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Cat. No. | Product Name | ||
---|---|---|---|
L2610 | 神经递质受体化合物库 | 1513 compounds | |
1513 种与神经递质受体相关的化合物,用于高通量、高内涵筛选; |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T3290 |
Pikamilone
匹卡米隆,Picamilon,Nicotinoyl-GABA |
Others | Others |
Pikamilone (Picamilon) 是一种智能药物。 | |||
T14571 |
Bifenazate
|
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
Bifenazate 是 GABA 受体的正向变构调节剂。 Bifenazate 是一种杀螨剂,可在 25 ppm 的浓度下控制 100% 的螨虫。 | |||
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。 | |||
T15775 |
Lotilaner
|
GABA Receptor; Parasite | Membrane transporter/Ion channel; Microbiology/Virology; Neuroscience |
Lotilaner 是杀寄生虫剂,是非竞争性的昆虫GABACl 受体拮抗剂,对果蝇 GABA 受体的IC50值为 23.84 nM。对家犬的 GABAA 无明显作用。 | |||
T10618 |
Broflanilide
|
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
Broflanilide 是昆虫抗狄氏剂 GABA 受体拮抗剂,可代谢为 Desmethyl-Broflanilide,抑制斜纹夜蛾 RDL GABAR,IC50值为 1.3 nM。 | |||
TQ0023 |
Lorediplon
|
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
Lorediplon 是一种新型催眠药物,作为 GABAA 受体调节剂,在 α1 亚基上具有差异活性,与促进睡眠有关。 | |||
T4176 |
rac-BHFF
(R,S)-BHFF |
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
rac-BHFF ((R,S)-BHFF) 是具有口服活性的 GABAB 受体的异构增强剂,有抗焦虑活性。 | |||
T16539 |
Piperazine citrate
|
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
Piperazine citrate 是一种六元环化合物,有驱虫的作用。 | |||
T5375 |
Loreclezole
|
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
Loreclezole 是一种选择性 GABAA 受体调节剂,可作为含有 β2 或 β3 亚基的受体的正变构调节剂,有抗癫痫作用。 | |||
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。 | |||
T26600 |
Alpidem
Ananxyl,阿尔吡登 |
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
Alpidem (Ananxyl) 可以选择性结合含有α1β2γ2 亚单位的GABAA 受体,具有抗焦虑作用。 | |||
T17144 |
TPA 023
|
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
TPA 023 是 GABAA α2/α3 亚型的特异性激动剂 (Ki = 0.19 - 0.41 nM)。 | |||
T9424 |
Temgicoluril
Tetramethylglycoluril,mebikar |
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
Temgicoluril (mebikar) 具有抗焦虑活性,作用于GABA 受体。 | |||
T7136 |
AZD-6280
|
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
AZD-6280 是一种新型的亚型选择性 GABAAα2/3 受体阳性调节剂,用于治疗广泛性焦虑症。 | |||
T8572 |
CL 218872
|
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
CL218872 是口服有活性的苯二氮卓类选择性激动剂,激动含有 α1 亚基的GABAA 受体(Ki:130 nM)。它在体内具有抗惊厥及抗焦虑效果。 | |||
T11822 |
LAU159
|
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
LAU159 是一种功能选择性的阳性 α1β3 GABA(A) 受体调节剂,EC50是2.2 μM。 | |||
T3644 |
U93631
|
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
U93631 是一种具有新型化学结构的 GABAA 受体配体,IC50 为 100 nM,它在重组 GABAA 受体中诱导 GABA 诱导的全细胞 Cl 电流快速,这种效果随时间依赖性衰减。 | |||
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。 | |||
T2196 |
Fipronil
氟虫腈,Fluocyanobenpyrazole,Termidor |
P450; GluCls; GABA Receptor | Membrane transporter/Ion channel; Metabolism; Microbiology/Virology; Neuroscience |
Fipronil (Fluocyanobenpyrazole) 是昆虫GABA 受体的选择性拮抗剂,可抑制蟑螂神经元中谷氨酸盐引起的脱敏和非脱敏。在分离的大鼠肝微粒体中,它诱导细胞色素 P450 (CYP) 亚型CYP1A1/2、CYP2B1/2和CYP3A1/2的活性。 | |||
T11349 |
GABAA receptor agent 1
|
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
GABAA receptor agent 1 是GABAA 受体的高亲和力配体,有抗惊厥活性。 | |||
T0715 |
Chlormezanone
Trancopal,氯美扎酮,芬那露 |
Others; GABA Receptor | Membrane transporter/Ion channel; Neuroscience; Others |
Chlormezanone (Trancopal) 是一种非苯二氮卓类药物,用于治疗焦虑症和肌肉痉挛。 | |||
T82357 |
GABA receptor Antagonist 1
|
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
GABA receptorAntagonist 1 (compound 7w) 在抑制PxRDL1GABAR方面具有高特异性,IC50为7.08 nmol/L。针对P. xylostella、S. frugiperda、S. exigua和S. litura的杀虫活性显著,相应的LC50值分别为0.09、0.84、0.87和0.68 mg/L。此化合物对蜜蜂的急性毒性为中等(48小时,LD50=2.22μg/成虫),而对斑马鱼的急性毒性较低(LC50: 42.4mg/L)。 | |||
T1240 |
Flumazenil
Ro 15-1788,氟马西尼 |
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
Flumazenil (Ro 15-1788) 是一种有竞争性的GABAA 受体拮抗剂,以剂量依赖的方式逆转苯二氮卓类药物诱导的作用,包括镇静、精神运动缺陷、健忘和换气不足。 | |||
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。 | |||
T7622 |
Gabazine
SR95531,克他命 |
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
Gabazine (SR95531) 是GABAA 受体的一种选择性竞争性拮抗剂,IC50值约为 0.2 μM。 | |||
T13536 |
Afoxolaner
|
Chloride channel; GABA Receptor; Parasite | Membrane transporter/Ion channel; Microbiology/Virology; Neuroscience |
Afoxolaner 是一种异恶唑啉杀虫剂/杀螨剂,可对抗犬的肩胛硬蜱。 它作用于昆虫的 γ-氨基丁酸(GABA)受体谷氨酸受体,抑制 GABA 和谷氨酸调节的氯离子吸收,导致过度的神经元刺激和节肢动物死亡。 | |||
T23104 |
Ocinaplon
DOV 273547,奥西普隆 |
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
Ocinaplon (DOV 273547) 是一种GABAA 受体的阳性变构调节剂,在 α1 亚基处有较高的活性。 | |||
T1128 |
Oxiracetam
奥拉西坦,ISF2522 |
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
Oxiracetam (ISF2522) 是一种 γ-氨基丁酸 (GABA) 的环状衍生物,可用于治疗认知障碍。 | |||
T12207 |
NEO 376
SPI-376 |
Dopamine Receptor; 5-HT Receptor; GABA Receptor | GPCR/G Protein; Membrane transporter/Ion channel; Neuroscience |
NEO 376 (SPI-376) 是选择性5-HT1 受体、GABA 受体和多巴胺受体调节剂,可用于精神病的研究。 | |||
TQ0040 |
ONO-8590580
CS-2894 |
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
ONO-8590580 (CS-2894) 是一种 GABAA α5 负变构调节剂。 | |||
T2067 |
NS11394
NS 11394 |
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
NS11394 是可口服GABAA 的阳性变构调节剂 (PAM),Ki 值为 0.5 nM。它对GABAA 的选择性依次为 α5、α3、α2 和α1 受体,具有抗炎和抗焦虑活性。 | |||
T8887 |
2'MeO6MF
|
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
2'MeO6MF 是可透过血脑屏障的α2β1γ2L 和所有含α1的GABAA 受体的正变构调节剂。它也可以直接激活α2β2/3和α2β2/3γ2L GABAA 受体。它具有抗焦虑和促进安定作用。它可提供神经保护作用并改善功能恢复,还可抑制中风诱发的炎症反应。 | |||
T11684 |
Isoguvacine hydrochloride
1,2,3,6-tetrahydro-4-pyridinecarboxylic acid hydrochloride,异四氢烟酸 |
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
Isoguvacine hydrochloride (1,2,3,6-tetrahydro-4-pyridinecarboxylic acid hydrochloride) 是 GABA 受体激动剂。它与大鼠突触皮质膜结合并激活 α1β2γ2S、α2β2γ2S、α3β2γ2S、α5β2γ2S 和 ρ1 亚基 GABAA 受体。 | |||
T4363 |
CGP52432
4-苄氧基苯基异硫氰酸酯,CGP 52432 |
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
CGP52432 是一种GABAB 受体拮抗剂,IC50值为 85 nM。 | |||
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。 | |||
T21793 |
CGP 35348
|
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
CGP 35348 是 GABAB 受体的选择性拮抗剂 (EC50 = 34 μM)。 CGP 35348 可用于研究白化新生小鼠脑损伤后的神经肌肉协调和空间学习。 | |||
T7699 |
AZD7325
AZD-7325 |
P450; GABA Receptor | Membrane transporter/Ion channel; Metabolism; Neuroscience |
AZD7325 (AZD-7325) 是具有口服活性的α2和α3受体正向别构调节剂,Ki 分别是 0.3 和 1.3 nM。它是中等 CYP1A2和强效 CYP3A4诱导剂,有用于焦虑和 dravet 综合征相关的研究潜力。 | |||
T6355 |
(R)-baclofen
STX209,Arbaclofen,(R)-巴氯芬 |
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
(R)-baclofen (STX209) 是一种选择性GABAB 受体激动剂。 | |||
T4993 |
Afloqualone
氟喹酮,HQ-495 |
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
Afloqualone (HQ-495) 是一种 GABA 受体激动剂。靶点:体外 GABA 受体:Afloqualone 是一种喹唑啉酮家族 GABA 能药物。由于其在 GABAa 受体β亚型的激动剂活性,它具有镇静和肌肉松弛作用。 | |||
T1860 |
Imepitoin
AWD 131-138,ELB-138,伊匹妥英 |
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
Imepitoin (AWD 131-138) 是一种新型的低亲和力部分苯二氮卓受体激动剂,有抗惊厥和抗焦虑作用。 | |||
T4688 |
Pipequaline hydrochloride
PK-8165 hydrochloride,盐酸哌夸林 |
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
Pipequaline hydrochloride (PK-8165 hydrochloride) 是一种苯二氮卓受体部分激动剂,有抗焦虑作用。 | |||
T13690 |
Etifoxine hydrochloride
盐酸艾替伏辛,HOE 36-801 hydrochloride |
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
Etifoxine hydrochloride (HOE 36-801 hydrochloride) 是GABAA 受体亚基 α1β2γ2 和 α1β3γ2 的阳性变构调节剂,是具有 GABA 能的非苯二氮卓类抗焦虑和抗惊厥药物。 | |||
T0169 |
Nefiracetam
DM9384,奈非西坦,DZL-221 |
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
Nefiracetam (DM9384) 是一种 GABA 能、胆碱能和单胺能神经元系统增强剂,用于治疗 Ro 5-4864 引起的抽搐。 | |||
T12492 |
Pivagabine
CXB-722,匹伐加宾 |
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
Pivagabine (CXB-722) 是疏水性 4-氨基丁酸的衍生物,具有神经调节活性。它可穿透大鼠的血脑屏障,拮抗足部休克对大鼠脑中 GABAA 受体功能和促肾上腺皮质激素释放因子 (CRF) 浓度的影响。 | |||
T0349 |
Riluzole
PK 26124,RP-54274,利鲁唑 |
GABA Receptor; Sodium Channel; NMDAR | Membrane transporter/Ion channel; Neuroscience |
Riluzole (RP-54274) 是一种谷氨酸拮抗剂,用作抗惊厥药并延长肌萎缩侧索硬化症患者的生存期。它还抑制 GABA 摄取,IC50值为 43 μM。 | |||
T2407 |
Tiagabine
噻加宾,TGB,NO050328,Gabitril,NO328 |
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
Tiagabine (NO050328) 是具有抗惊厥特性的选择性 GABA 再摄取抑制剂,在突触体、神经元和神经胶质中,能够抑制 [3H]GABA 的重摄取,IC50值分别为 67、446 和 182 nM。 | |||
T5880 |
Aminooxyacetic acid hemihydrochloride
氨氧基乙酸半盐酸盐,羧甲基羟胺半盐酸盐,Carboxymethoxylamine Hemihydrochloride |
Others; GABA Receptor | Membrane transporter/Ion channel; Neuroscience; Others |
Aminooxyacetic acid hemihydrochloride (Carboxymethoxylamine Hemihydrochloride) 是一种苹果酸-天冬氨酸穿梭 (MAS) 抑制剂,也能抑制 GABA 降解酶GABA-T。 | |||
T11277 |
FG 7142
ZK 39106,LSU-65 |
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
FG 7142 (LSU-65) 是一种非选择性苯二氮卓类反向激动剂,对含 α1 亚基的 GABAA 受体具有高亲和力,Ki 为 91 nM。它还调节 GABA 诱导的 GABAA 受体上的氯离子通量,表达 α1 亚基,EC50为 137 nM。它可增加酪氨酸羟基化并导致小鼠大脑皮层中 β-肾上腺素受体的上调。 | |||
T14983 |
Clomethiazole
Distraneurin,Chlormethiazole,氯美噻唑,5-(2-CHLOROETHYL)-4-METHYLTHIAZOLE |
P450; GABA Receptor | Membrane transporter/Ion channel; Metabolism; Neuroscience |
Clomethiazole (Distraneurin) 是口服GABAA 激动剂,可抑制人肝微粒体中的细胞色素 P450 异构体,CYP2A6 和 CYP2E1。它有抗惊厥作用,具有治疗惊厥性癫痫持续状态的潜力。 | |||
T11307 |
Fluxametamide
4-[5-(3,5-二氯苯基)-4,5-二氢-5-(三氟甲基)-3- 异恶唑基]-N-[(甲氧基氨基)亚甲基]-2-甲基苯 甲酰胺 |
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
Fluxametamide 是广谱杀虫剂,是 GABA-和谷氨酸门控氯离子通道拮抗剂,对 M. domestica 中 GABACl 和 GluCl 的IC50值分别为 1.95 和 225 nM。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TN1023 |
Miltirone
|
P450; GABA Receptor | Membrane transporter/Ion channel; Metabolism; Neuroscience |
Miltirone 是存在于丹参中的一种天然产物,可作为中枢苯二氮受体部分激动剂,IC50值为 0.3 μM。 | |||
TQ0119 |
Cirsimaritin
|
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
Cirsimaritin 具有抗菌、抗炎、抗肿瘤、抗氧化特性和肾脏保护作用。 Cirsimaritin 与 GABAA 受体上的苯二氮卓位点结合较弱。 | |||
T4728 |
4-Acetamidobutanoic acid
N-acetyl GABA,4-ACETAMIDOBUTYRIC ACID,4-乙酰氨基丁酸 |
GABA Receptor; Endogenous Metabolite; Antibacterial | Membrane transporter/Ion channel; Metabolism; Microbiology/Virology; Neuroscience |
4-Acetamidobutanoic acid (4-ACETAMIDOBUTYRIC ACID) 可在血液、粪便和尿液以及人体前列腺组织中找到,也存在于从酵母到人类的所有真核生物中。它是GABA 衍生物,具有抗氧化和抗菌活性。 | |||
T5754 |
Kavain
|
NF-κB; GABA Receptor | Membrane transporter/Ion channel; Neuroscience; NF-κB |
Kavain 是从卡瓦胡椒中分离出来的卡瓦酸内酯,可以正向调控GABAA 受体,具有抗焦虑作用。 | |||
T7557 |
Guvacine hydrochloride
|
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
Guvacine hydrochloride 是从槟榔中得到的一种生物碱,是 GABA 摄取抑制剂,IC50为 10 μM。它对几种克隆的 GABA 转运体具有适度的选择性。 | |||
T3782 |
Jujuboside A
|
transporter; GABA Receptor | Membrane transporter/Ion channel; Metabolism; Neuroscience |
Jujuboside A 是从中药酸枣仁中提取的一种糖苷,可用于失眠和焦虑的相关研究。 | |||
T8036 |
6-Methylflavone
|
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
6-Methylflavone 是α1β2γ2L 和α1β2GABAA 受体激活剂。 | |||
TN1217 |
2'-O-Methylisoliquiritigenin
|
Dopamine Receptor; 5-HT Receptor; GABA Receptor | GPCR/G Protein; Membrane transporter/Ion channel; Neuroscience |
2'-O-Methylisoliquiritigenin 是从洋甘草中分离出来的一种天然产物,是由 NR 中特异性诱导的酶合成的。它上调 5-HT、NE、DA 和 GABA 途径,对 NE 通路有显著影响。 | |||
T3S2100 |
(-)-Securinine
一叶秋碱,Securinine |
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
(-)-Securinine (Securinine) 是来自叶底珠的一种生物碱,也是 GABAA 受体拮抗剂。 | |||
T5799 |
Arecaidine hydrochloride
|
Others | Others |
Arecaidine hydrochloride 是一种具有高效 GABA 吸收抑制功能的吡啶生物碱。它是 H+偶联的氨基酸转运蛋白 1 (PAT1,SLC36A1) 的底物,能够竞争性抑制 L-脯氨酸的摄取。 | |||
T2979 |
DL-Menthol
DL-薄荷醇,Hexahydrothymol,(±)-Menthol,薄荷醇 |
GABA Receptor; AChE | Membrane transporter/Ion channel; Neuroscience |
DL-Menthol ((±)-Menthol) 是单萜醇 (–)-薄荷醇和 (+)-薄荷醇的外消旋混合物,已在大麻中发现。它与 GABAA 受体的激活有关。 | |||
T2720 |
Ginsenoside Rc
Panaxoside Rc,人参皂苷Rc,人参皂苷 Rc |
Others; TNF; GABA Receptor; Interleukin | Apoptosis; Immunology/Inflammation; Membrane transporter/Ion channel; Neuroscience; Others |
Ginsenoside Rc (Panaxoside Rc) 是人参中的一种人参皂苷,可抑制 TNF-α 和 IL-1β 的表达。它增强 GABA 受体 A 介导的离子通道电流。 | |||
T0508 |
γ-Aminobutyric acid
Gamma-aminobutyric acid,4-Aminobutyric acid,4-氨基丁酸,γ-氨基丁酸,GABA,4-Aminobutanoic acid,Piperidic acid |
GABA Receptor; Endogenous Metabolite | Membrane transporter/Ion channel; Metabolism; Neuroscience |
γ-Aminobutyric acid (4-Aminobutyric acid) 是成年哺乳动物大脑中主要的抑制性神经递质,能够与离子移变 GABA 受体(GABAA) 受体和促代谢受体 (GABAB) 受体结合发挥作用。 | |||
T8268 |
6,2'-Dihydroxyflavone
6,2-二羟基黄酮,6,2'-二羟基黄酮 |
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
6,2'-Dihydroxyflavone 是一种新型GABAA 受体拮抗剂。 | |||
T1396 |
Bemegride
贝美格,Bemegrid,3-Ethyl-3-methylglutarimide,Agipnon |
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
Bemegride (3-Ethyl-3-methylglutarimide) 是一种中枢神经系统兴奋剂和巴比妥类中毒的解毒剂。 | |||
T2850 |
Bicuculline
荷包牡丹碱,(+)-Bicuculline,d-Bicuculline |
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
Bicuculline ((+)-Bicuculline) 是从东北延胡索中提取的一种生物碱,能阻断 Ca2+激活钾 (SK) 通道。它是一种竞争性的神经递质 GABAA 受体拮抗剂,IC50为 2 μM。 | |||
T2749 |
Ginkgolide A
银杏内酯A,BN-52020 |
GABA Receptor; Endogenous Metabolite | Membrane transporter/Ion channel; Metabolism; Neuroscience |
Ginkgolide A (BN-52020) 是从银杏叶提取出来的一种天然产物,是 GABA 拮抗剂,有用于多种炎症和免疫疾病的研究潜力。 | |||
T5S1882 |
Songorine
准葛尔乌头碱,Napellonine,Zongorine,Bullatine G |
Others; GABA Receptor | Membrane transporter/Ion channel; Neuroscience; Others |
Songorine (Napellonine) 是从乌头属中分离出的一种二萜生物碱,具有抗癌、抗心律不齐和抗炎活性。它是大鼠脑中的GABAA 受体拮抗剂,有用于上皮性卵巢癌的研究潜力。 | |||
TMS0418 |
Dihydroergotoxine mesylate
甲磺酸二氢麦角碱,Ergoloid mesylates,甲磺酸双氢麦角毒碱 |
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
Dihydroergotoxine mesylate (Ergoloid mesylates) 是系列生物碱盐混合物,对GABAA 受体高结合活性。它主要用于改善与衰老相关的精神退化的症状和身体症状。 | |||
T3698 |
alpha-Asarone
α-Asarone,trans-Asarone,α-细辛脑 |
P450; GABA Receptor; HMG-CoA Reductase | Membrane transporter/Ion channel; Metabolism; Neuroscience |
alpha-Asarone (trans-Asarone) 是来自胡萝卜的一种天然产物,具有抗抑郁等功效。 | |||
TN1202 |
(-)-α-Pinene
左旋-α-蒎烯,左旋-alpha-蒎烯,(1S)-(-)-Alpha-Pinene |
Virus Protease; GABA Receptor; Endogenous Metabolite; Antibacterial | Membrane transporter/Ion channel; Metabolism; Microbiology/Virology; Neuroscience |
(-)-α-Pinene ((1S)-(-)-Alpha-Pinene) 是一种单萜类化合物,通过延长 GABAergic 突触传递、作为 GABAA-BZD 受体的部分调节剂并直接与 GABAA 受体的 BZD 结合位点结合来增强 NREMS 的数量而不影响 NREMS 的强度。 | |||
TN1325 |
(2S)-6-Prenylnaringenin
(2S)-6-异戊烯基柚皮素,6-异戊二烯基柚皮素,6-Prenylnaringenin,6-PN |
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
(2S)-6-Prenylnaringenin (6-Prenylnaringenin) 是强效植物雌激素 8-prenylnaringenin 的异构体,是前脑中最有效的化合物,在 α+β 结合位点上起GABAA 正变构调节剂的作用。 | |||
T4590 |
(+)-Kavain
醉椒素,Kavain,L-KAWAIN,(R)-KAWAIN |
Calcium Channel; GABA Receptor; Sodium Channel; Monoamine Transporter | Membrane transporter/Ion channel; Metabolism; Neuroscience |
(+)-Kavain ((R)-KAWAIN) 是从卡瓦胡椒中提取的一种主要的卡瓦内酯,可通过电压依赖性的 Na+和 Ca2+通道相互作用,减弱血管平滑肌的收缩,具有抗惊厥作用。它可与α4β2δ GABAA 受体结合,加强 GABA 的功效,用于炎症疾病研究。 | |||
T7595 |
L-DABA
L-2,4-Diaminobutyric acid,L-2,4-二氨基丁酸氢溴酸盐,L-DAB HBR |
GABA Receptor; Endogenous Metabolite | Membrane transporter/Ion channel; Metabolism; Neuroscience |
L-DABA (L-2,4-Diaminobutyric acid) 是GABA 转氨酶的弱抑制剂,IC50值大于500 μM,具有抗肿瘤活性。 | |||
T8040 |
Cholesterol myristate
胆甾烯基豆蔻酸酯,Cholesteryl myristate,胆固醇肉豆蔻酸,Cholesteryl tetradecanoate |
Others; Potassium Channel; GABA Receptor; Endogenous Metabolite; AChR | Membrane transporter/Ion channel; Metabolism; Neuroscience; Others |
Cholesterol myristate (Cholesteryl myristate) 是粗吻海龙中的一种类固醇,可与多种离子通道结合,例如nAChR、GABAA 受体和内向整流钾离子通道。 | |||
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。 | |||
T8193 |
α-Thujone
Thujone,ALPHA-(-)-THUJONE,α-侧柏酮,(-)-α-侧柏酮 |
Apoptosis; Reactive Oxygen Species; GABA Receptor; AChR; Parasite; Autophagy | Apoptosis; Autophagy; Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Microbiology/Virology; Neuroscience; NF-κB |
α-Thujone 是一种从西方金钟柏精油中分离出来的单萜,可穿透血脑屏障。它是 GABAA 受体的可逆调节剂,在抑制 GABA 诱导的电流时,它的 IC50为 21 μM。它诱导 ROS 依赖性细胞毒性,还诱导细胞凋亡和自噬。它具有抗伤害,抗肿瘤、杀虫和驱虫活性。 | |||
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。 | |||
T0710 |
L-Cycloserine
Levcycloserine,Levcicloserina,(-)-Cycloserine,(S)-Cycloserine,Levcycloserinum,环丝氨酸,(S)-4-Amino-3-isoxazolidone |
HIV Protease; GABA Receptor | Membrane transporter/Ion channel; Microbiology/Virology; Neuroscience; Proteases/Proteasome |
L-Cycloserine ((-)-Cycloserine) 不可逆地抑制大肠杆菌以及各种动物大脑中的 GABA 吡哆醛 5'-磷酸依赖性转氨酶,导致体内抑制性神经递质 γ-氨基丁酸水平升高。 | |||
T2S1814 |
p-Hydroxybenzaldehyde
4-Formylphenol,4-羟基苯甲醛;对羟基苯甲醛,4-hydroxybenzaldehyde,对羟基苯甲醛,p-Oxybenzaldehyde |
Transaminase; GABA Receptor; Endogenous Metabolite | Membrane transporter/Ion channel; Metabolism; Neuroscience |
p-Hydroxybenzaldehyde (p-Oxybenzaldehyde) 是从天麻中提取的一种天然产物,对 GABA 转氨酶有抑制作用,有助于抗癫痫和抗惊厥活性。 | |||
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。 | |||
T3417 |
Amentoflavone
Didemethyl-ginkgetin,穗花杉双黄酮,Amenthoflavone,3',8''-Biapigenin |
Apoptosis; P450; Phospholipase; Reactive Oxygen Species; Opioid Receptor; COX; Antibacterial; RSV; Antifungal | Apoptosis; Endocrinology/Hormones; GPCR/G Protein; Immunology/Inflammation; Metabolism; Microbiology/Virology; Neuroscience; NF-κB |
Amentoflavone (3',8''-Biapigenin) 是一种具有很多生物活性的双黄酮类天然产物,有抗炎、抗氧化和神经保护等作用。 | |||
T3741 |
(-)-borneol
L-Borneol,冰片 |
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
(-)-borneol (L-Borneol) 对 GABA 受体具有高效的正向调节作用,EC50 为 237 μM。 | |||
TN3174 |
6-Methoxyflavanone
NSC50184 |
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
6-Methoxyflavanone(6-MeOF)是人重组GABA A受体GABA反应的正变构调节剂,具有抗焦虑活性和抗炎活性,可用于减轻顺铂诱导的神经性疼痛。 | |||
T5776 |
pimpinellin
|
Apoptosis; Anti-infection | Apoptosis; Microbiology/Virology |
Pimpinellin 是贯众的一种成分,可通过诱导肿瘤细胞凋亡抑制肿瘤细胞的生长,可作为具有 GABA 受体活性的蛋白质的拮抗剂。 | |||
T5734 |
(+)-BORNEOL
d-Borneol,(+)-冰片 |
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
(+)-BORNEOL (d-Borneol) 是一种天然的双环单萜,在中药中用于镇痛和麻醉;增强 GABA 受体活性,EC50 为 248 μM。 | |||
T4S1616 |
Sanggenon D
Sanggenone D |
GABA Receptor; Antibiotic | Membrane transporter/Ion channel; Microbiology/Virology; Neuroscience |
Sanggenon D (Sanggenone D) 是来自桑白皮的小分子化合物,是GABA(A)受体调节剂,具有抗氧化抗菌活性,抑制乳腺癌细胞增殖,通过调节脂肪酸生物合成系统来抑制金黄色葡萄球菌的生长。 | |||
T4881 |
Phosphorylethanolamine
O-Phosphorylethanolamine,乙醇胺磷酸酯 |
Others; Endogenous Metabolite | Metabolism; Others |
Phosphorylethanolamine (O-Phosphorylethanolamine) 是磷脂代谢的一种磷酸单酯代谢物。Phosphorylethanolamine 是磷脂合成的前体,也是磷脂分解的产物。与其他器官相比,大脑中磷酸单酯的含量要高得多。在大脑发育过程中,磷单酯通常在神经增生期间升高。这也与大脑发育过程中正常的程序性细胞死亡和突触修剪的发生相吻合。这些发现与磷酸单酯在膜生物合成中的作用是一致的。Phosphorylethanolamine 与抑制性神经递质GABA和GABAB受体部分激动剂 3-氨基丙基膦酸具有很强的结构相似性。Phosphorylethanolamine 是一种磷单酯,在阿尔茨海默病患者的大脑中减少。 | |||
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。 | |||
T75557 |
Withasomniferolide B
|
Others | Others |
Withasomniferolide B 是一种睡茄内酯。Withasomniferolide B 可以从 Withania somnifera 根部的 GABAA 受体阳性激活剂甲醇提取物中分离出来。 | |||
TN7559 |
Milbemectin
Milbemycin A3 (~30%) and Milbemycin A4 (~70%) Mixture |
Others | Others |
Milbemectin is composed of 30% milbemycin A3 and 70% milbemycin A4, exhibiting acaricidal and nematocidal properties effective against adult spider mites, their eggs, and C. elegans, with IC50 values of 5.3, 41.1, and 9.5 µg/ml, respectively. It functions as an allosteric agonist of the Drosophila RDL GABA receptor, and demonstrates efficacy against the pinewood nematode, B. xylophilus, with an LC20 of 0.0781 mg/liter. | |||
TN3351 |
Aflatrem
|
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
Aflatrem is a tremorgenic mycotoxin with acute neurotoxic effects, a single low dose of aflatrem is able to induce degeneration of neuronal processes in hippocampal neurotransmitter systems. Aflatrem potentiates the gamma-aminobutyric acid (GABA)-induced |
Cat. No. | Product Name | Species | Expression System |
---|---|---|---|
TMPY-00587 |
GABARAP Protein, Human, Recombinant (His & MBP)
GABARAP-a,GABA(A) receptor-associ... |
Human | E. coli |
The Atg8/LC3/GABARAP family of proteins, a group that has structural homology with ubiquitin, connects with a large set of binding partners to function in macroautophagy (hereafter autophagy). GABARAP in tumorigenesis in vivo by delaying cell death and its associated immune-related response. GABARAPs are uniquely required for antimicrobial host defense through cytosolic distribution of interferon-inducible GTPases. GABARAPs as the first known direct interaction partners of Nef that are essential... | |||
TMPJ-00015 |
GABARAP Protein, Human, Recombinant (His & hFc)
GABA(A) Receptor-Associated Protein,HCG198... |
Human | E. coli |
GABARAP Protein, Human, Recombinant (His & hFc) is expressed in E. coli expression system with N-6xHis and C-Fc tag. The predicted molecular weight is 50 KDa and the accession number is Q6IAW1. | |||
TMPJ-00016 |
GABARAP Protein, Human, Recombinant (GST)
GABARAP,GABA(A) Receptor-Associat... |
Human | E. coli |
GABARAP Protein, Human, Recombinant (GST) is expressed in E. coli expression system with N-GST tag. The predicted molecular weight is 37 KDa and the accession number is Q6IAW1. | |||
TMPH-01368 |
GABRP Protein, Human, Recombinant (His)
GABRP,GABA(A) receptor subunit pi,Gamma-am... |
Human | E. coli |
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel. In the uterus, the function of the receptor appears to be related to tissue contractility. The binding of this pI subunit with other GABA(A) receptor subunits alters the sensitivity of recombinant receptors to modulatory agents such as pregnanolone. GABRP Protein, Human, Recombinant (His) is expressed in E. coli... | |||
TMPH-01367 |
GABRB2 Protein, Human, Recombinant (His)
GABA(A) receptor subunit beta-2,GABRB2,Gam... |
Human | E. coli |
GABRB2 Protein, Human, Recombinant (His) is expressed in E. coli expression system with N-6xHis tag. The predicted molecular weight is 29.3 kDa and the accession number is P47870. | |||
TMPH-01366 |
GABRA1 Protein, Human, Recombinant (His)
GABRA1,GABA(A) receptor subunit alpha-1,Ga... |
Human | E. coli |
GABRA1 Protein, Human, Recombinant (His) is expressed in E. coli expression system with N-6xHis tag. The predicted molecular weight is 29.9 kDa and the accession number is P14867. | |||
TMPY-03991 |
DBI Protein, Human, Recombinant (His)
diazepam binding inhibitor (GABA receptor ... |
Human | E. coli |
The diazepam binding inhibitor (DBI), alternatively known as the acyl-CoA binding protein (ACBP), is involved in multiple biological actions. The polypeptide binds to the peripheral, or mitochondrial, benzodiazepine receptor and facilitates transport of cholesterol to the inner membrane to stimulate steroid synthesis. Through this action, DBI indirectly modulates gamma-aminobutyric acid (GABA)-mediated inhibitory neurotransmission. DBI can be postulated as a candidate gene for psychiatric phenot... | |||
TMPY-03461 |
GABARAPL2 Protein, Human, Recombinant (His)
GATE16,ATG8,ATG8C,GEF-2,GATE-16,GEF2,GABA(A) re... |
Human | E. coli |
GATE-16, also known as ATG8, belongs to the MAP1 LC3 family. It is expressed at high levels in the brain, heart, prostate, ovary, spleen and skeletal muscle. GATE-16 is expressed at very low levels in lung, thymus and small intestine. GATE-16 is involved in intra-Golgi traffic. It modulates intra-Golgi transport through coupling between NSF activity and SNAREs activation. It first stimulates the ATPase activity of NSF which in turn stimulates the association with GOSR1. | |||
TMPY-03268 |
GABARAPL1 Protein, Human, Recombinant (His)
GEC1,APG8-LIKE,APG8L,ATG8,ATG8B,ATG8L,GABA(A) r... |
Human | E. coli |
ATG8, also known as GABARAPL1, is a ubiquitin-like protein that has a crystal structure. ATG8 consists of a 5-stranded β-sheet, which is enclosed by two α-helices at one side and one α-helix at the other side and exhibits a conserved GABARAP domain. It functions in the formation of autophagosomal membranes. The transient conjugation of ATG8 to the autophagosomal membrane through a ubiquitin-like conjugation system is essential for autophagy in eukaryotes. Autophagy is induced upon nutrient deple... | |||
TMPH-03235 |
DBI Protein, Rat, Recombinant (His & Myc)
Endozepine (EP),ACBP,DBI,Acyl-CoA-binding protein,Diazepam-b... |
Rat | E. coli |
Binds medium- and long-chain acyl-CoA esters with very high affinity and may function as an intracellular carrier of acyl-CoA esters. It is also able to displace diazepam from the benzodiazepine (BZD) recognition site located on the GABA type A receptor. It is therefore possible that this protein also acts as a neuropeptide to modulate the action of the GABA receptor. DBI Protein, Rat, Recombinant (His & Myc) is expressed in E. coli expression system with N-10xHis and C-Myc tag. The predicted mo... | |||
TMPH-00890 |
DBI Protein, Human, Recombinant (aa 2-104, His)
Acyl-CoA-binding protein,Diazepam-binding inhibitor,DBI,Endo... |
Human | E. coli |
Binds medium- and long-chain acyl-CoA esters with very high affinity and may function as an intracellular carrier of acyl-CoA esters. It is also able to displace diazepam from the benzodiazepine (BZD) recognition site located on the GABA type A receptor. It is therefore possible that this protein also acts as a neuropeptide to modulate the action of the GABA receptor. DBI Protein, Human, Recombinant (aa 2-104, His) is expressed in E. coli expression system with N-6xHis tag. The predicted molecul... | |||
TMPH-02492 |
DBI Protein, Mouse, Recombinant (His & Myc)
Endozepine (EP),Diazepam-binding inhibitor,DBI,Acyl-CoA-bind... |
Mouse | E. coli |
Binds medium- and long-chain acyl-CoA esters with very high affinity and may function as an intracellular carrier of acyl-CoA esters. It is also able to displace diazepam from the benzodiazepine (BZD) recognition site located on the GABA type A receptor. It is therefore possible that this protein also acts as a neuropeptide to modulate the action of the GABA receptor. DBI Protein, Mouse, Recombinant (His & Myc) is expressed in E. coli expression system with N-10xHis and C-Myc tag. The predicted ... | |||
TMPY-00186 |
GHRH Protein, Human, Recombinant (hFc)
GRF,INN,growth hormone releasing hormone,GHRF |
Human | HEK293 Cells |
The role of hypothalamic growth hormone-releasing hormone (GHRH) in the release of growth hormone (GH) from the pituitary is well established. Extra-hypothalamic growth hormone-releasing hormone (GHRH) plays an important role in infertility. Growth hormone releasing hormone (GHRH) has recently been shown to increase the level of gamma-aminobutyric acid (GABA) and activate GABA receptors (GABARs) in the cerebral cortex. GABA is an inhibitory neurotransmitter that can inhibit seizures. GHRH may pl... | |||
TMPH-01248 |
ADAR Protein, Human, Recombinant (His & SUMO)
ADAR1,IFI-4,136 kDa double-stranded RNA-binding protein,Inte... |
Human | E. coli |
Catalyzes the hydrolytic deamination of adenosine to inosine in double-stranded RNA (dsRNA) referred to as A-to-I RNA editing. This may affect gene expression and function in a number of ways that include mRNA translation by changing codons and hence the amino acid sequence of proteins; pre-mRNA splicing by altering splice site recognition sequences; RNA stability by changing sequences involved in nuclease recognition; genetic stability in the case of RNA virus genomes by changing sequences duri... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TMID-0115 |
Dehydroepiandrosterone-2,2,3,4,4,6-d6
DHEA-d6 |
||
Dehydroepiandrosterone-2,2,3,4,4,6-d6 是 Dehydroepiandrosterone 的氘代化合物。Dehydroepiandrosterone 的 CAS 号为 53-43-0。Dehydroepiandrosterone 是一种类固醇激素。它通过多种信号传导途径介导其作用,并通过转化成雄激素和雌激素衍生物(例如,雄激素,雌激素,7α和7β DHEA (Prasterone),以及7α和7β表雄甾酮衍生物)在特异性受体上起作用。 |