55
7
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T8594 |
Pheneturide
2-PHENYLBUTYRYLUREA,S-46,Benuride,苯丁酰脲 |
Others | Others |
Pheneturide (Benuride) 是Phenobarbita l 脱羧后的产物,可阻止精神运动性癫痫发作。 | |||
T0283 |
Trimethadione
三甲双酮,3,5,5,-Trimethyloxazolidine-2,4-dione |
Calcium Channel | Membrane transporter/Ion channel; Metabolism |
Trimethadione (3,5,5,-Trimethyloxazolidine-2,4-dione) 是恶唑烷二酮类抗惊厥剂,也是一种 T 型钙通道阻滞剂,具有抗痛觉过敏作用,可用于研究失神发作。 | |||
T23782 |
Benzolamide
CL-11366,W 1803,CL 11366,CL11366,苯唑拉胺,W-1803 |
Carbonic Anhydrase | Metabolism |
Benzolamide (CL 11366) 是碳酸酐酶 (CA) 抑制剂,抑制hCA I(Ki:15 nM)、hCA II(Ki:9 nM)、EcoCAγ(Ki:94 nM)、VchCAγ(Ki:78 nM)、CAS3(Ki:54 nM)。它可用于研究青光眼和癫痫。 | |||
T7806 |
Licarbazepine
10,11-hydroxy-10,11 Dihydrocarbamezer,10,11-二氢-10-羟基卡马西平 |
Others | Others |
Licarbazepine (10,11-hydroxy-10,11 Dihydrocarbamezer) 是一种有效的电压门控钠通道阻滞剂,具有抗惊厥和稳定情绪的功效。 | |||
T15302 |
Fluzinamide
AHR-8559 |
Others | Others |
Fluzinamide(AHR-8559)对点燃性杏仁核癫痫发作有抗惊厥作用。 | |||
T27845 |
Losigamone
ADD-137022,AO33,AO 33,ADD 137022,AO-33,ADD137022;Losigamone |
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
Losigamone (AO-33) 是 GABA 受体的激动剂,可用于治疗部分性癫痫发作的研究。 | |||
T6507 |
Gabapentin hydrochloride
加巴喷丁盐酸盐,Neurontin HCl,Gabapentin HCl |
Calcium Channel; GABA Receptor | Membrane transporter/Ion channel; Metabolism; Neuroscience |
Gabapentin hydrochloride (Neurontin HCl) 是GABA 类似物,可用于缓解神经性疼痛。 | |||
T68054 |
Denzimol
|
Others | Others |
Denzimol 是一种新型抗惊厥化合物。Denzimol 对强直性癫痫发作具有选择性。 | |||
T3285L |
Eslicarbazepine
艾司利卡西平,Pazzul,EC 810-248-9,BIA 2-194,Stedesa,Erelib |
Beta-Secretase; Sodium Channel | Membrane transporter/Ion channel; Neuroscience |
Eslicarbazepine (Stedesa) 是口服有效抗惊厥试剂,在局部癫痫的辅助研究中具有价值。 | |||
T23717 |
Ameltolide
|
Others | Others |
Ameltolide 是一种抗惊厥剂。在动物模型中,它被证明能有效抑制癫痫发作。 | |||
T40864 |
Magnesium sulfate
|
Others | Others |
Magnesium sulfate 是目前预防和控制子痫发作的抗惊厥剂。Magnesium sulfate 也被广泛用作宫缩剂。 | |||
T12156 |
N-(2-Chloro-6-methylphenyl)-N'-4-pyridinylurea
|
Others | Others |
N-(2-Chloro-6-methylphenyl)-N'-4-pyridinylurea 是一种抗惊厥剂,对广泛强直和部分性发作挛性具有潜在的研究价值。 | |||
T1249 |
Beclamide
N-Benzyl-3-chloropropionamide,Chloracon,Chlorakon,贝克拉胺(INN) |
Others | Others |
Beclamide (Chlorakon) 是一种抗惊厥药,具有抗惊厥作用。 | |||
T29201 |
Z944
Z 944,Z-944 |
Calcium Channel | Membrane transporter/Ion channel; Metabolism |
Z944 是有效的 T 型钙通道拮抗剂,对跨模态和视觉识别记忆障碍有缓解作用。 | |||
T22171 |
WWL123
|
MAGL | Metabolism |
WWL123 是一种有效的选择性 ABHD6 抑制剂,IC50 为 430 nM。WWL123 可穿过血脑屏障并抑制脑实质中的 ABHD6。WWL123 阻断 ABHD6 在 Pentylenetetrazole (PTZ)诱导的 R6/2 小鼠癫痫样发作和自发性癫痫发作中发挥抗癫痫作用。 | |||
T21526 |
α-Guanidinoglutaric Acid
|
Others | Others |
α-Guanidinoglutaric Acid 存在于猫大脑皮层钴诱导的致癫痫病灶组织中。 α-Guanidinoglutaric Acid 诱导的癫痫发作与血清素功能异常有关,它们是由 5-HT 水平的降低引起的。 | |||
T6953 |
Prilocaine
Citanest,丙胺卡因,Propitocaine,NSC 40027 |
ATPase; Sodium Channel | Membrane transporter/Ion channel |
Prilocaine (NSC-40027) 是一种氨基酰胺类局部麻醉剂,作用于神经元膜上的钠通道并限制癫痫发作的扩散。它是Na/K-ATPase 抑制剂,具有神经毒性作用。 | |||
T73556 |
CZL55
|
Caspase | Apoptosis; Proteases/Proteasome |
CZL55 是一种有效的 caspase-1 抑制剂,IC50 值为0.024 μM 。CZL55 具有较低的细胞毒性,可用于研究热性癫痫 (FS)。 | |||
T68058 |
Dulozafone
F1933 |
Others | Others |
Dulozafone (F1933) 具有抗在脑杏仁核点燃模型中显示出抗惊厥活性,可保护完全点燃的大鼠免受全身性癫痫发作。 | |||
T3285 |
Eslicarbazepine Acetate
Zebinix,Aptiom,BIA 2-093,Exalief,艾司利卡西平醋酸酯,Stedesa |
Beta-Secretase; Sodium Channel | Membrane transporter/Ion channel; Neuroscience |
Eslicarbazepine Acetate (Zebinix) 是一种抗癫痫药物。Eslicarbazepine acetate 也是 β-内分泌酶(β-Secretase)和电压门控钠离子通道的双抑制剂。 | |||
T23508 |
VU 0255035
|
AChR | Neuroscience |
VU 0255035 是高度选择性、竞争性和血脑屏障通透性的毒蕈碱 M1 受体拮抗剂,IC50为 130 nM,可减少毛果芸香碱诱导的小鼠癫痫发作。 | |||
T0675 |
Topiramate
RWJ 17021,McN 4853,托吡酯 |
Potassium Channel; Calcium Channel; GABA Receptor; Sodium Channel; GluR; Carbonic Anhydrase; iGluR | Membrane transporter/Ion channel; Metabolism; Neuroscience |
Topiramate (RWJ 17021) 是一种GluR5受体拮抗剂,可通过增强GABAergic 活性,抑制kainate/AMPA 受体,抑制钠和钙通道的电压敏感,增加钾电导并抑制碳酸酐酶来产生抗癫痫作用,用于治疗部分性和全身性癫痫发作。 | |||
T14384 |
AZD8797
KAN-0440567,KAND567 |
CXCR | Autophagy; GPCR/G Protein; Immunology/Inflammation |
AZD8797 (KAND567) 是一种可口服且具有选择性和有效性的人 CX3CR1 变构拮抗剂,对 CX3CR1 和 CXCR2 具有抑制作用,对SARS-CoV-2诱导的神经元损伤有潜在的保护作用,可防止癫痫发作后偏头痛模型大鼠痛觉过敏和小胶质细胞活化的恶化。 | |||
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。 | |||
T0192 |
Levetiracetam
左乙拉西坦,UCB L059,SIB-S1 |
DNA Methyltransferase; Others; Calcium Channel | Chromatin/Epigenetic; Membrane transporter/Ion channel; Metabolism; Others |
Levetiracetam (SIB-S1) 是一种化学增敏剂,增强 Temozolomide 对胶质母细胞瘤干细胞增殖和凋亡的影响。它调节 HDAC 水平,最终使 MGMT 沉默从而提高 Temozolomide 的有效性。它是一种抗癫痫药,可结合突触小泡蛋白 SV2A。 | |||
T37149 |
Carbamazepine 10,11-epoxide
|
Others | Others |
Carbamazepine 10,11-epoxide 是抗惊厥药卡马西平 (carbamazepine) 的活性代谢物。它由卡马西平通过微粒体中的细胞色素 P450 (CYP) 同种型 CYP3A4 和 CYP2C8 形成,微粒体分别由表达 CYP3A4 或 CYP2C8 的 HepG2 细胞制备。它对小鼠电击诱发的癫痫发作具有抗惊厥活性。 | |||
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。 | |||
T23037 |
N-Acetylglycyl-D-glutamic acid
|
Others | Others |
Excitatory peptide that induces seizures | |||
T25307 |
Denzimol hydrochloride
REC 15-1533 |
||
Denzimol hydrochloride 是一种新型抗惊厥药物,能抑制电性和化学性诱发的强直性癫痫发作,但不能阻止阵挛性癫痫发作。其表现与苯妥英和卡马西平相似,但与巴比妥类和苯二氮卓类不同。 | |||
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 ... | |||
TP2028 |
Galanin (1-29)(rat, mouse)
Galanin (1-29) (rat, mouse) |
||
Non-selective galanin receptor agonist (Ki values are 0.98, 1.48 and 1.47 nM for GAL1, GAL2 and GAL3 respectively). Anticonvulsant; prevents the occurrence of full kindled seizures in rats. | |||
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... | |||
T82294 | GLUT1-IN-3 | ||
GLUT1-IN-3 (Compd 4b) 是针对1型葡萄糖转运蛋白缺乏综合症相关疾病研究的化合物,具有有效抑制癫痫发作的作用。 | |||
T28766 |
SGE-516
SGE516 |
||
SGE516 is a neuroactive steroid and a positive allosteric modulator of both gamma- and delta-containing GABAA receptors. SGE516 reduces neuronal firing rates and epileptiform activity in vitro. SGE-516 protects against acute seizures and reduces neuronal | |||
T37557 |
(-)-(α)-Kainic Acid (hydrate)
|
||
(-)-(α)-Kainic Acid (hydrate) 是一种有效的兴奋性毒性剂,可诱发癫痫发作。(-)-(α)-Kainic Acid (hydrate) 也是离子型谷氨酸受体亚型的激动剂。 | |||
T69780 |
VU6007477
|
||
VU6007477 is a novel M1 PAM. VU6007477 resulted in good rat M1 PAM potency (EC50 = 230 nM, 93% ACh max), minimal M1 agonist activity (agonist EC50 > 10 μM), good CNS penetration (rat brain/plasma Kp = 0.28, Kp,uu = 0.32; mouse Kp = 0.16, Kp,uu = 0.18), and no cholinergic adverse events (AEs, e.g., seizures). | |||
T70896 |
PF05020182
|
||
PF05020182 is novel potent and selective Kv7.2/4 potassium channel opener. PF-05020182 (2) significantly inhibits convulsions in the MES assay at doses tested, consistent with in vitro activity measure. The physiochemical properties, in vitro and in vivo activities of PF-05020182 support further development as an adjunctive treatment of refractory epilepsy. Facilitating activation, or delaying inactivation, of the native Kv7 channel reduces neuronal excitability, which may be beneficial in cont... | |||
T39207 |
L-803087 TFA
|
||
L-803087 TFA is a highly potent and selective agonist of the somatostatin sst4 receptor, exhibiting a Ki value of 0.7 nM. It displays a remarkable selectivity, being over 280-fold more preferential for the sst4 receptor compared to other somatostatin receptors. Furthermore, L-803087 TFA promotes AMPA-mediated synaptic responses in hippocampal preparations and enhances kainate-induced seizures in mice. | |||
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... | |||
T7720 |
CGP 37849
CGP-37849,CGP37849 |
NMDAR; iGluR | Membrane transporter/Ion channel; Neuroscience |
CGP 37849 是一种竞争性口服活性 N-甲基-D-天冬氨酸 (NMDA) 受体拮抗剂((Ki = 35 nM)),具有有效性。CGP 37849 是啮齿动物的抗惊厥药,也具有抗抑郁和抗焦虑的特性。 | |||
T72748 |
(S,S)-BD-AcAc 2
(S,S)-Ketone Ester |
||
'(S,S)-BD-AcAc 2 ((S,S)-Ketone Ester) 作为 BD-AcAc 2 的 (S,S)-对映异构体,能够提高 AcAc 与丙酮水平,进而持续引发酮症并明显延缓中枢神经系统氧中毒(CNS-OT)所致的癫痫发作。' | |||
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... | |||
T35432 |
α-Conotoxin ImI (trifluoroacetate salt)
|
||
α-Conotoxin ImI is a conotoxin that has been found inC. imperialisand has receptor antagonist and anticancer activities.1It is a peptide antagonist of homomeric α7 nicotinic acetylcholine receptors (nAChRs; IC50= 220 nM). α-Conotoxin ImI is selective for α7 nAChRs over α2β2, α3β2, α4β2, α2β4, α3β4, α4β4, and α1β1γδ subunit-containing nAChRs at 5 μM but does inhibit homomeric α9 nAChRs (IC50= 1,800 nM). Administration of paclitaxel in micelles containing α-conotoxin ImI decreases tumor growth in ... | |||
T26366L |
Prasterone sulfate sodium hydrate
Sodium dehydroepiandrosterone sulfate,Prasterone sulfate sodium salt dihydrate,5-Androsten-3β-ol-17-one sulfate sodium salt dihydrate |
||
Prasterone is an endogenous steroid hormone. Prasterone acts as an agonist at ERβ, NMDA, and σ1 receptors, a partial agonist at ERα and AR, and antagonist at GABA-A receptors. It displays a variety of biologocial activities, including enhancing working me | |||
T37608 |
Riluzole-13C,15N2
Riluzole-13C,15N2 |
||
Riluzole-13C,15N2 is intended for use as an internal standard for the quantification of riluzole by GC- or LC-MS. Riluzole is a benzothiazole derivative with anti-excitotoxic effects that acts by blocking the presynaptic release of glutamate, indirectly antagonizing glutamate receptors, and inactivating neuronal voltage-gated Na+ channels (ED50 = 2.3 μM). Riluzole suppresses glutamate-induced seizures in rats at an ED50 value of 3.2 mg/kg and displays neuroprotective effects in hypoxic animals a... | |||
T70186 |
Methazolamide-d6
|
||
Methazolamide-d6 is intended for use as an internal standard for the quantification of methazolamide by GC- or LC-MS. Methazolamide is a carbonic anhydrase inhibitor. It reduces intraocular pressure and cerebrospinal fluid flow in a rat model of glaucoma. Methazolamide reduces electroshock-induced seizures in rats with an ED50 value of 19.2 mg/kg. It also inhibits production of reactive oxygen species (ROS) in a primary cortical neuron (PCN) cellular model of subarachnoid hemorrhage (SAH) and re... | |||
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... | |||
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. | |||
T73436 |
AK-IN-1
|
||
AK-IN-1(化合物 4072-2732)是针对腺苷(Ado)具有竞争性抑制作用而对 ATP 不产生竞争性抑制作用的腺苷激酶(AK)抑制剂。在浓度为 2, 4, 10 µM 的条件下,AK-IN-1 能够分别抑制 86%、87% 和 89% 的 AK 活性。该化合物在包括缺血、炎症和癫痫发作在内的多种疾病研究领域展示出了良好的潜力。 | |||
T83963 |
Z-DEVD-FMK Caspase-3 Inhibitor
|
||
Z-DEVD-FMK Caspase-3 Inhibitor 是一种可渗透细胞膜的、不可逆的 caspase-3/CPP32 抑制剂,能够抑制肿瘤细胞的凋亡。在动物体内,它在大鼠发作后的海马区具有神经保护作用,且显著减少创伤后的细胞凋亡,并在诱发的大鼠创伤性脑损伤之前和之后改善神经学恢复情况。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T0728 |
Ethosuximide
Zarontin,乙琥胺 |
Calcium Channel | Membrane transporter/Ion channel; Metabolism |
Ethosuximide (Zarontin) 是一种抗癫痫药物,可改善多种神经退行性疾病模型的表型,且阻断低电压激活的 T 型钙通道。 | |||
T5968 |
DL-Homocysteine thiolactone hydrochloride
DL-Homocysteinethiolactone hydrochloride,DL-高半胱氨酸硫内酯盐酸盐 |
Endogenous Metabolite | Metabolism |
DL-Homocysteine thiolactone hydrochloride (DL-Homocysteinethiolactone hydrochloride) 是具有根生长抑制特性的环状氨基酸衍生物。 | |||
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。 | |||
T3S1416 |
Decursin
Decursinol angelate,前胡素,(+)-Decursin,紫花前胡素 |
Apoptosis; PKC | Apoptosis; Chromatin/Epigenetic; Cytoskeletal Signaling |
Decursin (Decursinol angelate) 是一种细胞毒性剂,是一种来自朝鲜当归根的有效蛋白激酶 C 激活剂。它通过 Hippo/YAP 信号通路抑制 HepG2 细胞的生长。它通过下调 CXCR7 表达来抑制胃癌中的肿瘤生长,迁移和侵袭。 | |||
T4716 |
Pyrrole-2-carboxylic acid
吡咯-2-羧酸,2-Pyrrolecarboxylic acid,Minaline |
Endogenous Metabolite | Metabolism |
Pyrrole-2-carboxylic acid (Minaline) 是一种天然生物碱类,从海洋细菌Pelomonas puraquaesp. Nov 中分离得到。 | |||
T4776 |
Glycerol
Glycerin,甘油 |
Endogenous Metabolite | Metabolism |
Glycerol 是甘油三酯(即脂肪和油)和磷脂的重要成分。它在食品工业中被广泛用作甜味剂和保湿剂以及药物制剂。 | |||
T80716 |
α,β-Thujone
|
||
α,β-Thujone为特定植物精油成分,可导致雄性大鼠癌症,高剂量下亦能触发癫痫。 |