GABA Receptor

信号通路图

研究领域

抑制剂选择性比较

特异性亚型抑制剂

GABA Receptor产品

所有产品 GABA Receptor抑制剂(5) GABA Receptor激活剂(3) GABA Receptor拮抗剂(12) GABA Receptor激动剂(17) GABA Receptor调节剂(8)

目录号	产品描述	文献引用	实验数据
S1168	Valproic acid sodium salt (Sodium valproate) Valproic acid sodium salt (Sodium valproate)是一种HDAC选择性抑制剂，也会抑制HDAC2的蛋白酶体降解，用于治疗癫痫和躁郁症，并预防偏头痛。Valproic acid 可在小细胞肺癌细胞系中诱导 Notch1 信号转导。Valproic acid (VPA) 正用于研究治疗HIV和各种癌症的方法。Valproic acid (VPA) 通过上调 BNIP3 诱导自噬和线粒体自噬，并通过上调 PGC-1α 来诱导线粒体的生物合成。	Mol Med Rep, 2021, 23(1)9 Theranostics, 2020, 10(15):6790-6805 J Cell Physiol, 2020, 10.1002/jcp.29443	Western blot analysis of Acetylated Histone and Histone. 0-10μM sodium valproate was added.
S3018	Niflumic acid Niflumic acid是环氧合酶-2 (COX-2)抑制剂,用于治疗关节和肌肉疼痛。	Oncol Lett, 2020, 20(4):39
S4661	Tiagabine hydrochloride Tiagabine Hydrochloride (Gabitril, NO050328, NO328, TGB) 是tiagabine的盐酸盐形式，是哌啶甲酸衍生物，具有抗惊厥作用，它是选择性的GABA重吸收抑制剂。
S4675	Tiagabine Tiagabine (Gabitril, NO050328, NO328, TGB) 是一种抗惊厥的药物，是GABA重吸收的抑制剂。
S6470	Fluralaner Fluralaner (A1443, AH252723) 是一种口服的系统性的杀虫剂和杀螨剂。Fluralaner抑制 γ-aminobutyric acid (GABA)-gated chloride channels (GABAA receptors) 和 L-glutamate-gated chloride channels (GluCls)。
S1969	Nefiracetam Nefiracetam (DZL 221)作用于Ro 5-4864引起的抽搐，是GABAergic，胆碱及单胺类的神经系统增强剂。Phase 2。
S4772	alpha-Asarone Alpha (α)-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 is a centrally acting anti-epileptic which crosses the blood brain barrier and is used for the treatment of canine idiopathic epilepsy.
S1332	Flumazenil Flumazenil (RO 15-1788) 是一种苯二氮卓类拮抗剂。	Biomed Pharmacother, 2018, 107:1674-1681 Holist Nurs Pract, 2017, 31(3):193-203
S0303^New	CGP52432 CGP52432 是一种有效的 GABA_B autoreceptor 的选择性拮抗剂，其IC50值为0.085 μM。
S7071	(+)-Bicuculline (+)-Bicuculline是一种竞争性GABA_A受体拮抗剂，IC50为2 μM，也抑制Ca(2+)激活的钾离子通道。	Front Cell Neurosci, 2020, 14:24 Cancer Discov, 2020, CD-20-0160 Am J Physiol Lung Cell Mol Physiol, 2019, 316(1):L20-L34	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.
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.
S2026	Ginkgolide A Ginkgolide A (BN52020) 是银杏的提取物，是γ-氨基丁酸(GABA)拮抗剂，K_i为14.5 μM。	Cell Rep, 2020, 21;31(3):107521
S4587	Pentylenetetrazol Pentylenetetrazol (Pentylenetetrazole, Metrazole, pentetrazol, pentamethylenetetrazol, Corazol, Cardiazol, PTZ)是中枢神经系统和呼吸系统兴奋剂。是一种非竞争性地GABA(A)受体拮抗剂。
S6008	p-Hydroxybenzaldehyde p-Hydroxybenzaldehyde (4-Hydroxybenzaldehyde, 4-Formylphenol, p-Formylphenol)，存在于兰花Gastrodia elata、Galeola faberi和香草中，是一种羟基苯甲醛，可与NAD+和H20反应生成4-hydroxybenzoate、NADH和两质子。
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.
S4197	Bemegride Bemegride是一种中枢神经系统兴奋剂，及Barbiturate中毒的解毒剂。
S5049	Thiocolchicoside Thiocolchicoside (Thiocolchicine 2-glucoside analog, Coltramyl) 是一种天然存在的配糖体，来源于嘉兰百合的花种中，具有抗炎和止痛活性，同时具有显著的惊厥作用。它也是GABAA receptor的拮抗剂。
S6094	Imidazole-4(5)-acetic Acid Hydrochloride Imidazole-4(5)-acetic Acid Hydrochloride是GABAC receptors竞争性拮抗剂。
S9176	Pimpinellin Pimpinellin is a furocoumarin that acts as antagonist of proteins with GABA receptor activity.
S1338	Gabapentin HCl Gabapentin HCl是一种GABA类似物。
S1329	Etomidate Etomidate (R16659)是一种GABAA受体激动剂，用作短效的麻醉剂或者安定剂。
S2133	Gabapentin Gabapentin 是一种GABA类似物，用于治疗癫痫及神经痛。	Cell Death Dis, 2020, 11(9):764 Int J Clin Exp Pathol, 2018, 11(12):5536-5546
S3072	(R)-baclofen (R)-baclofen (STX 209)是一种γ-氨基丁酸衍生物，主要用于治疗痉挛。
S4574	Piperazine Piperazine (1,4-Diazacyclohexane, Diethylenediamine, exahydropyrazine, Piperazidine) 是GABA受体的激动剂，是一种用于治疗肠道线虫蛔虫和蛲虫的驱虫剂。
S4840	Baclofen Baclofen是GABA衍生物，被用作骨骼肌的弛缓药和中枢神经系统抑制剂。它能够激活GABA receptors，尤其是GABAB受体。
S3634	6-Hydroxyflavone (6-HF) 6-Hydroxyflavone是一种天然类黄酮，与GABAA receptors结合，是GABAA receptors的部分激动剂。
S4892	Phenibut Phenibut (Aminophenylbutyric acid, Fenibut, Phenigam, Phenybut, PhGABA, β-Phenyl-γ-aminobutyric acid, β-Phenyl-GABA)，作为GABA类似物，是靶向中枢神经系统的镇静剂，具有抗焦虑和镇静效果。
S2269	Baicalin Baicalin 是一种脯氨酰肽链内切酶抑制剂，影响GABA受体。	Reprod Fertil Dev, 2019, 31(5):983-992 J Nutr Biochem, 2013, 24(11):1953-62
S4961	3,4,5-Trimethoxycinnamic acid 3,4,5-Trimethoxycinnamic acid (TMCA)是Polygalae Radix的成分之一，可能通过作用于GABAA/BZ受体复合体而发挥抗癫痫活性。
S3786	Glabridin Glabridin, 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	Dihydromyricetin Dihydromyricetin (Ampelopsin, Ampeloptin)是具有良好性能的天然抗氧化剂。	Cell Signal, 2020, 65:109431 Fundam Clin Pharmacol, 2016, 30(6):596-606 Oncotarget, 2016, 10.18632/oncotarget.10836	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.
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.
S4270	Oxiracetam Oxiracetam (ISF 2522)，γ-氨基丁酸的环状衍生物(GABA)，作为益智药用以改善记忆力和学习。
S4700	4-Aminobutyric acid (GABA) 4-Aminobutyric acid (4-Aminobutanoic acid, GABA, Gamma-aminobutyric acid, Piperidic acid)是一种天然存在的神经递质，具有抑制中枢神经系统的活性。
S3748	Acamprosate Calcium Acamprosate是一种合成化合物，具有和氨基酸神经转运体GABA、氨基酸神经调质taurine类似的化学结构。
S5612	Isonipecotic acid Isonipecotic acid是杂环化合物，主要是作为GABAA receptor部分激动剂发挥作用。
S6755^New	NS 11394 NS11394是GABAA受体的正向别构调节剂，对α3和α5亚型具有选择性。
S5131	Homotaurine Homotaurine 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.
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.
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.
S5805	Allopregnanolone Allopregnanolone是一种神经类固醇，在脑内由黄体酮合成而来，是高效的GABAA receptor正向别构调节剂。
S6611	Cyclothiazide Cyclothiazide是AMPA-type glutamate receptors（AMPA型谷氨酸受体）正向别构调节剂，在神经发育与功能中发挥关键作用。	Cell Death Dis, 2020, 24;11(1):63 Eur J Med Chem, 2020, 15;192:112199 Int J Biol Sci, 2020, 25;16(11):1774-1784
S9409	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.
S3977	(-)-Borneol (-)-Borneol (L-Borneol), one of enantiomers of borneol, has a camphoraceous and evident woody odor.

目录号	产品描述	文献引用	实验数据
S1168	Valproic acid sodium salt (Sodium valproate) Valproic acid sodium salt (Sodium valproate)是一种HDAC选择性抑制剂，也会抑制HDAC2的蛋白酶体降解，用于治疗癫痫和躁郁症，并预防偏头痛。Valproic acid 可在小细胞肺癌细胞系中诱导 Notch1 信号转导。Valproic acid (VPA) 正用于研究治疗HIV和各种癌症的方法。Valproic acid (VPA) 通过上调 BNIP3 诱导自噬和线粒体自噬，并通过上调 PGC-1α 来诱导线粒体的生物合成。	Mol Med Rep,2021, 23(1)9 Theranostics,2020, 10(15):6790-6805 J Cell Physiol,2020, 10.1002/jcp.29443	Western blot analysis of Acetylated Histone and Histone. 0-10μM sodium valproate was added.
S3018	Niflumic acid Niflumic acid是环氧合酶-2 (COX-2)抑制剂,用于治疗关节和肌肉疼痛。	Oncol Lett,2020, 20(4):39
S4661	Tiagabine hydrochloride Tiagabine Hydrochloride (Gabitril, NO050328, NO328, TGB) 是tiagabine的盐酸盐形式，是哌啶甲酸衍生物，具有抗惊厥作用，它是选择性的GABA重吸收抑制剂。
S4675	Tiagabine Tiagabine (Gabitril, NO050328, NO328, TGB) 是一种抗惊厥的药物，是GABA重吸收的抑制剂。
S6470	Fluralaner Fluralaner (A1443, AH252723) 是一种口服的系统性的杀虫剂和杀螨剂。Fluralaner抑制 γ-aminobutyric acid (GABA)-gated chloride channels (GABAA receptors) 和 L-glutamate-gated chloride channels (GluCls)。

目录号	产品描述	文献引用	实验数据
S1969	Nefiracetam Nefiracetam (DZL 221)作用于Ro 5-4864引起的抽搐，是GABAergic，胆碱及单胺类的神经系统增强剂。Phase 2。
S4772	alpha-Asarone Alpha (α)-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 is a centrally acting anti-epileptic which crosses the blood brain barrier and is used for the treatment of canine idiopathic epilepsy.

目录号

产品描述

文献引用

实验数据

S1969

Nefiracetam

Nefiracetam (DZL 221)作用于Ro 5-4864引起的抽搐，是GABAergic，胆碱及单胺类的神经系统增强剂。Phase 2。

S4772

Alpha (α)-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 is a centrally acting anti-epileptic which crosses the blood brain barrier and is used for the treatment of canine idiopathic epilepsy.

目录号	产品描述	文献引用	实验数据
S1332	Flumazenil Flumazenil (RO 15-1788) 是一种苯二氮卓类拮抗剂。	Biomed Pharmacother, 2018, 107:1674-1681 Holist Nurs Pract, 2017, 31(3):193-203
S0303^New	CGP52432 CGP52432 是一种有效的 GABA_B autoreceptor 的选择性拮抗剂，其IC50值为0.085 μM。
S7071	(+)-Bicuculline (+)-Bicuculline是一种竞争性GABA_A受体拮抗剂，IC50为2 μM，也抑制Ca(2+)激活的钾离子通道。	Front Cell Neurosci, 2020, 14:24 Cancer Discov, 2020, CD-20-0160 Am J Physiol Lung Cell Mol Physiol, 2019, 316(1):L20-L34	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.
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.
S2026	Ginkgolide A Ginkgolide A (BN52020) 是银杏的提取物，是γ-氨基丁酸(GABA)拮抗剂，K_i为14.5 μM。	Cell Rep, 2020, 21;31(3):107521
S4587	Pentylenetetrazol Pentylenetetrazol (Pentylenetetrazole, Metrazole, pentetrazol, pentamethylenetetrazol, Corazol, Cardiazol, PTZ)是中枢神经系统和呼吸系统兴奋剂。是一种非竞争性地GABA(A)受体拮抗剂。
S6008	p-Hydroxybenzaldehyde p-Hydroxybenzaldehyde (4-Hydroxybenzaldehyde, 4-Formylphenol, p-Formylphenol)，存在于兰花Gastrodia elata、Galeola faberi和香草中，是一种羟基苯甲醛，可与NAD+和H20反应生成4-hydroxybenzoate、NADH和两质子。
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.
S4197	Bemegride Bemegride是一种中枢神经系统兴奋剂，及Barbiturate中毒的解毒剂。
S5049	Thiocolchicoside Thiocolchicoside (Thiocolchicine 2-glucoside analog, Coltramyl) 是一种天然存在的配糖体，来源于嘉兰百合的花种中，具有抗炎和止痛活性，同时具有显著的惊厥作用。它也是GABAA receptor的拮抗剂。
S6094	Imidazole-4(5)-acetic Acid Hydrochloride Imidazole-4(5)-acetic Acid Hydrochloride是GABAC receptors竞争性拮抗剂。
S9176	Pimpinellin Pimpinellin is a furocoumarin that acts as antagonist of proteins with GABA receptor activity.

目录号	产品描述	文献引用	实验数据
S1338	Gabapentin HCl Gabapentin HCl是一种GABA类似物。
S1329	Etomidate Etomidate (R16659)是一种GABAA受体激动剂，用作短效的麻醉剂或者安定剂。
S2133	Gabapentin Gabapentin 是一种GABA类似物，用于治疗癫痫及神经痛。	Cell Death Dis, 2020, 11(9):764 Int J Clin Exp Pathol, 2018, 11(12):5536-5546
S3072	(R)-baclofen (R)-baclofen (STX 209)是一种γ-氨基丁酸衍生物，主要用于治疗痉挛。
S4574	Piperazine Piperazine (1,4-Diazacyclohexane, Diethylenediamine, exahydropyrazine, Piperazidine) 是GABA受体的激动剂，是一种用于治疗肠道线虫蛔虫和蛲虫的驱虫剂。
S4840	Baclofen Baclofen是GABA衍生物，被用作骨骼肌的弛缓药和中枢神经系统抑制剂。它能够激活GABA receptors，尤其是GABAB受体。
S3634	6-Hydroxyflavone (6-HF) 6-Hydroxyflavone是一种天然类黄酮，与GABAA receptors结合，是GABAA receptors的部分激动剂。
S4892	Phenibut Phenibut (Aminophenylbutyric acid, Fenibut, Phenigam, Phenybut, PhGABA, β-Phenyl-γ-aminobutyric acid, β-Phenyl-GABA)，作为GABA类似物，是靶向中枢神经系统的镇静剂，具有抗焦虑和镇静效果。
S2269	Baicalin Baicalin 是一种脯氨酰肽链内切酶抑制剂，影响GABA受体。	Reprod Fertil Dev, 2019, 31(5):983-992 J Nutr Biochem, 2013, 24(11):1953-62
S4961	3,4,5-Trimethoxycinnamic acid 3,4,5-Trimethoxycinnamic acid (TMCA)是Polygalae Radix的成分之一，可能通过作用于GABAA/BZ受体复合体而发挥抗癫痫活性。
S3786	Glabridin Glabridin, 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	Dihydromyricetin Dihydromyricetin (Ampelopsin, Ampeloptin)是具有良好性能的天然抗氧化剂。	Cell Signal, 2020, 65:109431 Fundam Clin Pharmacol, 2016, 30(6):596-606 Oncotarget, 2016, 10.18632/oncotarget.10836	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.
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.
S4270	Oxiracetam Oxiracetam (ISF 2522)，γ-氨基丁酸的环状衍生物(GABA)，作为益智药用以改善记忆力和学习。
S4700	4-Aminobutyric acid (GABA) 4-Aminobutyric acid (4-Aminobutanoic acid, GABA, Gamma-aminobutyric acid, Piperidic acid)是一种天然存在的神经递质，具有抑制中枢神经系统的活性。
S3748	Acamprosate Calcium Acamprosate是一种合成化合物，具有和氨基酸神经转运体GABA、氨基酸神经调质taurine类似的化学结构。
S5612	Isonipecotic acid Isonipecotic acid是杂环化合物，主要是作为GABAA receptor部分激动剂发挥作用。

目录号	产品描述	文献引用
S6755^New	NS 11394 NS11394是GABAA受体的正向别构调节剂，对α3和α5亚型具有选择性。
S5131	Homotaurine Homotaurine 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.
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.
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.
S5805	Allopregnanolone Allopregnanolone是一种神经类固醇，在脑内由黄体酮合成而来，是高效的GABAA receptor正向别构调节剂。
S6611	Cyclothiazide Cyclothiazide是AMPA-type glutamate receptors（AMPA型谷氨酸受体）正向别构调节剂，在神经发育与功能中发挥关键作用。	Cell Death Dis, 2020, 24;11(1):63 Eur J Med Chem, 2020, 15;192:112199 Int J Biol Sci, 2020, 25;16(11):1774-1784
S9409	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.
S3977	(-)-Borneol (-)-Borneol (L-Borneol), one of enantiomers of borneol, has a camphoraceous and evident woody odor.

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GABA Receptor

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抑制剂选择性比较

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