobutyric acid type A (GABAA) receptor. |
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| S6755 |
NS 11394NS11394 is a subtype-selective positive allosteric modulator at GABAA receptors, with selectivity for the α3 and α5 subtypes. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S2996New |
L-DAB HBRL-DAB HBR (L-Dab Hydrobromide, L-2,4-Diaminobutyric acid hydrobromide) is an inhibitor of GABA (Gamma-aminobutyric acid) transaminase with IC50 of >500 μM. L-DAB HBR exhibits antitumor activity. |
||
| S5194New |
Furosemide sodiumFurosemide (Frusemide) sodium is a potent and orally active inhibitor of Na-K-Cl cotransporter (NKCC). Furosemide sodium is a subtype-selective antagonist of gamma-aminobutyric acid type A (GABAA) receptor. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S4494New |
MethionineMethionine (MRX-1024, D-Methionine) is an activitor of GABAA receptor that modulates neuronal activity. |
||
| S4423New |
Emamectin BenzoateEmamectin Benzoate (EMB, MK-244) activates gamma-amino butyric acid (GABA) transporter. Emamectin Benzoate induces of reactive oxygen species (ROS)-mediated DNA damage and apoptosis. |
||
| S4772 |
alpha-AsaroneAlpha (α)-asarone (trans-Asarone) is one of the main pharmacologically active compounds present in Acorus calamus Linn (Acoraceae), Acorus tatarinowii Schott (Acoraceae), and Acorus gramineus Solander. It has anticonvulsant, neuroprotective, anxiolytic and nootropic effects. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S7071 |
(+)-Bicuculline(+)-Bicuculline (d-Bicuculline) is a competitive antagonist of GABAA receptors with IC50 of 2 μM, also blocks Ca(2+)-activated potassium channels. |
-Bicuculline-S707101X0320161109.gif)
Effects of antagonists on the anti-hyperalgesic effects of sinomenine in CCI rats. * P<0.05 as compared to vehicle control group (N=8 per group). The GABAA receptor antagonist bicuculline but not the opioid receptor antagonist naltrexone nor the 5-HT1A receptor antagonist WAY100635 blocked the antinociceptive effects of 40 mg/kg sinomenine. |
|
| S0303 |
CGP52432CGP52432 is a potent and selective antagonist of GABAB autoreceptor with IC50 of 0.085 μM. |
||
| S2026 |
Ginkgolide AGinkgolide A (BN52020) is an extract from in Ginkgo biloba and a g-aminobutyric acid (GABA) antagonist with a Ki of 14.5 μM. |
||
| S6100New |
PicrotoxinPicrotoxin (Picrotin, Cocculin, Cocculus, NSC 403139), a plant alkaloid, is a non-competitive antagonist of neuronal GABA and glycine receptors. |
||
| S6008 |
p-Hydroxybenzaldehydep-Hydroxybenzaldehyde (4-Hydroxybenzaldehyde, 4-Formylphenol, p-Formylphenol), which can be found in the orchids Gastrodia elata, Galeola faberi and vanilla, is a hydroxybenzaldehyde that reacts with NAD+ and H2O to produce 4-hydroxybenzoate, NADH, and 2 protons. p-Hydroxybenzaldehyde at 101.7 μM can significantly reduce the GABA-induced chloride current of GABAA receptors(α1β2γ2S subtype) expressed. |
||
| S9065 |
SongorineSongorine, a ubiquitous alkaloid in the genus Aconitum, is a novel antagonist of the GABAA receptor in rat brain and has antiarrhythmic, antinociceptive, anti-inflammatory, regenerative and CNS-modulating properties. |
||
| S6094 |
Imidazole-4(5)-acetic Acid HydrochlorideImidazole-4(5)-acetic Acid Hydrochloride is a competitive antagonist at GABAC receptors. |
||
| S9176 |
PimpinellinPimpinellin is a furocoumarin that acts as antagonist of proteins with GABA receptor activity. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S3634 |
6-Hydroxyflavone (6-HF)6-Hydroxyflavone, a naturally occurring flavonoid, binds to GABAA receptors with moderate affinity and acts as a partial agonist of GABAA receptors. |
||
| S4724New |
Etomidate hydrochlorideEtomidate (Amidate, R 16659) hydrochloride is a general anesthetic that produces its effects by enhancing GABA(A) receptor activity. |
||
| S3786 |
GlabridinGlabridin (Q-100692, KB-289522, LS-176045), one of the active phytochemicals in licorice extract, binds to and activates the ligand binding domain of PPARγ, as well as the full length receptor. It is also a GABAA receptor positive modulator promoting fatty acid oxidation and improving learning and memory. |
||
| S2399 |
DihydromyricetinDihydromyricetin (Ampelopsin, Ampeloptin) is a natural antioxidant flavonoid from Ampelopsis grossedentata. |
ADH and ALDH expressions in 40% ethanol loaded mice for three hours. Group 1, 500 lM taraxerone; Group 2, 1 mM taraxerone; Group 3, 3 mM DHM (positive control); Group 4, DMSO (control); Group 5, saline. Taraxerone and DHM were dissolved in DMSO, and all treated samples (ethanol, taraxerone, DHM, DMSO, and saline) were administered orally (5 mL/kg body weight). The same letters denote significant differences at p < 0.05, and the error bar represents standard deviation. |
|
| S5612 |
Isonipecotic acidIsonipecotic acid (4-Piperidinecarboxylic acid, 4-Carboxypiperidine, Hexahydroisonicotinic acid) is a heterocyclic compound that mainly acts as a GABAA receptor partial agonist. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S9409 |
KavainKavain, the main kavalactone found mostly in the roots of the kava plant, has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na+ and Ca2+ channels. Kavain positively modulated γ-Aminobutyric acid type A (GABAA) receptor. |
||
| S6755 |
NS 11394NS11394 is a subtype-selective positive allosteric modulator at GABAA receptors, with selectivity for the α3 and α5 subtypes. |
