GABA Receptor

信号通路图

研究领域

抑制剂选择性比较
溶解性比较

目录号	产品目录	溶解度(25°C)
目录号	产品目录	水	DMSO	酒精
S1168	Valproic acid sodium salt (Sodium valproate)	33 mg/mL	33 mg/mL	33 mg/mL
S3018	Niflumic acid	<1 mg/mL	56 mg/mL	<1 mg/mL
S4661	Tiagabine hydrochloride	11 mg/mL	82 mg/mL	82 mg/mL
S1969	Nefiracetam	5 mg/mL	49 mg/mL	49 mg/mL
S1332	Flumazenil	<1 mg/mL	5 mg/mL	<1 mg/mL
S6094	Imidazole-4(5)-acetic Acid Hydrochloride	-1 mg/mL	10 mg/mL	-1 mg/mL
S9249	Securinine	-1 mg/mL	44 mg/mL	-1 mg/mL
S9176	Pimpinellin	-1 mg/mL	49 mg/mL	-1 mg/mL
s9065	Songorine	-1 mg/mL	71 mg/mL	-1 mg/mL
S5049	Thiocolchicoside	100 mg/mL	100 mg/mL	2 mg/mL
S7071	(+)-Bicuculline	<1 mg/mL	21 mg/mL	<1 mg/mL
S2026	Ginkgolide A	<1 mg/mL	81 mg/mL	2 mg/mL
S4587	Pentylenetetrazol	27 mg/mL	27 mg/mL	27 mg/mL
S4197	Bemegride	<1 mg/mL	31 mg/mL	31 mg/mL
S1338	Gabapentin HCl	42 mg/mL	<1 mg/mL	<1 mg/mL
S1329	Etomidate	<1 mg/mL	49 mg/mL	49 mg/mL
S2133	Gabapentin	34 mg/mL	<1 mg/mL	<1 mg/mL
S5612	Isonipecotic acid	26 mg/mL	<1 mg/mL	-1 mg/mL
S4840	Baclofen	0.1 mg/mL	<1 mg/mL	<1 mg/mL
S4892	Phenibut	-1 mg/mL	35 mg/mL	-1 mg/mL
S3072	(R)-baclofen	8 mg/mL	<1 mg/mL	<1 mg/mL
S4574	Piperazine	17 mg/mL	8 mg/mL	17 mg/mL
S3634	6-Hydroxyflavone (6-HF)	<1 mg/mL	47 mg/mL	<1 mg/mL
S2269	Baicalin	<1 mg/mL	89 mg/mL	<1 mg/mL
S3786	Glabridin	-1 mg/mL	64 mg/mL	-1 mg/mL
S2399	Dihydromyricetin	<1 mg/mL	64 mg/mL	64 mg/mL
S3663	Afloqualone	<1 mg/mL	56 mg/mL	28 mg/mL
S4270	Oxiracetam	31 mg/mL	31 mg/mL	<1 mg/mL
S4700	4-Aminobutyric acid (GABA)	20 mg/mL	<1 mg/mL	<1 mg/mL
S3748	Acamprosate Calcium	40 mg/mL	<1 mg/mL	<1 mg/mL
S5805	Allopregnanolone	<1 mg/mL	64 mg/mL	31 mg/mL

特异性亚型抑制剂

GABA Receptor产品

所有产品 GABA Receptor抑制剂(4) GABA Receptor激活剂(1) GABA Receptor拮抗剂(10) GABA Receptor激动剂(16) GABA Receptor调节剂(2) 新GABA Receptor产品

产品目录	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。	Nat Biotechnol, 2015, 10.1038/nbt.3130 J Neurosci, 2013, 33(17):7535-47 Cell Death Dis, 2016, 7:e2221	(A,B) Wild-type C57BL/6 male mice were treated with vehicle (saline) or 10 mg/kg of paraquat (PQ) for 3 days, and mice received VPA (3.5 mg/kg) or anacardic acid (5 mg/kg) starting 24 and 1 h before PQ injection. IL-6 mRNA expression was determined by real-time PCR.
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。
S4661	Tiagabine hydrochloride Tiagabine Hydrochloride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是一种抗惊厥的药物，是GABA重吸收的抑制剂。
S1969	Nefiracetam Nefiracetam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。
S1332	Flumazenil Flumazenil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
S6094^New	Imidazole-4(5)-acetic Acid Hydrochloride Imidazole-4(5)-acetic Acid Hydrochloride是GABAC receptors竞争性拮抗剂。
S9249^New	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.
S9176^New	Pimpinellin Pimpinellin is a furocoumarin that acts as antagonist of proteins with GABA receptor activity.
s9065^New	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.
S5049^New	Thiocolchicoside Thiocolchicoside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。
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。	Br J Pharmacol, 2016, 173(10):1693-702 Eur J Pharmacol, 2018, 823:105-109 Sci Rep, 2016, 6: 19266	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.
S2026	Ginkgolide A Ginkgolide A是银杏的提取物，是γ-氨基丁酸(GABA)拮抗剂，K_i为14.5 μM。
S4587	Pentylenetetrazol Pentylenetetrazol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。
S4197	Bemegride Bemegride是一种中枢神经系统兴奋剂，及Barbiturate中毒的解毒剂。
S1338	Gabapentin HCl Gabapentin HCl是一种GABA类似物。
S1329	Etomidate Etomidate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。
S5612^New	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。
S4840^New	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。
S4892	Phenibut Phenibut，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。
S3072	(R)-baclofen (R)-baclofen是一种γ-氨基丁酸衍生物，主要用于治疗痉挛。
S4574	Piperazine Piperazine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。
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。
S2269	Baicalin Baicalin 是一种脯氨酰肽链内切酶抑制剂，影响GABA受体。	J Nutr Biochem, 2013, 24(11):1953-62
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 是具有良好性能的天然抗氧化剂。	Food Chem Toxicol, 2012, 50(7):2508-14 Fundam Clin Pharmacol, 2016, 30(6):596-606 Oncotarget, 2016, 10.18632/oncotarget.10836	A. Cal27 cells transfected with GFP-LC3 plasmid were treated with different concentration of DHM for 24 h. The formation of GFP-LC3 puncta were examined using immunofluorescence and quantified. Scale bar 50 μm.
S3663	Afloqualone Afloqualone (AFQ) 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，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) γ-氨基丁酸(GABA)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。
S5805^New	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。
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.

产品目录	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。	Nat Biotechnol, 2015, 10.1038/nbt.3130 J Neurosci, 2013, 33(17):7535-47 Cell Death Dis, 2016, 7:e2221	(A,B) Wild-type C57BL/6 male mice were treated with vehicle (saline) or 10 mg/kg of paraquat (PQ) for 3 days, and mice received VPA (3.5 mg/kg) or anacardic acid (5 mg/kg) starting 24 and 1 h before PQ injection. IL-6 mRNA expression was determined by real-time PCR.
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。
S4661	Tiagabine hydrochloride Tiagabine Hydrochloride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是一种抗惊厥的药物，是GABA重吸收的抑制剂。

产品目录	产品描述	文献引用	实验数据
S1969	Nefiracetam Nefiracetam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。

产品目录

产品描述

文献引用

实验数据

S1969

Nefiracetam

Nefiracetam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。

产品目录	产品描述	文献引用	实验数据
S1332	Flumazenil Flumazenil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
S6094^New	Imidazole-4(5)-acetic Acid Hydrochloride Imidazole-4(5)-acetic Acid Hydrochloride是GABAC receptors竞争性拮抗剂。
S9249^New	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.
S9176^New	Pimpinellin Pimpinellin is a furocoumarin that acts as antagonist of proteins with GABA receptor activity.
s9065^New	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.
S5049^New	Thiocolchicoside Thiocolchicoside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。
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。	Br J Pharmacol, 2016, 173(10):1693-702 Eur J Pharmacol, 2018, 823:105-109 Sci Rep, 2016, 6: 19266	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.
S2026	Ginkgolide A Ginkgolide A是银杏的提取物，是γ-氨基丁酸(GABA)拮抗剂，K_i为14.5 μM。
S4587	Pentylenetetrazol Pentylenetetrazol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。
S4197	Bemegride Bemegride是一种中枢神经系统兴奋剂，及Barbiturate中毒的解毒剂。

产品目录	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。
S5612^New	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。
S4840^New	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。
S4892	Phenibut Phenibut，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。
S3072	(R)-baclofen (R)-baclofen是一种γ-氨基丁酸衍生物，主要用于治疗痉挛。
S4574	Piperazine Piperazine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。
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。
S2269	Baicalin Baicalin 是一种脯氨酰肽链内切酶抑制剂，影响GABA受体。	J Nutr Biochem, 2013, 24(11):1953-62
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 是具有良好性能的天然抗氧化剂。	Food Chem Toxicol, 2012, 50(7):2508-14 Fundam Clin Pharmacol, 2016, 30(6):596-606 Oncotarget, 2016, 10.18632/oncotarget.10836	A. Cal27 cells transfected with GFP-LC3 plasmid were treated with different concentration of DHM for 24 h. The formation of GFP-LC3 puncta were examined using immunofluorescence and quantified. Scale bar 50 μm.
S3663	Afloqualone Afloqualone (AFQ) 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，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) γ-氨基丁酸(GABA)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。

产品目录	产品描述	文献引用	实验数据
S5805^New	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。
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.

产品目录

产品描述

文献引用

实验数据

S5805^New

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。

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.

研究领域

产品类型

GABA Receptor

信号通路图

研究领域

特异性亚型抑制剂

GABA Receptor产品