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54

抑制剂 & 化合物

6

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T23513	VU10010 VU 10010	AChR	Neuroscience
	VU10010 (VU 10010) 是一种高度选择性的M4mAChR 变构增强剂，EC50为 400 nM。它与 M4mAChR 的变构位点结合，增强与 G 蛋白偶联，增加对乙酰胆碱的亲和力，还会增加卡巴胆碱引起的兴奋性传导抑制。
T3478	Ro 67-7476	GluR	Neuroscience
	Ro 67-7476 是mGluR1的正变位调节剂，能增强表达 rat mGluR1a 的 HEK293 细胞中谷氨酸诱导的钙释放，EC50为 60.1 nM。它是 P-ERK1/2 激动剂，可以在外源添加谷氨酸的情况下激活 ERK1/2 磷酸化 (EC50=163.3 nM)。
T7823	IDRA-21 7-氯-3-甲基-3,4-二氢-2H-1,2,4-苯并噻二嗪 1,1-二氧化物	GluR	Neuroscience
	IDRA-21 是一种阳性 AMPA 受体调节剂。
T9347	EAAT2 activator 1 3-[(2-Chloro-6-fluorobenzyl)thio]-6-pyridin-2-ylpyridazine	transporter	Metabolism
	EAAT2 activator 1 (3-[(2-Chloro-6-fluorobenzyl)thio]-6-pyridin-2-ylpyridazine) 是兴奋性氨基酸转运蛋白 2(EAAT2) 的有效激活剂，以剂量依赖性方式增加 EAAT2 蛋白水平。
T15728	LDN-212320 LDN-0212320,LDN/OSU-0212320,OSU-0212320	transporter	Metabolism
	LDN-212320 (OSU-0212320) 是兴奋性氨基酸转运体 2(EAAT2)/谷氨酸转运体(GLT-1)的激活剂。它通过上调海马和 ACC 星形胶质细胞 GLT-1 的水平来预防伤害性疼痛。
T82778	Cardioexcitatory peptide 1
	Cardioexcitatory peptide 1为从非洲大蜗牛(Achatina)心房分离的心兴奋性神经肽。该化合物对心脏具有显著的兴奋效应，并能影响肌肉组织的运动及神经活动。
T15446	GT 949	transporter	Metabolism
	GT 949 是氨基酸转运蛋白 2 (EAAT2) 的选择性兴奋性正变构调节剂 (EC50：0.26 nM)。
T4138	UCPH-101 UCPH 101	transporter	Metabolism
	UCPH-101 是一种兴奋性氨基酸转运子亚型 1 (EAAT1) 的抑制剂(IC50:0.66 μM)。
T0313	Evans blue Direct Blue 53,C.I. 23860,伊文思蓝	GluR	Neuroscience
	Evans blue (C.I. 23860) 是一种突触泡谷氨酸吸收的有效抑制剂，同时也是一种AMPA/kainate 受体拮抗剂。
T7401	(S)-3-AMino-2-Methylpropanoic acid-HCl	Others	Others
	(S)-3-AMino-2-Methylpropanoic acid-HCl 是一种氨基酸衍生物，是兴奋性神经递质谷氨酸的激动剂，影响神经系统。
TP2054L	Calcineurin Autoinhibitory Peptide acetate	Phosphatase	Metabolism
	Calcineurin Autoinhibitory Peptide acetate 是一种选择性的钙调磷酸酶抑制剂 (IC50 ~ 10 μM)。它可用于保护神经元免受兴奋性神经元死亡。
T76815	Lexatumumab ETR2-ST01,DR5 mAB,HGS-ETR 2	Apoptosis	Apoptosis
	Lexatumumab (HGS-ETR 2) 是一种靶向 TRAIL 受体 2 的人激动性单克隆抗体，具有抗癌活性，在恶性间皮瘤中诱导细胞凋亡 (apoptosis)。Lexatumumab 可用于研究恶性胸膜间皮瘤 (MPM)。
T22833	H-9 dihydrochloride	EGFR; 5-HT Receptor; PKA	Angiogenesis; GPCR/G Protein; JAK/STAT signaling; Neuroscience; Tyrosine Kinase/Adaptors
	H-9 dihydrochloride 是一种具有有效性的蛋白激酶（ PKA）抑制剂。H-9 Dihydrochloride 在低浓度下显著降低 5-HT 的兴奋性反应。H-9 Dihydrochloride 会对咽部活动产生影响。H-9 Dihydrochloride 对 EGF (表皮生长因子)依赖的上皮细胞系的信号转导和细胞生长有抑制作用。
T10893	CS-722 Free base	Others	Others
	CS-722 Free base是一种合成的中枢作用肌肉松弛剂，它展现出肌肉松弛效果并抑制脊髓反射。可能通过限制钠和钙流动，从而在海马培养物中减少自发的抑制性和兴奋性突触后电流。
T1065	Baclofen 巴氯芬,Lioresal	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	Baclofen (Lioresal) 是 γ-氨基丁酸 (GABA) 的亲脂性衍生物，是可口服的选择性代谢型 GABA-B 受体激动剂，具有高血脑屏障渗透率，用于治疗因脊髓损伤和多发性硬化引起的痉挛。
T25853	NBQX Disodium FG9202 disodium,NBQX 2Na	GluR	Neuroscience
	NBQX Disodium (FG9202 disodium) 是高度选择性，竞争型的 AMPA 受体拮抗剂，具有保护神经系统和抗惊厥活性的作用。NBQX Disodium 是NBQX 的盐类物质。 NBQX 是一种有效并具有选择性的AMPA /红藻氨酸受体拮抗剂，可用于拮抗谷氨酸的兴奋性毒性。在啮齿类动物模型中具有抗惊厥作用。
T8630	Baclofen hydrochloride 4-amino-3-(4-chlorophenyl)butanoic acid hydron chloride	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	Baclofen hydrochloride (4-amino-3-(4-chlorophenyl)butanoic acid hydron chloride) 是一种 GAMMA-AMINOBUTYRIC ACID 衍生物，是一种特异性 GABA-B 受体激动剂。它用于治疗肌肉痉挛，尤其是由于脊髓损伤引起的肌肉痉挛。其治疗效果来自于脊髓和脊髓上部位的作用，通常是减少兴奋性传递。
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。
T0267	Zonisamide AD 810,唑尼沙胺,CI 912	Calcium Channel; Sodium Channel; Carbonic Anhydrase	Membrane transporter/Ion channel; Metabolism
	Zonisamide (AD 810) 是锌酶碳酸酐酶 (carbonic anhydrase) 的有效抑制剂，对人类线粒体同工酶 hCA II 和 hCA V 作用的 Ki 值分别为 35.2 nM 和 20.6 nM。Zonisamide 具有抗癫痫活性，在癫痫、癫痫发作和帕金森病的研究中具有价值。
T22704	D-AP4	Others	Others
	broad spectrum excitatory amino acid receptor antagonist
T22479	(±)-HIP-A	Others	Others
	(±)-HIP-A is an excitatory amino acid transporter blocker.
T23864	CCPG (alpha-Carboxycyclopropyl)glycine,L-Ccg-I
	CCPG is an agonist of excitatory Amino Acid.
T71829	NSC-119128
	NSC-119128 is an excitatory amino acid transporter (EAAT) inhibitor.
T22480	(±)-HIP-B	Others	Others
	(±)-HIP-B is an excitatory amino acid transporter blocker.
T23037	N-Acetylglycyl-D-glutamic acid	Others	Others
	Excitatory peptide that induces seizures
T24074	Fropofol
	Fropofol is a potent ligand for a protein site governed largely. It producing excitatory activity in tadpoles and mice.
T40973	MDNI-caged-L-glutamate MDNI-caged-L-glutamate,MDNI-glu
	MDNI-glu is a photosensitive derivative of L-glutamate, a major excitatory amino acid, that is biologically inert. It demonstrates improved utilization of incident light.
T23930	Cysteic acid, L- NSC254030,L-Cysteic acid,Cysteinic acid,NSC 254030,NSC-254030
	L-Cysteic acid is a useful agonist at several rat metabotropic glutamate receptors. L-Cysteic acid is an analogue of cysteine sulfinic acid, may be used in studies of excitatory amino acids in the brain.
T17306	(R)-Baclofen hydrochloride Arbaclofen hydrochloride,(R)-巴氯芬盐酸盐	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	Arbaclofen hydrochloride, a Gamma-Aminobutyric Acid derivative, is a specific agonist of GABA-B receptors, it is used to treat spasticity, especially that due to spinal cord damage. It acts at spinal and supraspinal sites, generally reduces excitatory tra
T33653	Neurokinin A (4-10), nle(10)- 10-Nle-neurokinin A (4-10)
	Neurokinin A (4-10), nle(10)- is a neurologically active peptide translated from the pre-protachykinin gene. Neurokinin A has many excitatory effects on mammalian nervous systems and on the mammalian inflammatory and pain responses.
T39510	DL-TBOA ammonium
	DL-TBOA ammonium is a potent, non-transportable inhibitor of excitatory amino acid transporters. Its inhibitory effects are demonstrated by IC50 values of 70 μM, 6 μM, and 6 μM for excitatory amino acid transporter-1 (EAAT1), EAAT2, and EAAT3, respectively. Additionally, DL-TBOA ammonium significantly hampers the uptake of [14C]glutamate in COS-1 cell lines expressing human EAAT1 and EAAT2, evident by Ki values of 42 μM and 5.7 μM, respectively. Furthermore, this compound competitively blocks EA...
T69017	Ibotenic acid hydrate
	Ibotenic acid hydrate is a neurotoxic isoxazole (similar to Kainic acid and Muscimol) found in Amanita mushrooms. It causes motor depression, ataxia, and changes in mood, perceptions and feelings, and is a potent excitatory amino acid agonist.
T11055	DL-TBOA	transporter	Metabolism
	DL-TBOA inhibited [14C] glutamate uptake in COS-1 cells expressing human EAAT1 and EAAT2, with Ki values of 42 μM and 5.7 μM, respectively. DL-TBOA blocks EAAT4 and EAAT5 in a competitive manner, with Ki values of 4.4 μM and 3.2 μM, respectively. DL-TBOA
T39565	L-Glutamic acid-15N
	L-Glutamic acid-15N is the 15N-labeled version of L-Glutamic acid, an excitatory neurotransmitter and an agonist at metabotropic, kainate, NMDA, and AMPA glutamate receptor subtypes. It directly activates the release of dopamine (DA) from dopaminergic terminals.
TP1819	Substance P (1-9)
	Substance P (1-9) is nonapeptide, which decreases the inactivation of substance P by the guinea-pig ileum and urinary bladder. Subtance P is responsible for a number of excitatory effects on both central and peripheral neurons.
T16800	(RS)-AMPA (±)-AMPA	iGluR	Membrane transporter/Ion channel; Neuroscience
	(RS)-AMPA ((±)-AMPA) 是谷氨酸的一种类似物，对兴奋性神经递质 L-谷氨酸有激动作用。它不会干扰海藻酸或 NMDA 受体的结合位点。
T70340	JHU-58
	JHU-58 is a novel dipeptide MrgC agonist. JHU-58 inhibited both mechanical and heat hypersensitivity in rats after an L5 spinal nerve ligation (SNL). JHU58 attenuated the evoked excitatory postsynaptic currents in substantia gelatinosa (SG) neurons in wild-type mice, but not in Mrg knockout mice, after peripheral nerve injury.
T3011L	Kynurenine sulfate monohydrate L-Kynurenine sulfate monohydrate
	Kynurenine sulfate monohydrate is a precursor of kynurenic acid which is the only recognized endogenous excitatory amino acid receptor antagonist agent in the central nervous system. L-Kyn is known to be a pigment generating component in animals. In mamma
T71792	Quipazine maleate
	Quipazine maleate is a selective 5-HT receptor agonist that promotes the proliferation and apoptosis of human hepatocyte strain of L-02 strain and could also exert an excitatory effect on raphe neurons via stimulation of 5-HT2A receptors. Like quipazine, quipazine derivatives produce contracture of smooth muscle organs and bronchospasm.
TP1831	[Nle11]-Substance P
	[Nle11]-Substance P is a substance P analog that avoids methionine oxidation problems. Substance P was found in the gut as well as in the brain. It is responsible for a number of excitatory effects on both central and peripheral neurons.
T83512	[1,6-Aminosuberic acid]-arginine-Vasotocin
	[1,6-Aminosuberic acid]-arginine-Vasotocin，一种类似神经垂体激素的合成肽，对黄芪周期性振荡神经元（PON）展现兴奋作用。
T74129	L-Homocysteic acid
	L-Homocysteic acid (L-HCA) 是一种内源性兴奋性氨基酸，可作为NMDA 受体激动剂 (EC50: 14 μM)。L-Homocysteic acid 具有神经毒性，可用于神经系统疾病的研究。
T80065	Calcicludine	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	Calcicludine是Dendroaspis angusticeps产毒蛋白，针对高电压激活的calcium channel（特别是L型）有抑制作用，IC50为88 nM，影响兴奋性突触传递。
T80704	α-Pompilidotoxin α-PMTX
	α-Pompilidotoxin (α-PMTX) 是从 Anoplius samariensis 的毒液中分离的一种神经毒素。它能剂量依赖性地增强兴奋性突触后电流（EPSCs），并且这种增强作用是可逆的。α-Pompilidotoxin 在神经科学研究中被作为实验工具广泛应用。
T60242	(RS)-AMPA monohydrate
	(RS)-AMPA ((±)-AMPA) monohydrate 是谷氨酸的一种类似物，对兴奋性神经递质 L-谷氨酸 (L-glutamic acid) 有激动作用。(RS)-AMPA monohydrate 不会干扰海藻酸或 NMDA 受体的结合位点。
T75864	Calcineurin autoinhibitory peptide TFA
	Calcineurin autoinhibitory peptide TFA 为选择性Ca2+/钙调蛋白依赖性蛋白磷酸酶（钙调神经磷酸酶）抑制剂，IC50约为10 μM。该化合物能够保护神经元不受兴奋性神经元死亡影响。
T62127	AMPA-IN-1
	AMPA-IN-1 是一种 AMPA 受体的有效抑制剂。AMPA 受体是一种在大脑中广泛表达的受体，在调节快速兴奋性突触传递和突触可塑性中具有核心作用。AMPA-IN-1 对包括癫痫在内的多种中枢疾病具有潜在的研究价值。
TP1301	Orexin A (human, rat, mouse)
	Orexin A human, rat, mouse, a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A human, rat, mouse has been used to study its effect on the functioning of porcine pancreatic islets. It has also been used as an orexin receptor 1 (OX1R) agonist to study the effect of orexin systems in the effect of etonogestrel on respiratory response to prolonged metabolic acidosis.
T68918	Phenytoin-d10
	Phenytoin-d10 is intended for use as an internal standard for the quantification of phenytoin by GC- or LC-MS. Phenytoin is an anticonvulsant agent and active metabolite of fosphenytoin. Phenytoin is formed from fosphenytoin by tissue phosphatases. It inhibits neuronal voltage-gated sodium channels in a voltage-dependent manner. Phenytoin reduces the neuronal firing frequency and decreases the amplitude of excitatory post-synaptic potentials (EPSPs) in electrically stimulated rat corticostriatal...
T70063	GYKI 52466 HCl
	GYKI 52466 is an allosteric AMPA receptor antagonist. It selectively inhibits AMPA-induced inward currents (IC50 = 7.5 µM) over NMDA- or GABA-induced inward currents in primary rat hippocampal neurons at 50 µM but also inhibits kainate-induced inward currents in the same cells (IC50 = 11 µM).2 GYKI 52466 (10 µM) reduces the amplitude of spontaneous excitatory postsynaptic currents (EPSCs) in the same cells. It increases the latency to seizure onset and reduces mortality in a rat model of general...

化合物

Cat.No: T23513

Synonym: VU 10010

Target: AChR

Cat.No: T3478

Target: GluR

Cat.No: T7823

Synonym: 7-氯-3-甲基-3,4-二氢-2H-1,2,4-苯并噻二嗪 1,1-二氧化物

Target: GluR

EAAT2 activator 1

Cat.No: T9347

Synonym: 3-[(2-Chloro-6-fluorobenzyl)thio]-6-pyridin-2-ylpyridazine

Target: transporter

Cat.No: T15728

Synonym: LDN-0212320,LDN/OSU-0212320,OSU-0212320

Target: transporter

Cardioexcitatory peptide 1

Cat.No: T82778

Cat.No: T15446

Target: transporter

Cat.No: T4138

Synonym: UCPH 101

Target: transporter

Cat.No: T0313

Synonym: Direct Blue 53,C.I. 23860,伊文思蓝

Target: GluR

(S)-3-AMino-2-Methylpropanoic acid-HCl

Cat.No: T7401

Target: Others

Calcineurin Autoinhibitory Peptide acetate

Cat.No: TP2054L

Target: Phosphatase

Cat.No: T76815

Synonym: ETR2-ST01,DR5 mAB,HGS-ETR 2

Target: Apoptosis

H-9 dihydrochloride

Cat.No: T22833

Target: EGFR, 5-HT Receptor, PKA

CS-722 Free base

Cat.No: T10893

Target: Others

Cat.No: T1065

Synonym: 巴氯芬,Lioresal

Target: GABA Receptor

Cat.No: T25853

Synonym: FG9202 disodium,NBQX 2Na

Target: GluR

Baclofen hydrochloride

Cat.No: T8630

Synonym: 4-amino-3-(4-chlorophenyl)butanoic acid hydron chloride

Target: GABA Receptor

Cat.No: T38192

Target: Others

Cat.No: T0267

Synonym: AD 810,唑尼沙胺,CI 912

Target: Calcium Channel, Sodium Channel, Carbonic Anhydrase

Cat.No: T22704

Target: Others

Cat.No: T22479

Target: Others

Cat.No: T23864

Synonym: (alpha-Carboxycyclopropyl)glycine,L-Ccg-I

Cat.No: T71829

Cat.No: T22480

Target: Others

N-Acetylglycyl-D-glutamic acid

Cat.No: T23037

Target: Others

Cat.No: T24074

MDNI-caged-L-glutamate

Cat.No: T40973

Synonym: MDNI-caged-L-glutamate,MDNI-glu

Cysteic acid, L-

Cat.No: T23930

Synonym: NSC254030,L-Cysteic acid,Cysteinic acid,NSC 254030,NSC-254030

(R)-Baclofen hydrochloride

Cat.No: T17306

Synonym: Arbaclofen hydrochloride,(R)-巴氯芬盐酸盐

Target: GABA Receptor

Neurokinin A (4-10), nle(10)-

Cat.No: T33653

Synonym: 10-Nle-neurokinin A (4-10)

DL-TBOA ammonium

Cat.No: T39510

Ibotenic acid hydrate

Cat.No: T69017

Cat.No: T11055

Target: transporter

L-Glutamic acid-15N

Cat.No: T39565

Substance P (1-9)

Cat.No: TP1819

Cat.No: T16800

Synonym: (±)-AMPA

Target: iGluR

Cat.No: T70340

Kynurenine sulfate monohydrate

Cat.No: T3011L

Synonym: L-Kynurenine sulfate monohydrate

Quipazine maleate

Cat.No: T71792

[Nle11]-Substance P

Cat.No: TP1831

[1,6-Aminosuberic acid]-arginine-Vasotocin

Cat.No: T83512

L-Homocysteic acid

Cat.No: T74129

Cat.No: T80065

Target: Calcium Channel

α-Pompilidotoxin

Cat.No: T80704

Synonym: α-PMTX

(RS)-AMPA monohydrate

Cat.No: T60242

Calcineurin autoinhibitory peptide TFA

Cat.No: T75864

Cat.No: T62127

Orexin A (human, rat, mouse)

Cat.No: TP1301

Cat.No: T68918

Cat.No: T70063

Cat. No.	Product Name	Target	Signaling Pathways
T15643	Kainic acid 红藻氨酸,红藻氨酸, **	Others	Others
	Kainic acid 是一种 CNS 中兴奋性氨基酸受体亚型激动剂。
T2A2497	L-Glutamic acid 谷氨酸,(S)-Glutamic acid,glutamic acid,(+)-L-Glutamic acid,Aciglut,L-谷氨酸,glutacid,Glutaminol	Apoptosis; Ferroptosis; Endogenous Metabolite; iGluR	Apoptosis; Membrane transporter/Ion channel; Metabolism; Neuroscience
	L-Glutamic acid (Glutaminol) 作为一种兴奋性氨基酸神经递质，为谷氨酸盐受体所有亚型的激动剂，对多巴胺从神经末梢释放的过程有激动作用。
T39359	γ-Glu-Gly gamma-Glutamylglycine	Amino Acids and Derivatives	Metabolism
	γ-Glu-Gly（gamma-Glutamylglycine），一种γ-谷氨酰基二肽，是具有与GABA（γ-氨基丁酸）相似结构的人体脂质代谢产物，可作为兴奋性氨基酸的拮抗剂。
T5083	L-Cysteic acid monohydrate L-磺基丙氨酸一水合物,3-Sulfo-L-alanine Monohydrate	Endogenous Metabolite; GluR	Metabolism; Neuroscience
	L-Cysteic acid monohydrate (3-Sulfo-L-alanine Monohydrate) 是内源性代谢产物的一种。
T4705	Aminoadipic acid DL-2-Aminoadipic acid,DL-2-氨基己二酸	Others; Endogenous Metabolite	Metabolism; Others
	Aminoadipic acid (DL-2-Aminoadipic acid) 是赖氨酸主要生化途径中的代谢物。它是赖氨酸和糖碱代谢的中间体。它拮抗由谷氨酸受体 N-甲基-D-天冬氨酸调节的神经兴奋特性。
T35401	γ-Glu-Gly TFA
	γ-Glu-Gly TFA, a γ-glutamyl dipeptide, is a human lipid metabolite with a structure resembling GABA (γ-aminobutyric acid). It serves as an excitatory amino acid antagonist [1][2][3].

天然产物

Cat.No: T15643

Synonym: 红藻氨酸,红藻氨酸, **

Target: Others

L-Glutamic acid

Cat.No: T2A2497

Synonym: 谷氨酸,(S)-Glutamic acid,glutamic acid,(+)-L-Glutamic acid,Aciglut,L-谷氨酸,glutacid,Glutaminol

Target: Apoptosis, Ferroptosis, Endogenous Metabolite, iGluR

Cat.No: T39359

Synonym: gamma-Glutamylglycine

Target: Amino Acids and Derivatives

L-Cysteic acid monohydrate

Cat.No: T5083

Synonym: L-磺基丙氨酸一水合物,3-Sulfo-L-alanine Monohydrate

Target: Endogenous Metabolite, GluR

Aminoadipic acid

Cat.No: T4705

Synonym: DL-2-Aminoadipic acid,DL-2-氨基己二酸

Target: Others, Endogenous Metabolite

Cat.No: T35401

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