GABA Receptor

信号通路图

GABA Receptor信号通路图

GABA Receptor产品

  • 所有产品(62)
  • GABA Receptor抑制剂 (11)
  • GABA Receptor抗体 (2)
  • GABA Receptor激活剂 (7)
  • GABA Receptor拮抗剂 (14)
  • GABA Receptor激动剂 (14)
  • GABA Receptor调节剂 (12)
目录号 产品名 产品描述 文献引用 实验数据
S1168 Valproic Acid sodium Valproic Acid sodium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。
Sci Total Environ, 2022, 838(Pt 2):155825
Acta Pharmacol Sin, 2022, 10.1038/s41401-022-00932-4
Transl Psychiatry, 2022, 12(1):130
S7071 (+)-Bicuculline (+)-Bicuculline (d-Bicuculline)是一种竞争性GABAA受体拮抗剂,IC50为2 μM,也抑制Ca(2+)激活的钾离子通道。
Research Square, 2024, 10.21203/rs.3.rs-3480364/v1
J Exp Med, 2022, 219-12e20220541
Acta Pharmacol Sin, 2022, 10.1038/s41401-021-00854-7
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。
Adv Sci (Weinh), 2023, 10(3):e2203718
iScience, 2022, 25-9:104952
Adv Sci (Weinh), 2021, e2004846
S2399 Dihydromyricetin Dihydromyricetin (Ampelopsin, Ampeloptin)是具有良好性能的天然抗氧化剂。
Front Pharmacol, 2022, 13:932092
Molecules, 2021, 26(5)1210
Cell Signal, 2020, 65:109431
S2133 Gabapentin Gabapentin 是一种GABA类似物,用于治疗癫痫及神经痛。
Mol Oncol, 2022, 10.1002/1878-0261.13281
Mol Pharmacol, 2022, 101(4):236-245
Cell Death Dis, 2020, 11(9):764
S1332 Flumazenil Flumazenil 是一种苯二氮卓类拮抗剂。
J Exp Med, 2022, 219-12e20220541
Biomed Pharmacother, 2018, 107:1674-1681
Holist Nurs Pract, 2017, 31(3):193-203
S1338 Gabapentin HCl Gabapentin HCl(Neurontin HCl)是一种GABA类似物。
Mol Pharmacol, 2022, 101(4):236-245
Int J Clin Exp Pathol, 2018, 11(12):5536-5546
J Aging Sci, 2017, 5:1
S0303 CGP52432 CGP52432 是一种有效的 GABAB autoreceptor 的选择性拮抗剂,其IC50值为0.085 μM。
Research Square, 2024, 10.21203/rs.3.rs-3480364/v1
J Cell Biochem, 2022, 10.1002/jcb.30231
Front Neurosci, 2021, 15:741214
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。
J Cell Biochem, 2022, 10.1002/jcb.30231
S3018 Niflumic acid Niflumic acid(Nifluril)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
S2026 Ginkgolide A Ginkgolide A (BN52020) 是银杏的提取物,是γ-氨基丁酸(GABA)拮抗剂,Ki为14.5 μM。
Cell Rep, 2020, 21;31(3):107521
S5194 Furosemide sodium Furosemide (Frusemide) sodium 是一种有效的、口服活性的 Na-K-Cl cotransporter (NKCC) 的抑制剂。Furosemide sodium 是一种 gamma-aminobutyric acid type A (GABAA) receptor 的亚型选择性拮抗剂。
Ren Fail, 2022, 44(1):1345-1355
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
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。
Theranostics, 2023, 13(4):1355-1369
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。
E1247 SR95531 Gabazine(SR95531)是一种有效的GABAA受体竞争性变构拮抗剂,对GABA受体的IC50为9 µM。
A5209 GABARAP Rabbit Recombinant mAb
E3045 Chinese Arborvilea Seed Extract Chinese Arborvilea Seed Extract提取自侧柏Platycladus orientalis (L.)Franco的干燥成熟种仁,具有明显的抗焦虑作用,其作用机制可能与增加海马组织γ-氨基丁酸(GABA)的水平和降低谷氨酸(Glu)的水平有关。
A5210 GABARAPL2 Rabbit Recombinant mAb
E2848 Afoxolaner Afoxolaner (NexGard)是一种来自异恶唑啉家族的新型杀虫剂/杀螨剂分子,作用于昆虫γ-氨基丁酸受体(gamma-aminobutyric acid receptor, GABA)和谷氨酸受体,抑制GABA和谷氨酸调节的氯离子摄取, 导致节肢动物的神经元过度刺激和死亡。
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.
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.
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。
S2996 L-DAB HBR L-DAB HBR (L-Dab Hydrobromide, L-2,4-Diaminobutyric acid hydrobromide) 是一种 GABA (Gamma-aminobutyric acid) transaminase 的抑制剂,IC50值大于500 μM。L-DAB HBR 表现出抗肿瘤活性。
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。
E2354 Valepotriate Valepotriate从Valeriana jatamansi Jones中分离一种不稳定的环烯醚萜,通过显著增加GABAA、谷氨酸脱羧酶65 (glutamic acid decarboxylase 65)和Bcl-2的表达,以及降低caspase-3表达发挥抗癫痫作用。
S0049 Zuranolone (SAGE-217) Zuranolone(SAGE-217, CS-2797)是一种有效的神经活性类固醇,是GABAA受体的正向变构调节剂,对α1β2γ2受体的EC50为296 nM。
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.
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.
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。
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。
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。
Cell Mol Life Sci, 2024, 81(1):104
E3607 Crateva nurvala Extract Crateva Nurvala Extract来源于沙梨木Crataeva nurvala Buch. 的树皮。沙梨木是一种重要的药用植物,其茎皮部分主要用于阻塞性和非阻塞性尿路病的研究。沙梨木也用于治疗前列腺肿大和恢复膀胱敏感性。
E0599 Arecaidine hydrochloride Arecaidine hydrochloride是槟榔果(Areca catechu)的一种成分,可抑制GABA和β-丙氨酸的吸收,但不抑制甘氨酸的吸收。
E0101 AZD6280 AZD6280是一种选择性γ-氨基丁酸(gamma-aminobutyric acid, GABAA) (α2/3)受体调节剂,用于泛化性焦虑症(generalized anxiety disorder, GAD)的治疗。
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。
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。
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.
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。
S6008 p-Hydroxybenzaldehyde p-Hydroxybenzaldehyde (4-Hydroxybenzaldehyde, 4-Formylphenol, p-Formylphenol),存在于兰花Gastrodia elataGaleola 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.
S1989 GABAA receptor agent 1 GABAA receptor agent 1是γ-氨基丁酸A (Gamma-aminobutyric acid A, GABAA)受体的高亲和力配体,具有强大的抗惊厥活性。
S4197 Bemegride Bemegride(Bemegrid,3-Ethyl-3-methylglutarimide)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。
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。
S0164 AZD7325 AZD7325是一种有效且具有口服活性的部分选择性正变构调节剂(PAM),作用于GABAAα2和Aα3受体,Ki分别为0.3 和1.3 nM,对Aα1和Aα5的拮抗作用较小。
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.
S6094 Imidazole-4(5)-acetic Acid Hydrochloride Imidazole-4(5)-acetic Acid Hydrochloride是GABAC receptors竞争性拮抗剂。
E2232 Guvacine hydrochloride Guvacine hydrochloride是一种产自槟榔果的生物碱,是γ-氨基丁酸(gamma-Aminobutyric acid, GABA)转运蛋白的抑制剂,对克隆的GABA转运蛋白具有一定的选择性,IC50值分别为14 μM (human GAT-1)、39 μM (rat GAT-1)、58 μM (rat GAT-2)、119 μM (human GAT-3)、378 μM (rat GAT-3)和1870 μM (human BGT-3)。
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 Imepitoin Imepitoin(ELB-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.
S6100 Picrotoxin Picrotoxin (Picrotin, Cocculin, Cocculus, NSC 403139) 是一种植物生物碱,是神经元 GABAglycine receptors 的非竞争性拮抗剂。此产品为危化品(急性毒性/易燃/皮肤腐蚀),请在穿戴防护面罩、防护手套和防护服后使用。
S3748 Acamprosate Calcium Acamprosate (N-Acetylhomotaurine, Calcium acetylhomotaurinate,N-acetylhomotaurinate)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。
S4423 Emamectin Benzoate Emamectin Benzoate (EMB, MK-244) 激活 gamma-amino butyric acid (GABA) transporter。Emamectin Benzoate 可诱导活性氧(ROS)介导的 DNA damage 和细胞凋亡。
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)L-glutamate-gated chloride channels (GluCls)
S3977 (-)-Borneol (-)-Borneol (L-Borneol), one of enantiomers of borneol, has a camphoraceous and evident woody odor.
S4494 Methionine Methionine (MRX-1024, D-Methionine) 是 GABAA receptor 的激活剂,可调节神经元活性。
S9176 Pimpinellin Pimpinellin is a furocoumarin that acts as antagonist of proteins with GABA receptor activity.
E3508 Magnolia Obovata Extract Magnolia Obovata Extract是从木兰magnolia obovata中提取的,通过增强GABA受体和抗神经炎症机制具有抗焦虑作用。
S5612 Isonipecotic acid Isonipecotic acid (4-Piperidinecarboxylic acid, 4-Carboxypiperidine, Hexahydroisonicotinic acid)是杂环化合物,主要是作为GABAA receptor部分激动剂发挥作用。
S6755 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。
E0960 RO5186582 RO5186582 (Basmisanil, RG1662)是一种高选择性的GABAAα5负变构调节剂。
S1168 Valproic Acid sodium Valproic Acid sodium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。
Sci Total Environ, 2022, 838(Pt 2):155825
Acta Pharmacol Sin, 2022, 10.1038/s41401-022-00932-4
Transl Psychiatry, 2022, 12(1):130
S3018 Niflumic acid Niflumic acid(Nifluril)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
E1247 SR95531 Gabazine(SR95531)是一种有效的GABAA受体竞争性变构拮抗剂,对GABA受体的IC50为9 µM。
E2848 Afoxolaner Afoxolaner (NexGard)是一种来自异恶唑啉家族的新型杀虫剂/杀螨剂分子,作用于昆虫γ-氨基丁酸受体(gamma-aminobutyric acid receptor, GABA)和谷氨酸受体,抑制GABA和谷氨酸调节的氯离子摄取, 导致节肢动物的神经元过度刺激和死亡。
S2996 L-DAB HBR L-DAB HBR (L-Dab Hydrobromide, L-2,4-Diaminobutyric acid hydrobromide) 是一种 GABA (Gamma-aminobutyric acid) transaminase 的抑制剂,IC50值大于500 μM。L-DAB HBR 表现出抗肿瘤活性。
E0599 Arecaidine hydrochloride Arecaidine hydrochloride是槟榔果(Areca catechu)的一种成分,可抑制GABA和β-丙氨酸的吸收,但不抑制甘氨酸的吸收。
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。
E2232 Guvacine hydrochloride Guvacine hydrochloride是一种产自槟榔果的生物碱,是γ-氨基丁酸(gamma-Aminobutyric acid, GABA)转运蛋白的抑制剂,对克隆的GABA转运蛋白具有一定的选择性,IC50值分别为14 μM (human GAT-1)、39 μM (rat GAT-1)、58 μM (rat GAT-2)、119 μM (human GAT-3)、378 μM (rat GAT-3)和1870 μM (human BGT-3)。
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)L-glutamate-gated chloride channels (GluCls)
E3508 Magnolia Obovata Extract Magnolia Obovata Extract是从木兰magnolia obovata中提取的,通过增强GABA受体和抗神经炎症机制具有抗焦虑作用。
A5209 GABARAP Rabbit Recombinant mAb
A5210 GABARAPL2 Rabbit Recombinant mAb
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。
E3045 Chinese Arborvilea Seed Extract Chinese Arborvilea Seed Extract提取自侧柏Platycladus orientalis (L.)Franco的干燥成熟种仁,具有明显的抗焦虑作用,其作用机制可能与增加海马组织γ-氨基丁酸(GABA)的水平和降低谷氨酸(Glu)的水平有关。
E2354 Valepotriate Valepotriate从Valeriana jatamansi Jones中分离一种不稳定的环烯醚萜,通过显著增加GABAA、谷氨酸脱羧酶65 (glutamic acid decarboxylase 65)和Bcl-2的表达,以及降低caspase-3表达发挥抗癫痫作用。
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 Imepitoin Imepitoin(ELB-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.
S4423 Emamectin Benzoate Emamectin Benzoate (EMB, MK-244) 激活 gamma-amino butyric acid (GABA) transporter。Emamectin Benzoate 可诱导活性氧(ROS)介导的 DNA damage 和细胞凋亡。
S4494 Methionine Methionine (MRX-1024, D-Methionine) 是 GABAA receptor 的激活剂,可调节神经元活性。
S7071 (+)-Bicuculline (+)-Bicuculline (d-Bicuculline)是一种竞争性GABAA受体拮抗剂,IC50为2 μM,也抑制Ca(2+)激活的钾离子通道。
Research Square, 2024, 10.21203/rs.3.rs-3480364/v1
J Exp Med, 2022, 219-12e20220541
Acta Pharmacol Sin, 2022, 10.1038/s41401-021-00854-7
S1332 Flumazenil Flumazenil 是一种苯二氮卓类拮抗剂。
J Exp Med, 2022, 219-12e20220541
Biomed Pharmacother, 2018, 107:1674-1681
Holist Nurs Pract, 2017, 31(3):193-203
S0303 CGP52432 CGP52432 是一种有效的 GABAB autoreceptor 的选择性拮抗剂,其IC50值为0.085 μM。
Research Square, 2024, 10.21203/rs.3.rs-3480364/v1
J Cell Biochem, 2022, 10.1002/jcb.30231
Front Neurosci, 2021, 15:741214
S2026 Ginkgolide A Ginkgolide A (BN52020) 是银杏的提取物,是γ-氨基丁酸(GABA)拮抗剂,Ki为14.5 μM。
Cell Rep, 2020, 21;31(3):107521
S5194 Furosemide sodium Furosemide (Frusemide) sodium 是一种有效的、口服活性的 Na-K-Cl cotransporter (NKCC) 的抑制剂。Furosemide sodium 是一种 gamma-aminobutyric acid type A (GABAA) receptor 的亚型选择性拮抗剂。
Ren Fail, 2022, 44(1):1345-1355
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.
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。
Cell Mol Life Sci, 2024, 81(1):104
S6008 p-Hydroxybenzaldehyde p-Hydroxybenzaldehyde (4-Hydroxybenzaldehyde, 4-Formylphenol, p-Formylphenol),存在于兰花Gastrodia elataGaleola 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(Bemegrid,3-Ethyl-3-methylglutarimide)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。
S6100 Picrotoxin Picrotoxin (Picrotin, Cocculin, Cocculus, NSC 403139) 是一种植物生物碱,是神经元 GABAglycine receptors 的非竞争性拮抗剂。此产品为危化品(急性毒性/易燃/皮肤腐蚀),请在穿戴防护面罩、防护手套和防护服后使用。
S9176 Pimpinellin Pimpinellin is a furocoumarin that acts as antagonist of proteins with GABA receptor activity.
S2399 Dihydromyricetin Dihydromyricetin (Ampelopsin, Ampeloptin)是具有良好性能的天然抗氧化剂。
Front Pharmacol, 2022, 13:932092
Molecules, 2021, 26(5)1210
Cell Signal, 2020, 65:109431
S2133 Gabapentin Gabapentin 是一种GABA类似物,用于治疗癫痫及神经痛。
Mol Oncol, 2022, 10.1002/1878-0261.13281
Mol Pharmacol, 2022, 101(4):236-245
Cell Death Dis, 2020, 11(9):764
S1338 Gabapentin HCl Gabapentin HCl(Neurontin HCl)是一种GABA类似物。
Mol Pharmacol, 2022, 101(4):236-245
Int J Clin Exp Pathol, 2018, 11(12):5536-5546
J Aging Sci, 2017, 5:1
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。
J Cell Biochem, 2022, 10.1002/jcb.30231
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
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。
Theranostics, 2023, 13(4):1355-1369
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。
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。
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。
S3748 Acamprosate Calcium Acamprosate (N-Acetylhomotaurine, Calcium acetylhomotaurinate,N-acetylhomotaurinate)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 (4-Piperidinecarboxylic acid, 4-Carboxypiperidine, Hexahydroisonicotinic acid)是杂环化合物,主要是作为GABAA receptor部分激动剂发挥作用。
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。
Adv Sci (Weinh), 2023, 10(3):e2203718
iScience, 2022, 25-9:104952
Adv Sci (Weinh), 2021, e2004846
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.
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.
S0049 Zuranolone (SAGE-217) Zuranolone(SAGE-217, CS-2797)是一种有效的神经活性类固醇,是GABAA受体的正向变构调节剂,对α1β2γ2受体的EC50为296 nM。
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。
E0101 AZD6280 AZD6280是一种选择性γ-氨基丁酸(gamma-aminobutyric acid, GABAA) (α2/3)受体调节剂,用于泛化性焦虑症(generalized anxiety disorder, GAD)的治疗。
S0164 AZD7325 AZD7325是一种有效且具有口服活性的部分选择性正变构调节剂(PAM),作用于GABAAα2和Aα3受体,Ki分别为0.3 和1.3 nM,对Aα1和Aα5的拮抗作用较小。
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.
S6755 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。
E0960 RO5186582 RO5186582 (Basmisanil, RG1662)是一种高选择性的GABAAα5负变构调节剂。

GABA Receptor抑制剂选择性比较

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
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