Home Neuronal Signaling -Transmembrane Transporters GABA Receptor

GABA Receptor

Choose Selective GABA Receptor Inhibitors

GABA Receptor Signaling Pathway Map

GABA Receptor Signaling Pathways
Isoform-selective Inhibitors

GABA Receptor Products

  • All (51)
  • GABA Receptor Inhibitors (6)
  • GABA Receptor Activators (5)
  • GABA Receptor Antagonists (13)
  • GABA Receptor Agonists (18)
  • GABA Receptor Modulators (9)
  • New GABA Receptor Products
Catalog No. Product Name Information Product Use Citations Product Validations
S1168 Valproic Acid (NSC 93819) sodium salt Valproic Acid sodium salt (NSC 93819, Sodium valproate) is a HDAC inhibitor by selectively inducing proteasomal degradation of HDAC2, used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches. Valproic acid induces Notch1 signaling in small cell lung cancer (SCLC) cells. Valproic acid is under investigation for treatment of HIV and various cancers. Valproic acid (VPA) induces autophagy and mitophagy by upregulation of BNIP3 and mitochondrial biogenesis by upregulating PGC-1α.
Sci Total Environ, 2022, 838(Pt 2):155825
Transl Psychiatry, 2022, 12(1):130
Pigment Cell Melanoma Res, 2021, 10.1111/pcmr.13014
S2996 L-DAB HBR

L-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.
S3018 Niflumic acid Niflumic acid is an inhibitor of cyclooxygenase-2 used for joint and muscular pain.
Oncol Lett, 2020, 20(4):39
S4661 Tiagabine hydrochloride Tiagabine Hydrochloride (Gabitril, NO050328, NO328, TGB) is the hydrochloride salt form of tiagabine, a nipecotic acid derivative with anticonvulsant property. A selective gamma-aminobutyric acid (GABA) reuptake inhibitor.
S4675 Tiagabine Tiagabine (Gabitril, NO050328, NO328, TGB) is an anti-convulsive medication and a selective gamma-aminobutyric acid (GABA) reuptake inhibitor.
S6470 Fluralaner Fluralaner (A1443, AH252723) is a systemic insecticide and acaricide that is administered orally.Fluralaner inhibits γ-aminobutyric acid (GABA)-gated chloride channels (GABAA receptors) and L-glutamate-gated chloride channels (GluCls)
S1969 Nefiracetam Nefiracetam (DZL 221) is a GABAergic, cholinergic, and monoaminergic neuronal system enhancer for Ro 5-4864-induced convulsions. Phase 2.
S4423 Emamectin Benzoate Emamectin Benzoate (EMB, MK-244) activates gamma-amino butyric acid (GABA) transporter. Emamectin Benzoate induces of reactive oxygen species (ROS)-mediated DNA damage and apoptosis.
S4494 Methionine Methionine (MRX-1024, D-Methionine) is an activitor of GABAA receptor that modulates neuronal activity.
S4772 alpha-Asarone Alpha (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.
S5319 AWD 131-138 AWD 131-138 (Imepitoin, ELB-138) is a centrally acting anti-epileptic which crosses the blood brain barrier and is used for the treatment of canine idiopathic epilepsy. AWD 131-138 (Imepitoin) is an antiepileptic and antianxietic drug, AWD 131-138 can stimulate different recombinant isoforms of the rat GABA(A) receptor through the benzodiazepine binding site.
S0303 CGP52432 CGP52432 is a potent and selective antagonist of GABAB autoreceptor with IC50 of 0.085 μM.
J Cell Biochem, 2022, 10.1002/jcb.30231
Front Neurosci, 2021, 15:741214
S1332 Flumazenil (RO 15-1788) Flumazenil (RO 15-1788) is a competitive GABAA receptor antagonist, used in the treatment of benzodiazepine overdoses.
Biomed Pharmacother, 2018, 107:1674-1681
Holist Nurs Pract, 2017, 31(3):193-203
S2026 Ginkgolide A Ginkgolide A (BN52020) is an extract from in Ginkgo biloba and a g-aminobutyric acid (GABA) antagonist with a Ki of 14.5 μM.
Cell Rep, 2020, 21;31(3):107521
S4197 Bemegride Bemegride is a central nervous system stimulant and antidote for barbiturate poisoning.
S4587 Pentylenetetrazol Pentylenetetrazol (Pentylenetetrazole, Metrazole, pentetrazol, pentamethylenetetrazol, Corazol, Cardiazol, PTZ) displays activity as a central nervous system and respiratory stimulant. It is considered a non-competitive GABA(A) receptor antagonist.
S5049 Thiocolchicoside Thiocolchicoside (Thiocolchicine 2-glucoside analog, Coltramyl) is a natural occuring glycoside originated from the flower seeds of superba gloriosa with anti-inflammatory and analgesic properties as well as pronounced convulsant activity. It is also an antagonist of GABAA receptor.
S5194 Furosemide sodium Furosemide (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.
S6008 p-Hydroxybenzaldehyde p-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.
S6094 Imidazole-4(5)-acetic Acid Hydrochloride Imidazole-4(5)-acetic Acid Hydrochloride is a competitive antagonist at GABAC receptors.
S7071 (+)-Bicuculline (+)-Bicuculline (d-Bicuculline) is a competitive antagonist of GABAA receptors with IC50 of 2 μM, also blocks Ca(2+)-activated potassium channels.
Acta Pharmacol Sin, 2022, 10.1038/s41401-021-00854-7
Biomedicines, 2021, 9(12)1927
Neurobiol Dis, 2021, 156:105407
S9065 Songorine Songorine, 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.
S9176 Pimpinellin Pimpinellin is a furocoumarin that acts as antagonist of proteins with GABA receptor activity.
S9249 Securinine Securinine, a major natural alkaloid product from the root of the plant Securinega suffruticosa, acts as a γ-amino butyric acid (GABA) receptor antagonist.
S1329 Etomidate Etomidate (R16659) is a GABAA receptor agonist, used as a short-acting anaesthetic agent or sedative.
S1338 Gabapentin HCl Gabapentin HCl is a GABA analogue, used to treat seizures and neuropathic pain.
Mol Pharmacol, 2022, 101(4):236-245
Int J Clin Exp Pathol, 2018, 11(12):5536-5546
J Aging Sci, 2017, 5:1
S2133 Gabapentin Gabapentin is a GABA analogue, used to treat seizures and neuropathic pain.
Mol Pharmacol, 2022, 101(4):236-245
Cell Death Dis, 2020, 11(9):764
Int J Clin Exp Pathol, 2018, 11(12):5536-5546
S2269 Baicalin (NSC-661431) Baicalin (NSC-661431) is a known prolyl endopeptidase inhibitor and affects the GABA receptors.
Molecules, 2021, 26(5)1210
Innate Immun, 2021, 27(7-8):533-542
Reprod Fertil Dev, 2019, 31(5):983-992
S2399 Dihydromyricetin Dihydromyricetin (Ampelopsin, Ampeloptin) is a natural antioxidant flavonoid from Ampelopsis grossedentata.
Molecules, 2021, 26(5)1210
Cell Signal, 2020, 65:109431
J Med Virol, 2019, 91(8):1440-1447
S3072 (R)-baclofen (R)-baclofen (STX 209) is a derivative of gamma-aminobutyric acid primarily used to treat spasticity.
J Cell Biochem, 2022, 10.1002/jcb.30231
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.
S3663 Afloqualone Afloqualone (AFQ, HQ-495) is a quinazolinone family GABAergic drug with muscle-relaxant and sedative effects, showing the agonist activity at the β subtype of the GABAa receptor.
S3748 Acamprosate Calcium Acamprosate (N-Acetylhomotaurine, Calcium acetylhomotaurinate), is a synthetic compound with a chemical structure similar to the amino acid neurotransmitter gamma-aminobutyric acid (GABA) and the amino acid neuromodulator taurine.
S3786 Glabridin Glabridin (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.
Life Sci, 2021, S0024-3205(20)31752-5
S4270 Oxiracetam Oxiracetam (ISF 2522), a cyclic derivative of gamma-aminobutyric acid (GABA), is used as a nootropic drug to improve memory and learning.
S4574 Piperazine Piperazine (1,4-Diazacyclohexane, Diethylenediamine, exahydropyrazine, Piperazidine), GABA receptor agonist, is an anthelmintic used in the treatment of the intestinal nematodes Ascaris lumbricoides and Enterobius vermicularis.
S4700 4-Aminobutyric acid (GABA) 4-Aminobutyric acid (4-Aminobutanoic acid, GABA, Gamma-aminobutyric acid, Piperidic acid) is a naturally occurring neurotransmitter with central nervous system (CNS) inhibitory activity.
S4724 Etomidate hydrochloride Etomidate (Amidate, R 16659) hydrochloride is a general anesthetic that produces its effects by enhancing GABA(A) receptor activity.
S4840 Baclofen Baclofen is a gamma-amino-butyric acid (GABA) derivative used as a skeletal muscle relaxant and central nervous system depressant. It activates GABA receptors, specifically the GABAB receptors.
S4892 Phenibut Phenibut (Aminophenylbutyric acid, Fenibut, Phenigam, Phenybut, PhGABA, β-Phenyl-γ-aminobutyric acid, β-Phenyl-GABA), a GABA analogue, is a central nervous system depressant with anxiolytic and sedative effects.
S4961 3,4,5-Trimethoxycinnamic acid 3,4,5-Trimethoxycinnamic acid (TMCA) is one of the constituents of Polygalae Radix and may exert anti-seizure activity by acting at the GABAA/BZ receptor complex.
S5612 Isonipecotic acid Isonipecotic acid (4-Piperidinecarboxylic acid, 4-Carboxypiperidine, Hexahydroisonicotinic acid) is a heterocyclic compound that mainly acts as a GABAA receptor partial agonist.
E0960New RO5186582 RO5186582 (Basmisanil, RG1662) is a highly selective GABAAα5 negative allosteric modulator.
S3959 (+)-Borneol (+)-Borneol is one of enantiomers of borneol which is a valuable medical material, senior aromatic spice, and chemical material and has been used in food and also folk medicine.
S3977 (-)-Borneol (-)-Borneol (L-Borneol), one of enantiomers of borneol, has a camphoraceous and evident woody odor. (-)-Borneol has a highly efficacious positive modulating action at GABA receptor with an EC50 of 237 μM.
S5131 Homotaurine Homotaurine (Tramiprosate, Alzhemed, 3-Amino-1-propanesulfonic acid) is a synthetic organic compound that has GABAergic activity by mimicking GABA. It is a GABAA partial agonist as well as a GABAB receptor partial agonist with low efficacy.
S5596 (1S)-(-)-α-Pinene α-Pinene is found in the oils of many species of many coniferous trees, notably the pine and has insecticidal activity. (1S)-(-)-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.
S5805 Allopregnanolone Allopregnanolone, a neurosteroid synthesized from progesterone in brain, acts as a highly potent positive allosteric modulator of the GABAA receptor.
S6611 Cyclothiazide Cyclothiazide is a positive allosteric modulator of ionotropic α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA)-type glutamate receptors with critical roles in neurological development and function.
Adv Sci (Weinh), 2021, e2004846
Cell Death Discov, 2021, 7(1):201
Exp Cell Res, 2021, 406(1):112735
S6755 NS 11394 NS11394 is a subtype-selective positive allosteric modulator at GABAA receptors, with selectivity for the α3 and α5 subtypes.
S9409 Kavain Kavain ((+)-Kavain), 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.
S1168 Valproic Acid (NSC 93819) sodium salt Valproic Acid sodium salt (NSC 93819, Sodium valproate) is a HDAC inhibitor by selectively inducing proteasomal degradation of HDAC2, used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches. Valproic acid induces Notch1 signaling in small cell lung cancer (SCLC) cells. Valproic acid is under investigation for treatment of HIV and various cancers. Valproic acid (VPA) induces autophagy and mitophagy by upregulation of BNIP3 and mitochondrial biogenesis by upregulating PGC-1α.
Sci Total Environ, 2022, 838(Pt 2):155825
Transl Psychiatry, 2022, 12(1):130
Pigment Cell Melanoma Res, 2021, 10.1111/pcmr.13014
S2996 L-DAB HBR

L-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.
S3018 Niflumic acid Niflumic acid is an inhibitor of cyclooxygenase-2 used for joint and muscular pain.
Oncol Lett, 2020, 20(4):39
S4661 Tiagabine hydrochloride Tiagabine Hydrochloride (Gabitril, NO050328, NO328, TGB) is the hydrochloride salt form of tiagabine, a nipecotic acid derivative with anticonvulsant property. A selective gamma-aminobutyric acid (GABA) reuptake inhibitor.
S4675 Tiagabine Tiagabine (Gabitril, NO050328, NO328, TGB) is an anti-convulsive medication and a selective gamma-aminobutyric acid (GABA) reuptake inhibitor.
S6470 Fluralaner Fluralaner (A1443, AH252723) is a systemic insecticide and acaricide that is administered orally.Fluralaner inhibits γ-aminobutyric acid (GABA)-gated chloride channels (GABAA receptors) and L-glutamate-gated chloride channels (GluCls)
S1969 Nefiracetam Nefiracetam (DZL 221) is a GABAergic, cholinergic, and monoaminergic neuronal system enhancer for Ro 5-4864-induced convulsions. Phase 2.
S4423 Emamectin Benzoate Emamectin Benzoate (EMB, MK-244) activates gamma-amino butyric acid (GABA) transporter. Emamectin Benzoate induces of reactive oxygen species (ROS)-mediated DNA damage and apoptosis.
S4494 Methionine Methionine (MRX-1024, D-Methionine) is an activitor of GABAA receptor that modulates neuronal activity.
S4772 alpha-Asarone Alpha (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.
S5319 AWD 131-138 AWD 131-138 (Imepitoin, ELB-138) is a centrally acting anti-epileptic which crosses the blood brain barrier and is used for the treatment of canine idiopathic epilepsy. AWD 131-138 (Imepitoin) is an antiepileptic and antianxietic drug, AWD 131-138 can stimulate different recombinant isoforms of the rat GABA(A) receptor through the benzodiazepine binding site.
S0303 CGP52432 CGP52432 is a potent and selective antagonist of GABAB autoreceptor with IC50 of 0.085 μM.
J Cell Biochem, 2022, 10.1002/jcb.30231
Front Neurosci, 2021, 15:741214
S1332 Flumazenil (RO 15-1788) Flumazenil (RO 15-1788) is a competitive GABAA receptor antagonist, used in the treatment of benzodiazepine overdoses.
Biomed Pharmacother, 2018, 107:1674-1681
Holist Nurs Pract, 2017, 31(3):193-203
S2026 Ginkgolide A Ginkgolide A (BN52020) is an extract from in Ginkgo biloba and a g-aminobutyric acid (GABA) antagonist with a Ki of 14.5 μM.
Cell Rep, 2020, 21;31(3):107521
S4197 Bemegride Bemegride is a central nervous system stimulant and antidote for barbiturate poisoning.
S4587 Pentylenetetrazol Pentylenetetrazol (Pentylenetetrazole, Metrazole, pentetrazol, pentamethylenetetrazol, Corazol, Cardiazol, PTZ) displays activity as a central nervous system and respiratory stimulant. It is considered a non-competitive GABA(A) receptor antagonist.
S5049 Thiocolchicoside Thiocolchicoside (Thiocolchicine 2-glucoside analog, Coltramyl) is a natural occuring glycoside originated from the flower seeds of superba gloriosa with anti-inflammatory and analgesic properties as well as pronounced convulsant activity. It is also an antagonist of GABAA receptor.
S5194 Furosemide sodium Furosemide (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.
S6008 p-Hydroxybenzaldehyde p-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.
S6094 Imidazole-4(5)-acetic Acid Hydrochloride Imidazole-4(5)-acetic Acid Hydrochloride is a competitive antagonist at GABAC receptors.
S7071 (+)-Bicuculline (+)-Bicuculline (d-Bicuculline) is a competitive antagonist of GABAA receptors with IC50 of 2 μM, also blocks Ca(2+)-activated potassium channels.
Acta Pharmacol Sin, 2022, 10.1038/s41401-021-00854-7
Biomedicines, 2021, 9(12)1927
Neurobiol Dis, 2021, 156:105407
S9065 Songorine Songorine, 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.
S9176 Pimpinellin Pimpinellin is a furocoumarin that acts as antagonist of proteins with GABA receptor activity.
S9249 Securinine Securinine, a major natural alkaloid product from the root of the plant Securinega suffruticosa, acts as a γ-amino butyric acid (GABA) receptor antagonist.
S1329 Etomidate Etomidate (R16659) is a GABAA receptor agonist, used as a short-acting anaesthetic agent or sedative.
S1338 Gabapentin HCl Gabapentin HCl is a GABA analogue, used to treat seizures and neuropathic pain.
Mol Pharmacol, 2022, 101(4):236-245
Int J Clin Exp Pathol, 2018, 11(12):5536-5546
J Aging Sci, 2017, 5:1
S2133 Gabapentin Gabapentin is a GABA analogue, used to treat seizures and neuropathic pain.
Mol Pharmacol, 2022, 101(4):236-245
Cell Death Dis, 2020, 11(9):764
Int J Clin Exp Pathol, 2018, 11(12):5536-5546
S2269 Baicalin (NSC-661431) Baicalin (NSC-661431) is a known prolyl endopeptidase inhibitor and affects the GABA receptors.
Molecules, 2021, 26(5)1210
Innate Immun, 2021, 27(7-8):533-542
Reprod Fertil Dev, 2019, 31(5):983-992
S2399 Dihydromyricetin Dihydromyricetin (Ampelopsin, Ampeloptin) is a natural antioxidant flavonoid from Ampelopsis grossedentata.
Molecules, 2021, 26(5)1210
Cell Signal, 2020, 65:109431
J Med Virol, 2019, 91(8):1440-1447
S3072 (R)-baclofen (R)-baclofen (STX 209) is a derivative of gamma-aminobutyric acid primarily used to treat spasticity.
J Cell Biochem, 2022, 10.1002/jcb.30231
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.
S3663 Afloqualone Afloqualone (AFQ, HQ-495) is a quinazolinone family GABAergic drug with muscle-relaxant and sedative effects, showing the agonist activity at the β subtype of the GABAa receptor.
S3748 Acamprosate Calcium Acamprosate (N-Acetylhomotaurine, Calcium acetylhomotaurinate), is a synthetic compound with a chemical structure similar to the amino acid neurotransmitter gamma-aminobutyric acid (GABA) and the amino acid neuromodulator taurine.
S3786 Glabridin Glabridin (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.
Life Sci, 2021, S0024-3205(20)31752-5
S4270 Oxiracetam Oxiracetam (ISF 2522), a cyclic derivative of gamma-aminobutyric acid (GABA), is used as a nootropic drug to improve memory and learning.
S4574 Piperazine Piperazine (1,4-Diazacyclohexane, Diethylenediamine, exahydropyrazine, Piperazidine), GABA receptor agonist, is an anthelmintic used in the treatment of the intestinal nematodes Ascaris lumbricoides and Enterobius vermicularis.
S4700 4-Aminobutyric acid (GABA) 4-Aminobutyric acid (4-Aminobutanoic acid, GABA, Gamma-aminobutyric acid, Piperidic acid) is a naturally occurring neurotransmitter with central nervous system (CNS) inhibitory activity.
S4724 Etomidate hydrochloride Etomidate (Amidate, R 16659) hydrochloride is a general anesthetic that produces its effects by enhancing GABA(A) receptor activity.
S4840 Baclofen Baclofen is a gamma-amino-butyric acid (GABA) derivative used as a skeletal muscle relaxant and central nervous system depressant. It activates GABA receptors, specifically the GABAB receptors.
S4892 Phenibut Phenibut (Aminophenylbutyric acid, Fenibut, Phenigam, Phenybut, PhGABA, β-Phenyl-γ-aminobutyric acid, β-Phenyl-GABA), a GABA analogue, is a central nervous system depressant with anxiolytic and sedative effects.
S4961 3,4,5-Trimethoxycinnamic acid 3,4,5-Trimethoxycinnamic acid (TMCA) is one of the constituents of Polygalae Radix and may exert anti-seizure activity by acting at the GABAA/BZ receptor complex.
S5612 Isonipecotic acid Isonipecotic acid (4-Piperidinecarboxylic acid, 4-Carboxypiperidine, Hexahydroisonicotinic acid) is a heterocyclic compound that mainly acts as a GABAA receptor partial agonist.
E0960New RO5186582 RO5186582 (Basmisanil, RG1662) is a highly selective GABAAα5 negative allosteric modulator.
S3959 (+)-Borneol (+)-Borneol is one of enantiomers of borneol which is a valuable medical material, senior aromatic spice, and chemical material and has been used in food and also folk medicine.
S3977 (-)-Borneol (-)-Borneol (L-Borneol), one of enantiomers of borneol, has a camphoraceous and evident woody odor. (-)-Borneol has a highly efficacious positive modulating action at GABA receptor with an EC50 of 237 μM.
S5131 Homotaurine Homotaurine (Tramiprosate, Alzhemed, 3-Amino-1-propanesulfonic acid) is a synthetic organic compound that has GABAergic activity by mimicking GABA. It is a GABAA partial agonist as well as a GABAB receptor partial agonist with low efficacy.
S5596 (1S)-(-)-α-Pinene α-Pinene is found in the oils of many species of many coniferous trees, notably the pine and has insecticidal activity. (1S)-(-)-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.
S5805 Allopregnanolone Allopregnanolone, a neurosteroid synthesized from progesterone in brain, acts as a highly potent positive allosteric modulator of the GABAA receptor.
S6611 Cyclothiazide Cyclothiazide is a positive allosteric modulator of ionotropic α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA)-type glutamate receptors with critical roles in neurological development and function.
Adv Sci (Weinh), 2021, e2004846
Cell Death Discov, 2021, 7(1):201
Exp Cell Res, 2021, 406(1):112735
S6755 NS 11394 NS11394 is a subtype-selective positive allosteric modulator at GABAA receptors, with selectivity for the α3 and α5 subtypes.
S9409 Kavain Kavain ((+)-Kavain), 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.
E0960New RO5186582 RO5186582 (Basmisanil, RG1662) is a highly selective GABAAα5 negative allosteric modulator.
Tags: GABA inhibition | GABA receptor activation | GABA function | GABA drugs | GABA activity | GABA pathway | GABA-A receptor function | GABA receptor function | GABA activation | gamma aminobutyric acid function | GABA cancer | GABA assay | GABA receptor drugs | GABA receptor inhibition | GABA receptor signaling | GABA receptors review | GABA agonists list | GABA antagonist drugs | GABA inhibitor drugs | GABA inhibitor review