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30

抑制剂 & 化合物

7

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T0680	Lamotrigine LTG,BW430C,拉莫三嗪	5-HT Receptor; Sodium Channel; Autophagy	Autophagy; GPCR/G Protein; Membrane transporter/Ion channel; Neuroscience
	Lamotrigine (BW430C) 是一种抗癫痫剂和情绪稳定剂，可研究癫痫、局灶性癫痫等。。它选择性地阻断电压门控钠离子通道，稳定突触前神经元膜，抑制谷氨酸释放。
T8963	CYM2503	Neuropeptide Y Receptor	GPCR/G Protein; Neuroscience
	CYM2503 是 GAL2 受体的正变构调节剂 (PAM)，可在体外增强甘丙肽诱导的 IP1 产生。它对受体的正构甘丙肽结合位点没有亲和力（通过其无法置换碘化甘丙肽或自行诱导 IP1 积累来衡量）。
T22746	Tesmilifene fumarate DPPE fumarate	Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Neuroscience
	Tesmilifene fumarate (DPPE fumarate) 是一种 H1C 受体拮抗剂，可增强化疗的细胞毒性且保护正常细胞。
T3563	Lvguidingan	Others	Others
	Lvguidingan 是一种抗惊厥药。
T0786	Clidinium bromide 克利溴铵,Ro 2-3773	AChR	Neuroscience
	Clidinium bromide (Ro 2-3773) 是季胺抗毒蕈碱剂，可通过减少胃酸和减慢肠道速度，缓解痉挛和腹部疼痛的症状。
T11908	LY2365109 hydrochloride LY2365109盐酸盐	GlyT	Neuroscience
	LY2365109 hydrochloride 是高选择性GlyT1抑制剂，抑制过表达 hGlyT1 细胞摄取谷氨酸的IC50值为 15.8 nM.
TP1187	C-Type Natriuretic Peptide (CNP) (1-22), human CNP (1-22), human	RAAS	Endocrinology/Hormones
	C-Type Natriuretic Peptide (CNP) (1-22), human 是一种利钠肽受体 B (NPR-B) 激动剂，是一种 CNP 的 1-22 片段。它对生理激动剂组胺和 5-HT 刺激或直接由 Forskolin 刺激的 cAMP 合成具有抑制作用。其中CNP 是一种有效的、内皮衍生的松弛剂和生长抑制因子。
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。
T16801	(RS)-(Tetrazol-5-yl)glycine LY 285265,D,L-(tetrazol-5-yl)glycine	NMDAR; iGluR	Membrane transporter/Ion channel; Neuroscience
	(RS)-(Tetrazol-5-yl)glycine (LY 285265) 是一种高效且选择性的 N-甲基-D-天冬氨酸 (NMDA) 受体激动剂。它能够诱导小鼠癫痫发作反应和 Fos。它对 GluN1/GluN2D 和 GluN1/GluN2A 的EC50分别为 99 nM，1.7 μM。
T10774	CFM-2	iGluR	Membrane transporter/Ion channel; Neuroscience
	CFM-2, a potent and selective non-competitive antagonist of AMPAR (AMPAR), exhibits anticonvulsant activity across various seizure models.
T2523	Rufinamide CGP 33101,E 2080,卢非酰胺,RUF 331	Sodium Channel	Membrane transporter/Ion channel
	Rufinamide (E 2080) 是一种新型镇痫化合物，可用于研究 Lennox-Gastaut 综合症。
T16977	Talampanel GYKI-53773,LY-300164	Apoptosis; GluR	Apoptosis; Neuroscience
	Talampanel (LY-300164) 是一种口服和选择型 AMPA 受体拮抗剂，具有抗癫痫活性。在啮齿动物的中风模型中，它具有神经保护作用。Talampanel 减弱 caspase-3 依赖性细胞凋亡。
T38808	Cyclamic acid sodium Cyclohexylsulfamicacidsodium,Sodiumcyclamate	Carbonic Anhydrase	Metabolism
	Cyclamic acid sodium (Cyclohexylsulfamicacidsodium) 是一种碳酸酐酶抑制剂，是食品和药品中使用最广泛的人工甜味剂之一。Cyclamic acid sodium 在最大电休克惊厥发作模型显示出中等的抗惊厥活性。Cyclamic acid sodium 可用于研究癌症。
T24167	Inflachromene ICM	Others	Others
	Inflachromene(ICM) 是一种 HMGB1 和 HMGB 表达抑制剂，具有抗炎活性。Inflachromene 通过抑制 HMGB1 易位来减轻小鼠癫痫模型的癫痫发作严重程度，通过 HMGB1/2 调节的 TLR4-NF-κB 通路抑制内膜增生，通过调节 Beclin 1 活性来抑制自噬。Inflachromene 可用于研究癫痫。
T11800	L-803087	Somatostatin	GPCR/G Protein
	L-803087 是一种具有高效性和选择性的生长抑素 sst4 受体激动剂，对 sst4 的 Ki 值为 0.7 nM，比其他生长抑素受体的选择性高 280 倍以上。L-803087 在体外诱导 AMPA 介导的海马突触反应，在体内增加了海藻酸盐促使的小鼠癫痫发作。
T0939	Phenytoin 苯妥英,Diphenylhydantoin,5,5-Diphenylhydantoin	Virus Protease; Sodium Channel	Membrane transporter/Ion channel; Microbiology/Virology
	Phenytoin (5,5-Diphenylhydantoin) 是一种有效的电压门控钠离子通道阻滞剂，可减少小鼠乳腺肿瘤的生长和转移，具有抗癫痫活性。
T38294	4-Deoxypyridoxine hydrochloride	S1P Receptor	GPCR/G Protein
	4-Deoxypyridoxine hydrochloride 通过抑制 S1P 裂解酶 (SPL) 活性来抑制细胞内 S1P 的降解，与 S1P 一样，减少化学诱导的胰岛素瘤细胞系的细胞凋亡。
T71956	Pimprinine
	Pimprinine is an alkaloid. It is a potent inhibitor of MAO (monoamine oxidase). More recently, pimprinine showed promising anticonvulsant activity in electric seizure threshold.
T37119	1,2,3-Trioctanoyl-rac-glycerol-13C3 1,2,3-Trioctanoyl-rac-glycerol-13C3
	1,2,3-Trioctanoyl-rac-glycerol-13C3 is intended for use as an internal standard for the quantification of 1,2,3-trioctanoyl-rac-glycerol by GC- or LC-MS. 1,2,3-Trioctanoyl-rac-glycerol is a triacylglycerol that contains octanoic acid at the sn-1, sn-2, and sn-3 positions. Dietary administration of 1,2,3-trioctanoyl-rac-glycerol increases hippocampal levels of the glycolytic metabolites glucose 6-phosphate, fructose 6-phosphate, and β-hydroxybutyrate and the seizure threshold in the 6 Hz psychomo...
T38224	2,3-Dehydro-2-deoxy-N-acetylneuraminic acid
	N-acetyl-2,3-dehydro-2-Deoxyneuraminic acid (DANA) is an inhibitor of human neuriminidases (sialidases) NEU1-4 (IC50s = 143, 43, 61, and 74 μM, respectively). In vivo, DANA (30 μL of a 5 mM solution) reduces latency to first seizure and increases seizure duration in a rat model of potassium-induced seizures.
T37950	2-(Isopentylamino)naphthalene-1,4-dione
	2-(Isopentylamino)naphthalene-1,4-dione is a vitamin K analog.1It inhibits spasms induced by pentylenetetrazole and tonic hindlimb extension induced by maximal electroshock (MES) in mice (ED50s = 349.2 and 108.1 mg/kg, respectively). It also protects mice against seizures in the 6 Hz psychomotor seizure test (ED50s = 152.7 and 263.7 mg/kg at stimulus intensities of 32 and 44 mA, respectively). 1.Li, X., Himes, R.A., Prosser, L.C., et al.Discovery of the first vitamin K analogue as a potential tr...
T82057	Iota-conotoxin RXIA
	Iota-conotoxin RXIA是一种作用于电压门控钠通道（Nav1.2, 1.6, 1.7）的激动剂，其在小鼠脑内注射后能够引发青蛙运动神经轴突的重复动作电位以及癫痫样发作。
T60492	Lamotrigine hydrate
	Lamotrigine hydrate 是口服有效的抗惊厥剂或抗癫痫剂，通过选择性地阻断电压门控Na+通道，稳定突触前神经元膜并抑制谷氨酸释放。Lamotrigine hydrate 可用于研究癫痫、局灶性癫痫等神经性疾病。
T69202	NBQX sodium
	NBQX, also known as FG9202, is an AMPA receptor antagonist. NBQX blocks AMPA receptors in micromolar concentrations (~10–20 µM) and also blocks kainate receptors. In experiments, it is used to counter glutamate excitotoxicity. NBQX was found to have anticonvulsant activity in rodent seizure models. As the disodium salt, NBQX is soluble in water at high concentrations (at least up to 100 mM).
T79806	5-HT2A&5-HT2C agonist-1	5-HT Receptor	GPCR/G Protein; Neuroscience
	5-HT2A&5-HT2C agonist-1 (Example 2) 是一种选择性的5-HT2A和5-HT2C受体激动剂，其IC50值分别为196 nM和0.9 nM。本化合物主要应用于研究抑郁症、酒精依赖、烟草和可卡因成瘾、炎症、丛集性头痛、PTSD、癫痫等中枢神经系统相关疾病。
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...
T79805	5-HT2 agonist-1 free base	5-HT Receptor	GPCR/G Protein; Neuroscience
	5-HT2 agonist-1 (Compound 24) free base 是一种作用于5-HT2A, 5-HT2B和5-HT2C受体的激动剂，其IC50值分别为10 nM, 8.3 nM和1.6 nM。该化合物主要应用于研究抑郁症、酒精依赖、烟草及可卡因成瘾、炎症、丛集性头痛、创伤后应激障碍(PTSD)、癫痫以及其他中枢神经系统相关疾病。
T79804	5-HT2 agonist-1	5-HT Receptor	GPCR/G Protein; Neuroscience
	5-HT2 agonist-1 (Compound 24) 是一种选择性5-HT2A, 5-HT2B和5-HT2C激动剂，其IC50值分别为10 nM, 8.3 nM和1.6 nM。5-HT2 agonist-1 free base主要用于研究治疗抑郁症、酗酒、吸烟与可卡因依赖、炎症、丛集性头痛、创伤后应激障碍(PTSD)、癫痫以及其他中枢神经系统疾病。
T37215	5α,6β-Dihydroxycholestanol
	5α,6β-Dihydroxycholestanol is an oxysterol metabolite of cholesterol formed from conversion of cholesterol epoxides by 5,6-epoxysterol hydrolase. It inhibits NMDA-mediated calcium influx in HEK293 cells expressing NR1/NR2B NMDA receptors in a concentration-dependent manner. It also binds to voltage-gated sodium (Nav) channels and decreases action potentials in hippocampal neurons in vitro when used at a concentration of 10 uM. It increases survival of spinal cord motoneurons, cortical neurons, a...
T37847	Zonisamide-13C2,15N Zonisamide-13C2,15N
	Zonisamide-13C2,15N is intended for use as an internal standard for the quantification of zonisamide by GC- or LC-MS. Zonisamide is an antiepileptic agent.1 It selectively inhibits the repeated firing of sodium channels (IC50 = 2 μg/ml) in mouse embryo spinal cord neurons and inhibits spontaneous channel firing when used at concentrations greater than 10 μg/ml.2 In rat cerebral cortex neurons, zonisamide (1-1,000 μM) inhibits T-type calcium channels with a maximum reduction of 60% of the calcium...

化合物

Cat.No: T0680

Synonym: LTG,BW430C,拉莫三嗪

Target: 5-HT Receptor, Sodium Channel, Autophagy

Cat.No: T8963

Target: Neuropeptide Y Receptor

Tesmilifene fumarate

Cat.No: T22746

Synonym: DPPE fumarate

Target: Histamine Receptor

Cat.No: T3563

Target: Others

Clidinium bromide

Cat.No: T0786

Synonym: 克利溴铵,Ro 2-3773

Target: AChR

LY2365109 hydrochloride

Cat.No: T11908

Synonym: LY2365109盐酸盐

Target: GlyT

C-Type Natriuretic Peptide (CNP) (1-22), human

Cat.No: TP1187

Synonym: CNP (1-22), human

Target: RAAS

Cat.No: T0267

Synonym: AD 810,唑尼沙胺,CI 912

Target: Calcium Channel, Sodium Channel, Carbonic Anhydrase

(RS)-(Tetrazol-5-yl)glycine

Cat.No: T16801

Synonym: LY 285265,D,L-(tetrazol-5-yl)glycine

Target: NMDAR, iGluR

Cat.No: T10774

Target: iGluR

Cat.No: T2523

Synonym: CGP 33101,E 2080,卢非酰胺,RUF 331

Target: Sodium Channel

Cat.No: T16977

Synonym: GYKI-53773,LY-300164

Target: Apoptosis, GluR

Cyclamic acid sodium

Cat.No: T38808

Synonym: Cyclohexylsulfamicacidsodium,Sodiumcyclamate

Target: Carbonic Anhydrase

Cat.No: T24167

Synonym: ICM

Target: Others

Cat.No: T11800

Target: Somatostatin

Cat.No: T0939

Synonym: 苯妥英,Diphenylhydantoin,5,5-Diphenylhydantoin

Target: Virus Protease, Sodium Channel

4-Deoxypyridoxine hydrochloride

Cat.No: T38294

Target: S1P Receptor

Cat.No: T71956

1,2,3-Trioctanoyl-rac-glycerol-13C3

Cat.No: T37119

Synonym: 1,2,3-Trioctanoyl-rac-glycerol-13C3

2,3-Dehydro-2-deoxy-N-acetylneuraminic acid

Cat.No: T38224

2-(Isopentylamino)naphthalene-1,4-dione

Cat.No: T37950

Iota-conotoxin RXIA

Cat.No: T82057

Lamotrigine hydrate

Cat.No: T60492

Cat.No: T69202

5-HT2A&5-HT2C agonist-1

Cat.No: T79806

Target: 5-HT Receptor

Cat.No: T70063

5-HT2 agonist-1 free base

Cat.No: T79805

Target: 5-HT Receptor

5-HT2 agonist-1

Cat.No: T79804

Target: 5-HT Receptor

5α,6β-Dihydroxycholestanol

Cat.No: T37215

Zonisamide-13C2,15N

Cat.No: T37847

Synonym: Zonisamide-13C2,15N

Cat. No.	Product Name	Target	Signaling Pathways
T0983	Penicillamine 青霉胺,d-penicillamin,Dimethyl Cysteine,D-青霉胺,Artamine,D-(-)-Penicillamine	Antibiotic	Microbiology/Virology
	Penicillamine (Artamine) 是一种 penicillin 的代谢降解产物，是一种螯合剂，可作用于威尔逊氏病。
TN2865	(E)-3,4,5-Trimethoxycinnamic acid O-Methylsinapic acid,3,4,5-三甲氧基肉桂酸,3,4,5-Trimethoxy-trans-cinnamic acid,3,4,5-Trimethoxyphenylacrylic acid	Others	Others
	(E)-3,4,5-Trimethoxycinnamic acid (O-Methylsinapic acid) 是一种来自羌活根和根茎的天然产物。
T2983	3,4,5-Trimethoxycinnamic acid 3-(3,4,5-Trimethoxyphenyl)acrylic Acid,O-Methylsinapic acid,3,4,5-三甲氧基肉桂酸	GABA Receptor; Endogenous Metabolite	Membrane transporter/Ion channel; Metabolism; Neuroscience
	3,4,5-Trimethoxycinnamic acid (O-Methylsinapic acid) 是从远志中分离得到的苯丙素类天然产物，可延长动物的睡眠时间，增强 GAD65 和 GABAA 受体 γ 亚基，具有抗应激作用。
T9299	D-Leucine D-亮氨酸,(R)-Leucine	Endogenous Metabolite	Metabolism
	D-Leucine ((R)-Leucine) 具有抗癫痫特性，活性比L-leucine，能够有效终止癫痫发作。在体外，它能够抑制长期点位，但基底突触传递无影响。
T2S1464	Thiocolchicoside 硫秋水仙苷;噻可撒可,Thiocolchicine 2-glucoside analog,硫秋水仙苷,Coltramyl	Others; GABA Receptor	Membrane transporter/Ion channel; Neuroscience; Others
	Thiocolchicoside (Thiocolchicine 2-glucoside analog) 是秋水仙碱的半合成硫衍生物，是竞争性 GABAA 受体拮抗剂和甘氨酸受体拮抗剂。它是肌肉松弛剂，具有抗炎作用，可用于缓解疼痛的研究。
TMS1461	Qingyangshengenin B 青阳参甙元B,青阳参苷元B,Otophylloside B	Beta Amyloid	Neuroscience
	Qingyangshengenin B (Otophylloside B) 是一种分离自 Qingyangshen 的 C-21 甾体苷。它能够在 mRNA 水平上抑制 Aβ 的表达来减少 Aβ 的沉积，对 Aβ 的毒性有保护作用。它具有抗癫痫作用。
TN4722	Otophylloside F	Others	Others
	Otophylloside F can suppress the seizure-like locomotor activity caused by pentylenetetrazole in zebrafish.

天然产物

Cat.No: T0983

Synonym: 青霉胺,d-penicillamin,Dimethyl Cysteine,D-青霉胺,Artamine,D-(-)-Penicillamine

Target: Antibiotic

(E)-3,4,5-Trimethoxycinnamic acid

Cat.No: TN2865

Synonym: O-Methylsinapic acid,3,4,5-三甲氧基肉桂酸,3,4,5-Trimethoxy-trans-cinnamic acid,3,4,5-Trimethoxyphenylacrylic acid

Target: Others

3,4,5-Trimethoxycinnamic acid

Cat.No: T2983

Synonym: 3-(3,4,5-Trimethoxyphenyl)acrylic Acid,O-Methylsinapic acid,3,4,5-三甲氧基肉桂酸

Target: GABA Receptor, Endogenous Metabolite

Cat.No: T9299

Synonym: D-亮氨酸,(R)-Leucine

Target: Endogenous Metabolite

Thiocolchicoside

Cat.No: T2S1464

Synonym: 硫秋水仙苷;噻可撒可,Thiocolchicine 2-glucoside analog,硫秋水仙苷,Coltramyl

Target: Others, GABA Receptor

Qingyangshengenin B

Cat.No: TMS1461

Synonym: 青阳参甙元B,青阳参苷元B,Otophylloside B

Target: Beta Amyloid

Otophylloside F

Cat.No: TN4722

Target: Others

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