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. |
|
|
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. |
|
|