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Search Results for " gaba-in-1 "

28

抑制剂 & 化合物

2

天然产物

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同位素

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Cat. No.	Product Name	Target	Signaling Pathways
T82356	GABA-IN-1
	GABA-IN-1 (Compound 6)为GABA抑制剂，具备显著的杀幼虫效能与杀虫功能，在浓度为50 mg/L时，致死率达93%。
T62185	GABA-AT-IN-1
	GABA-AT-IN-1 (Compound 6) 是一种能够透过血脑屏障的 γ-氨基丁酸转氨酶（GABA-AT）抑制剂。GABA-AT-IN-1 可以明显增加小鼠大脑 GABA 水平，能够用作抗惊厥药物。
T12930	SKF89976A hydrochloride d,l-SKF89976A hydrochloride	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	SKF89976A hydrochloride (d,l-SKF89976A hydrochloride) 是GABA 转运蛋白GAT-1的选择性抑制剂，抑制 CHO 细胞中的 GAT-1，GAT-2 和 GAT-3，IC50分别为 0.28 μM，137.34 μM 和 202.8 μM。
T37190	L-Allylglycine	Dehydrogenase; GABA Receptor	Membrane transporter/Ion channel; Metabolism; Neuroscience
	L-Allylglycine 是 GABA 合成酶（谷氨酸脱羧酶）的有效抑制剂。
T4440	Saclofen	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	Saclofen 是竞争性GABAB 受体拮抗剂(IC50:7.8 μM)。它可研究 GABAB 受体调节大脑中缓慢抑制性突触后电位的功能。
T36520	COR659	Cannabinoid Receptor; GABA Receptor	GPCR/G Protein; Membrane transporter/Ion channel; Neuroscience
	COR659 是一种有效的 GABAB 的阳性变构调节剂。COR659具有缓解大鼠对酒精和巧克力成瘾的作用。
T38192	Unifiram	Others	Others
	Unifiram 是一种认知增强剂。 Unifiram 诱导大鼠海马 CA1 区场兴奋性突触后电位 (fEPSP) 幅度的持久增加 (EC50= 27 nM) 并增加大鼠大脑皮层中乙酰胆碱 (ACh) 的释放。
T82355	GABA-IN-2
	GABA-IN-2 (Compound 5) 为GABA抑制剂，展现出杀幼虫效果和显著的杀虫能力，在浓度50 mg/L下的死亡率达到87%。
T61319	Onfasprodil
	Onfasprodil, a negative allosteric modulator of NR2B, has been identified as a potential compound for researching Alzheimer's disease. This compound, in combination with a GABA receptor regulator.[1]
T78111	NCS-382 sodium	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	NCS-382 (sodium) 为一种高效GABA受体拮抗剂，具备抗镇静及抗催眠特性，适用于神经系统疾病研究。
T70414	NNC-711
	NNC-711 is a potent and selective inhibitor of GABA uptake by GAT-1 (IC50 values are 0.04, 171, 1700 and 622 μM for hGAT-1, rGAT-2, hGAT-3 and hBGT-1 respectively). NNC-711 is anticonvulsant following systemic administration in vivo.
T79399	E2730	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	E2730是一种针对γ-氨基丁酸(GABA)转运蛋白1(GAT1)的非竞争性选择性抑制剂，它能口服有效且有抗癫痫的作用。这种化合物能够随着环境中GABA水平的增加而增强其抑制GAT1的活性，从而有选择性地抑制GABA的回收。在实验模型中，E2730 (剂量范围为5-50 mg/kg; 经口给药) 在大鼠杏仁核点燃模型和小鼠的多种癫痫模型中，包括角膜点燃 (5-50 mg/kg)、耐药的6Hz-44mA精神运动癫痫 (5-50 mg/kg)、脆性X综合征 (2.5-300 mg/kg) 及Dravet综合征模型 (10 mg/kg, 20 mg/kg)，展现了显著的体内活性。
T60842	GABAA receptor agonist 1
	GABAA receptor agonist 1 (compound 3e) 是有效的 GABAA 受体激动剂，它结合在GABAA 受体的 GABAA 结合位点结合以产生 GABA 能效应。GABAA receptor agonist 1 在 FST 和 TST 抑郁症的经典小鼠模型中具有抗抑郁活性，在抑郁症研究中具有潜力。
T37194	5α-Androst-16-en-3α-ol
	5α-Androst-16-en-3α-ol is a steroid pheromone that has been found in boar testes and human male axillary sweat and has diverse biological activities.1,2It enhances GABA-activated currents in primary mouse cerebellar granule cells (EC50= 0.4 μM).25α-Androst-16-en-3α-ol (0.1-1 μM) increases the amplitude of GABA-activated currents in HEK293 cells expressing human α1β2γ2and α2β2γ2subunit-containing GABAAreceptors.In vivo, 5α-androst-16-en-3α-ol (5-10 mg/kg) decreases immobility time in the forced s...
T37201	CAY10787
	CAY10787 is an oxysterol and a negative allosteric modulator of GABAAreceptors.1,2It reduces GABA-induced currents in HEK cells expressing α1β1γ2or α4β3γ2subunit-containing GABAAreceptors (IC50s = 1.5 and 1 μM, respectively).2CAY10787 (500 nM) reduces GABA-induced depolarization of peptidergic and non-peptidergic nociceptors, C-LTMRs, and cold thermosensors in isolated mouse dorsal root ganglion (DRG) neurons.In vivo, CAY10787 (2, 10, and 50 mg/kg) increases latency to nocifensive behaviors in t...
T73818	Homocarnosine TFA
	Homocarnosine TFA, 作为一种大脑特定的γ-氨基丁酸(GABA)与组氨酸的二肽, 具备抑制性神经调节功能。它在神经元内由GABA合成，既显示出抗惊厥效应，也表现抗氧化、抗炎作用，能防止DNA损伤并抑制晚期糖基化终产物的形成。
T61625	GABAA receptor agonist 2
	GABAA receptor agonist 2 (compound 4c) is a highly potent GABAA receptor agonist which exhibits anti-depressive properties in classical mouse models of depression, such as the FST and TST. By binding to the GABA binding site on the GABAA receptor, GABAA receptor agonist 2 produces GABAergic effects. Notably, Compound 4c holds promise for depression research [1].
T84878	CGP36216 hydrochloride
	CGP36216 hydrochloride是选择性GABA突触前受体拮抗剂，其Ki值与GABAB受体结合为0.3μM。适用于焦虑及创伤相关障碍研究。
T72215	Lesogaberan hydrochloride AZD-3355 hydrochloride
	Lesogaberan (AZD-3355) hydrochloride 是一种有效的选择性 GABAB 受体激动剂，对人重组 GABAB 受体的 EC50为 8.6 nM。通过脑膜中 [3H]GABA 结合位移测量，Lesogaberan hydrochloride 对大鼠 GABAB 和 GABAA 受体的亲和力 (Kis)：分别为 5.1 nM 和 1.4 μM。Lesogaberan hydrochloride 通过外周作用模式抑制短暂的食管下括约肌松弛。
T68550	SKF89976A HCl
	SKF89976A is a potent GABA uptake inhibitor, which is selective for GAT-1 (IC50 values are 0.13, 550, 944 and 7210 μM for hGAT-1, rGAT-2, hGAT-3 and hBGT-1 respectively). SKF89976A inhibits transport current competitively (Ki = 7 μM) and transmitter-gated current non-competitively (Ki = 0.03 nM). It is able to pass the blood-brain barrier after systemic administration and is active in vivo.
T37388	Afizagabar
	Afizagabar (S44819) is a first-in-class, competitive, and selective antagonist at the GABA-binding site of the α5-GABAAR, with an IC50 of 585 nM for α5β2γ2 and a Ki of 66 nM for α5β3γ2. Afizagabar enhances hippocampal synaptic plasticity and exhibits pro-cognitive efficacy[1]. Afizagabar (S44819) is a competitive α5-GABAAR antagonist (Kb=221 nM). Afizagabar selectively inhibits extrasynaptic α5-GABAARs of mouse CA1 pyramidal neurons[1]. Afizagabar (1 and 3 mg/kg; i.p.) significantly diminishes t...
T80218	GAD65(247-266) epitope TFA	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	GAD65(247-266) epitope TFA 为T细胞表位，与I-Ag7（I型糖尿病相关分子）竞争性结合，亲和力较低。该表位源自胰岛抗原，GAD65 是谷氨酸脱羧酶 65，涉及将谷氨酸转换为γ-氨基丁酸（GABA）。
T70292	DDPM-2571 HCl
	DDPM-2571 is a highly potent and in vivo active inhibitor of GABA transporter subtype 1 with anticonvulsant, anxiolytic, antidepressant and antinociceptive properties. DDPM-2571 was quickly distributed into the brain and was highly effective in the prevention of chemically-induced seizures (pentylenetetrazole and pilocarpine models) and 6-Hz convulsions. It demonstrated significant anxiolytic-like and antidepressant-like properties. DDPM-2571 had antinociceptive properties, both in the hot plate...
T37699	Org 24598
	Potent and selective inhibitor of the glial glycine transporter GlyT1b (IC50 = 6.9 nM). Displays negligible activity at GlyT-2, adrenoreceptors, dopamine, 5HT receptors and noradrenaline, dopamine, 5HT and GABA transporters (pIC50 in vivo. Chue et al (2013) Glycine reuptake inhibition as a new therapeutic approach in schizophrenia: focus on the glycine transporter 1 (GlyT1). Curr.Pharm.Des. 19 1311 PMID:23194655 \|Brown et al (2001) Discovery and SAR of org 24598-a selective glycine uptake inhibi...
T79423	BuChE-IN-9
	BuChE-IN-9 (compound 22a) 作为eqBuChE的抑制剂，表现出相当的效力，具有173 nM的IC50值。除此之外，BuChE-IN-9对人BACE1、Aβ聚集及小鼠mGAT1和mGAT4也具有抑制作用，并且显示出显著的抗遗忘特性。
T80487	MmTx2 toxin Micrurotoxin 2	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	MmTx2 toxin作为一种GABAA受体调节剂，具有提升GABAA受体对激动剂反应敏感性的作用。该毒素来源于珊瑚蛇的毒液，并在神经系统相关疾病（例如癫痫、精神分裂症及慢性疼痛）的研究中发挥重要用途。
T36521	Alaproclate (hydrochloride)
	Alaproclate is a selective serotonin reuptake inhibitor (SSRI).1,2 It inhibits depletion of serotonin (5-HT) induced by 4-methyl-α-ethyl-m-tyramine in rat cerebral cortex, hippocampus, hypothalamus, and striatum (EC50s = 18, 4, 8, and 12 mg/kg, respectively).1 Alaproclate inhibits NMDA-evoked currents and depolarization-induced voltage-dependent potassium currents in rat hippocampal neurons (IC50s = 1.1 and 6.9 μM, respectively) and does not inhibit GABA-evoked currents when used at concentratio...
T65396	Piperazine 2HCl
	Piperazine (2HCl) is gamma-aminobutyric acid (GABA) agonists and its major effects appear to be on the central nervous system. Piperazine was the anthelmintic with the greatest number of reports of toxicoses and suspected toxicoses in cats. Piperazine neurotoxicity in cats and dogs usually was manifested by muscle tremors, ataxia, and/or behavioral disturbances within 24 hours after estimated daily dose(s) between 20 and 110 mg/kg[1]. For di-substituted derivatives, ciprofloxacin was selected an...

化合物

Cat.No: T82356

Cat.No: T62185

SKF89976A hydrochloride

Cat.No: T12930

Synonym: d,l-SKF89976A hydrochloride

Target: GABA Receptor

Cat.No: T37190

Target: Dehydrogenase, GABA Receptor

Cat.No: T4440

Target: GABA Receptor

Cat.No: T36520

Target: Cannabinoid Receptor, GABA Receptor

Cat.No: T38192

Target: Others

Cat.No: T82355

Cat.No: T61319

Cat.No: T78111

Target: GABA Receptor

Cat.No: T70414

Cat.No: T79399

Target: GABA Receptor

GABAA receptor agonist 1

Cat.No: T60842

5α-Androst-16-en-3α-ol

Cat.No: T37194

Cat.No: T37201

Homocarnosine TFA

Cat.No: T73818

GABAA receptor agonist 2

Cat.No: T61625

CGP36216 hydrochloride

Cat.No: T84878

Lesogaberan hydrochloride

Cat.No: T72215

Synonym: AZD-3355 hydrochloride

Cat.No: T68550

Cat.No: T37388

GAD65(247-266) epitope TFA

Cat.No: T80218

Target: GABA Receptor

Cat.No: T70292

Cat.No: T37699

Cat.No: T79423

Cat.No: T80487

Synonym: Micrurotoxin 2

Target: GABA Receptor

Alaproclate (hydrochloride)

Cat.No: T36521

Piperazine 2HCl

Cat.No: T65396

Cat. No.	Product Name	Target	Signaling Pathways
T5089	5-Aminovaleric acid	Others; Endogenous Metabolite	Metabolism; Others
	5-Aminovaleric acid 被认为是 GABA 的亚甲基同系物，是GABA 的弱激动剂。它是赖氨酸降解产物。它既能够内源性产生，也能够通过赖氨酸的细菌分解代谢产生。
T3S2259	Methyl eugenol 4-allylveratrole,eugenyl methyl ether,O-methyleugenol,Eugenol Methyl ether,丁香酚甲醚,丁子香酚甲醚	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	Methyl eugenol (4-allylveratrole) 是一种苯丙类化合物，存在于植物叶子、果实、根茎中，当植物相应的部位因食草动物进食而受损时，就会释放。它可用于消灭雄性东方果蝇。

天然产物

5-Aminovaleric acid

Cat.No: T5089

Target: Others, Endogenous Metabolite

Cat.No: T3S2259

Synonym: 4-allylveratrole,eugenyl methyl ether,O-methyleugenol,Eugenol Methyl ether,丁香酚甲醚,丁子香酚甲醚

Target: GABA Receptor

Cat. No.	Product Name	Target	Signaling Pathways
T71206	Tiagabine-d6 hydrochloride
	Tiagabine-d6 is intended for use as an internal standard for the quantification of tiagabine by GC- or LC-MS. Tiagabine is an inhibitor of GABA transporter 1. It inhibits seizures induced by DMCM in mice. Tiagabine reduces allodynia in a rodent model of neuropathic pain when used at a dose of 72.8 µmol/kg, and it acts synergistically with gabapentin to delay pain responses in mice in the hot plate test. Formulations containing tiagabine have been used as adjunctive therapies in the treatment of ...

同位素

Tiagabine-d6 hydrochloride

Cat.No: T71206

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