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抑制剂 & 化合物

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天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T21543	AP 18	TRP/TRPV Channel	Membrane transporter/Ion channel
	AP-18 是选择性的 TRPA1 抑制剂。AP-18 可以抑制 50 μM 肉桂醛诱导的 TRPA1 激活，在小鼠和人中的 IC50 分别为 4.5 μM 和 3.1 μM。AP-18 可以逆转 CFA 诱导的小鼠机械性痛觉过敏。AP-18 可以浓度依赖的方式减弱 30 μM AITC 诱导的 Yo-Pro 摄取(IC50= 10.3 μM)。
T8702	SKF-83566	Dopamine Receptor; 5-HT Receptor; AChR	GPCR/G Protein; Neuroscience
	SKF-83566 是一种具有血脑渗透性和口服活性的 D1 样多巴胺受体拮抗剂和一种较弱的竞争性 5-HT2 受体拮抗剂，Ki 为 11 nM。它是竞争性多巴胺转运蛋白抑制剂，可用于研究帕金森氏症和对尼古丁渴望的缓解的相关研究。
T19940	Sulfoxaflor GF 2372,氟啶虫胺腈,GF 2032,XDE 208	AChR	Neuroscience
	Sulfoxaflor (GF 2032) 是 nAChR1 和 nAChR2 亚型的激动剂，是一种作用于昆虫中枢神经系统的内吸性杀虫剂。 Sulfoxaflor 用于防治吸食汁液的昆虫，如褐飞虱、烟粉虱、桃蚜和棉蚜。
T30824	Cgp 29030A Cgp29030A,Cgp-29030A	Others	Others
	CGP 29030A 是一种新的哌嗪衍生物，具有镇痛活性，对潜在的痛觉背角神经元有显著的抑制作用，可用于研究疼痛性疾病。
T64317	ZZL-7	Serotonin Transporter	Neuroscience
	ZZL-7是一种起效快的抗抑郁药。ZZL-7破坏中缝背核（DRN）神经元一氧化氮合酶（nNOS）和血清素转运蛋白（SERT）之间的相互作用。ZZL-7可以很容易地穿过血脑屏障。ZZL-7在重度抑郁症（MDD）中具有研究价值。
T68025	Zoliprofen	Others	Others
	Zoliprofen 是一种一种高效的且可口服的非甾体抗炎剂，具有抗炎、解热和镇痛活性，对角叉菜素、制霉菌素、刀豆球蛋白A 诱导的大鼠爪水肿，以及抗大鼠兔血清诱导的骨折或背皮水肿具有抑制作用。Zoliprofen 在大鼠和兔子中对胶原蛋白或花生四烯酸引起的血小板聚集方面比布洛芬和非诺洛芬有效20倍。Zoliprofen 对小鼠内毒素诱导的腹泻和花生四烯酸诱导的兔急性死亡抑制作用显著。
TP1934	L-R4W2
	Vanilloid TRPV1 (VR1) receptor antagonist peptide (IC50 ~ 0.1 μM); blocks Ca2+ currents in dorsal root ganglion neurons. Analgesic in vivo.
T28516	ReN-1869 NNC-05-1869,NNC 05-1869,NNC-051869,ReN 1869
	ReN-1869 is a histamine H1 receptor antagonist. ReN 1869 is active against inflammation and neurogenic pain. ReN-1869 produces potent and selective antinociceptive effects on dorsal horn neurons after inflammation and neuropathy.
TP2070	BDS I
	Potent and reversible Kv3.4 potassium channel blocker (IC50 = 47 nM); also attenuates inactivation of sodium currents by acting on Nav1.7 and Nav1.3 channels. Enhances TTX-sensitive sodium currents in rat small dorsal root ganglion neurons. Neuroprotective.
T25110	AS1069562 AS-1069562,AS 1069562
	AS1069562 is an inhibitor of serotonin (5-HT) and norepinephrine (NE) reuptake which acts by notably restoring reduced insulin-like growth factor 1 and fibroblast growth factor 2 mRNA levels in dorsal root ganglion and spinal cord, respectively.
T16135	MRS 1523	Others	Others
	MRS 1523 can exert an antihyperalgesic effect through N-type Ca channel block and action potential inhibition in isolated rat dorsal root ganglion (DRG) neurons. MRS 1523 is an effective and selective adenosine A3 receptor antagonist Ki: 18.9 nM and 113 n
T37296	GI-530159
	TREK1 and TREK2 channel activator (EC50 = 0.76 μM in Rb efflux assay in TREK1-expressing CHO cells). Exhibits selectivity for TREK1/2 over TRAAK, TASK3 and a range of other potassium channels. Hyperpolarizes membrane potential of dorsal root ganglion neurons and depresses neuronal activity in vitro. Loucif et al (2018) GI-530159, a novel, selective, mechanosensitive two-pore-domain potassium (K2P) channel opener, reduces rat dorsal root ganglion neuron excitability. Br.J.Pharmacol. 175 2272 PMID...
T37086	PDDHV
	PDDHV is a resiniferatoxin-type phorboid vanilloid with capsaicin-like selectivity for the cloned rat transient receptor potential cation channel subfamily V member 1 (TRPV1), formerly known as vanilloid receptor 1. It induces Ca2+-uptake by rat dorsal root ganglion neurons with an EC50 value of 70 nM.
T80455	ω-Conotoxin CVIB	Sodium Channel	Membrane transporter/Ion channel
	ω-Conotoxin CVIB为非选择性N型及P/Q型电压门控钙通道(VGCC)拮抗剂，能够抑制背根神经节(DRG)中神经元去极化后激活全细胞VGCC电流，其pIC50值为7.64。
T26564	ADCI SGB-017,SGB017,SGB 017
	ADCI is an inhibitor of voltage-activated sodium channels and N-methyl-D-aspartate (NMDA)-receptor-gated channels. Inhibition of sodium channels by ADCI was voltage dependent. High doses of ADCI increased dopamine metabolism in the prefrontal cortex and/o
T80428	Jingzhaotoxin-34	Sodium Channel	Membrane transporter/Ion channel
	Jingzhaotoxin-34是一种含35个氨基酸残基的多肽神经毒素，能特异性抑制TTX-S钠电流（IC50约85 nM），对大鼠背根神经节TTX-R钠电流无显著作用。
T36859	C16 Globotriaosylceramide (d18:1/16:0) C16 Globotriaosylceramide (d18:1/16:0)
	C16 globotriaosylceramide is an endogenous sphingolipid found in mammalian cell membranes that is synthesized from C16 lactosylceramide . C16 globotriaosylceramide acts as a receptor for Shiga toxin in B cell-derived Raji cells and THP-1 monocytes. It accumulates in endothelial cells, pericytes, vascular smooth muscle cells, renal epithelial cells, dorsal ganglia neuronal cells, and myocardial cells in patients with Fabry disease. C16 globotriaosylceramide is also upregulated in plasma of patien...
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...
T76358	Neuropeptide Y (1-24) (human)
	Neuropeptide Y (1-24) (human) 是一种神经肽，它能够抑制大鼠输精管电刺激引发的抽搐反应，同时在体内刺激 N-methyl-D-aspartate (NMDA) 促使大鼠海马背侧 CA3 区神经元激活。
T79246	6-Iodoamiloride	Sodium Channel	Membrane transporter/Ion channel
	6-Iodoamiloride作为一种有效的酸敏感离子通道1(ASIC1)抑制剂，其IC50值为88 nM。同时，该化合物能够抑制大鼠背根神经节神经元中ASIC3介导的电流，其IC50值为230 nM。
T80185	Huwentoxin I HWTX-I	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	Huwentoxin I (HWTX-I)为一种肽毒素，针对电压门控钠通道和N型钙通道具有抑制作用。该化合物对大鼠海马神经元和蟑螂DUM神经元的钠离子通道展现出抑制能力，其IC50值分别为66.1 nM和4.80 nM。
T75944	Spadin TFA
	Spadin TFA 是一种从血液中释放的前肽衍生的天然肽，是一种有效的 TREK-1 通道阻滞剂，其 IC50值为 10 nM。Spadin TFA 增强小鼠中缝背核 5-HT 神经传递，诱导海马 CREB 激活和神经发生。Spadin TFA 可用于抗抑郁研究。
T80186	Hainantoxin-III	Sodium Channel	Membrane transporter/Ion channel
	Jingzhaotoxin-V是一种多肽，具有抑制作用，IC50值为604.2 nM，可显著抑制非洲爪蟾卵母细胞的钾电流。此外，Jingzhaotoxin-V对大鼠背根神经节神经元中的河豚毒素抗性钠电流和河豚毒素敏感钠电流也有抑制效果，其IC50值分别为27.6 nM和30.2 nM[1]。
TP2136	(d(CH2)51,Tyr(Me)2,Arg8)-Vasopressin
	Selective vasopressin V1A receptor antagonist. Inhibits vasopressin and oxytocin-induced increases in intracellular calcium concentrations in vitro (IC50 values are 5 and 30 nM respectively). Exhibits potent and prolonged antivasopressor activity and indu
T80421	CSD-CH2(1,8)-NH2	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	CSD-CH2(1,8)-NH2 是一种针对KOR的选择性且竞争性拮抗剂，具有较低的Ki值（6.8 nM），能够抑制DRG神经元内的钙动员，并能拮抗U50,488的抗伤害效应，常用于神经精神疾病研究领域。
T80425	Jingzhaotoxin-V	Sodium Channel	Membrane transporter/Ion channel
	Jingzhaotoxin-V是Chilobrachys jingzhao蜘蛛毒液中的一种含29个氨基酸残基的多肽。该化合物抑制大鼠背根神经节神经元的河豚毒素抗性和河豚毒素敏感sodium currents，相应IC50值为27.6 nM与30.2 nM。同时，Jingzhaotoxin-V也能抑制表达在爪蟾卵母细胞中的Kv4.2钾电流，IC50值为604.2 nM。
T83948	Sakura 6
	Sakura 6是一种合成的5-HT转运体(SERT)结合肽，促进SERT与神经元型一氧化氮合酶的相互作用，降低SERT活性和细胞表面的SERT，增加自我抑制，减少突触5-HT释放并降低背侧绕束核的放电。在抑郁症小鼠模型中诱导急性抑郁表型。
T80495	mHuwentoxin-IV	Sodium Channel	Membrane transporter/Ion channel
	mHuwentoxin-IV是一种经天然修饰的Huwentoxin-IV。该化合物针对背根神经节中河豚毒素敏感(TTX-S)电压门控钠通道(sodium channels)表现出抑制作用，IC50值为54.16 nM。mHuwentoxin-IV对这些钠通道的抑制作用并不会因强去极化电压而逆转。
T37439	C18 Globotriaosylceramide (d18:1/18:0)
	C18 globotriaosylceramide is an endogenous sphingolipid found in mammalian cell membranes that is synthesized from lactosylceramide . It inhibits aggregation of human neutrophils induced by phorbol 12-myristate 13-acetate (PMA; 10008014) when used at a concentration of 1 μM. C18 globotriaosylceramide acts as a receptor for Shiga toxin in B cell-derived Raji cells and THP-1 monocytes. It accumulates in the brain, heart, kidney, liver, lung, and spleen in a mouse model of Fabry disease, a lysosoma...
T36185	Globotriaosylceramides (hydroxy) (porcine)
	Globotriaosycleramides are glycosphingolipids found in mammalian cell membranes that are synthesized from lactosylceramides . They act as receptors for Shiga and Shiga-like toxins in vitro and in vivo. Globotriaosylceramides accumulate in endothelial cells, pericytes, vascular smooth muscle cells, renal epithelial cells, dorsal ganglia neuronal cells, and myocardial cells in patients with Fabry disease, a lysosomal storage disorder characterized by a deficiency in the enzyme α-galactosidase A. G...
T36186	Globotriaosylceramides (porcine)
	Globotriaosycleramides are glycosphingolipids found in mammalian cell membranes that are synthesized from lactosylceramides . They act as receptors for Shiga and Shiga-like toxins in vitro and in vivo. Globotriaosylceramides accumulate in endothelial cells, pericytes, vascular smooth muscle cells, renal epithelial cells, dorsal ganglia neuronal cells, and myocardial cells in patients with Fabry disease, a lysosomal storage disorder characterized by a deficiency in the enzyme α-galactosidase A. G...
T80066	ShK toxin	Potassium Channel	Membrane transporter/Ion channel
	ShK toxin 是从加勒比海葵（Stichodactylu helianthus）的全身提取物中分离出的一种蛋白，能够阻断电压依赖性钾通道(Kv1.3 通道)。在竞争实验中，ShK toxin 与树突毒素 I 及α-树突毒素相互竞争，以与大鼠脑突触体膜结合，从而促进乙酰胆碱的释放。此外，ShK toxin 抑制培养的大鼠背根神经节神经元中的K+ 电流，并且能够抑制T淋巴细胞的增殖。
T38042	Resolvin D4 Resolvin D4,RvD4
	Resolvin D4 (RvD4) is a specialized pro-resolving mediator derived from docosahexaenoic acid . [1] It has been detected in human milk, in the dorsal pouch of mice before and after infection with S. aureus, and in untreated tissues from humans, mice, and sardines.[2][3] RvD4, at 10 ng/mouse, reduces neutrophil infiltration in zymosan A-induced peritonitis and, at 200 ng/mouse, diminishes neutrophil infiltration in response to S. aureus infection. [3] With isolated cells, RvD4 promotes phagocytosi...
T83701	TRPV1-Tat TFA Transient Receptor Potential Vanilloid 1-Tat,736-745-Tat
	TRPV1-Tat是一种针对瞬时受体电位范烤苷1 (TRPV1) 的肽类拮抗剂。它由来自TRPV1的A-激酶锚蛋白(AKAP)结合域的736-745个氨基酸以及来自HIV Tat的细胞穿透肽序列组成。TRPV1-Tat (200 µM) 能够在使用初级小鼠背根神经节的整细胞膜片钳技术中抑制由热或棕榈酸酯12-肉豆蔻酸13-醋酸酯(PMA014)引起的电流。当以10或30 µM剂量给药时，它能增加大鼠后爪机械痛阈。
T83909	6-hydroxy Buspirone BMY 28674,BMS-52821
	6-hydroxy Buspirone是抗焦虑化合物buspirone的活性代谢产物，通过细胞色素P450（CYP）亚型CYP3A4从buspirone转化而来。该化合物在大鼠海马和背侧缝核的5-羟色胺（5-HT）受体亚型5-HT1A上具有亲和力（EC50s分别为4和1 µM），并作为多巴胺D2、D3、D4受体拮抗剂（IC50s分别为3.1、4.9、和0.85 µM）。同时，它还以浓度依赖性方式抑制表达人类转运体的S2近端小管细胞中的有机阳离子转运体1（OCT1）、OCT2和OCT3。
T83732	Tat-CBD3A6K TFA
	Tat-CBD3A6K是一种肽类化合物，为N型电压门控钙通道Cav2.2以及collapsin response mediator protein 2 (CRMP2) 蛋白-蛋白相互作用抑制剂Tat-CBD3的衍生物。Tat-CBD3A6K (10 mg/kg) 能够阻止由d4T (stavudine)引发的大鼠抗逆转录病毒神经病痛模型中爪撤回阈值的下降，并减少同一大鼠分离的背根神经节(DRG)神经元的动作电位数量。通过硬膜途径给予Tat-CBD3A6K (30 µM/animal) 能够减少由萜类生物碱辣椒素引发的大鼠硬脑膜血流增加。
T83728	Tat-AKAP79 (326-336) TFA Tat-A-kinase Anchor Protein 79 (326-336)
	Tat-AKAP79 (326-336) 是一种肽，由HIV-1 Tat蛋白质转导域与对应于A-kinase anchor protein 79 (AKAP79) 326至336残基的11个氨基酸肽链相连组成。在200 µM浓度下，能抑制蛋白激酶A (PKA) 或PKC激活诱导的瞬时受体电位钒通道1 (TRPV1) 在分离的大鼠背根神经节 (DRG) 神经元中的敏感化。在体内，Tat-AKAP79 (326-336) 抑制小鼠由甲醛或phorbol 12-myristate 13-acetate (PMA014) 引发的伤害性行为。它还延长了小鼠对辐射热刺激爪子撤回的潜伏期，并在卡拉胶诱导的炎症性疼痛小鼠模型中增加了爪子撤回的机械阈力。
T83739	Myr-Tat-CBD3 TFA Myr-Tat-Calcium Channel-binding Domain 3,N-myristate-Tat-CBD3
	Myr-Tat-CBD3是一种抑制N型电压门控钙通道Cav2.2与collapsin response mediator protein 2 (CRMP2)之间的蛋白-蛋白相互作用的抑制剂。在10 µM的浓度下，该化合物能够约81%地抑制Cav2.2-CRMP2相互作用，并在大鼠初级背根神经节(DRG)神经元中抑制钾诱导的钙流入（IC50约为2.8 µM）。在20 µM的浓度下，Myr-Tat-CBD3能抑制钙电流，但不影响钠电流，在初级DRG神经元中表现出这种特性。经过脊髓内给药，myr-Tat-CBD3（20 µg/5 µl）能够防止大鼠脚掌撤回潜伏期因carrageenan注射而减少。此外，Myr-Tat-CBD3减少大鼠因线索引起的寻求可卡因行为的复发。
T83731	Tat-CBD3 TFA
	Tat-CBD3是一种抑制N型电压门控钙通道Cav2.2与collapsin response mediator protein 2 (CRMP2)之间的蛋白质-蛋白质相互作用的抑制剂。它还能抑制CRMP2与NMDA受体NR2B亚单位之间的蛋白质-蛋白质相互作用。在无细胞实验中，Tat-CBD3 (10 µM)能将Cav2.2-CRMP2相互作用抑制43%，并在免疫共沉淀实验中抑制NMDA受体NR2B亚单位-CRMP2相互作用。它能在初级大鼠背根神经节 (DRG) 神经元中减少约60%的电压诱导钙电流，并在初级大鼠海马神经元中减少谷氨酸诱导的胞内钙水平增加。Tat-CBD3 (20 mg/kg)在大鼠中脑动脉闭塞 (MCAO) 引发的脑缺血模型中减少梗死体积。鞘内给药Tat-CBD3 (20 µg/5 µl)可防止大鼠卡拉胶诱导的热敏感性。
T37127	L-AP4 monohydrate L-AP4 monohydrate
	L-AP4 (L-APB) monohydrate is a potent and specific agonist for the group III mGluRs, with EC50s of 0.13, 0.29, 1.0, 249 μM for mGlu4, mGlu8, mGlu6 and mGlu7 receptors, respectively[1][2]. L-AP4 (5-30 μg, intrathecal inhection 4-5 days) significantly increases the paw withdrawal threshold in response to application of von Frey filaments in eight nerve-ligated rats in a dose-dependent manner. Intrathecal administration of different doses of L-AP4 is not associated with any evident motor dysfunctio...

化合物

Cat.No: T21543

Target: TRP/TRPV Channel

Cat.No: T8702

Target: Dopamine Receptor, 5-HT Receptor, AChR

Cat.No: T19940

Synonym: GF 2372,氟啶虫胺腈,GF 2032,XDE 208

Target: AChR

Cat.No: T30824

Synonym: Cgp29030A,Cgp-29030A

Target: Others

Cat.No: T64317

Target: Serotonin Transporter

Cat.No: T68025

Target: Others

Cat.No: TP1934

Cat.No: T28516

Synonym: NNC-05-1869,NNC 05-1869,NNC-051869,ReN 1869

Cat.No: TP2070

Cat.No: T25110

Synonym: AS-1069562,AS 1069562

Cat.No: T16135

Target: Others

Cat.No: T37296

Cat.No: T37086

ω-Conotoxin CVIB

Cat.No: T80455

Target: Sodium Channel

Cat.No: T26564

Synonym: SGB-017,SGB017,SGB 017

Jingzhaotoxin-34

Cat.No: T80428

Target: Sodium Channel

C16 Globotriaosylceramide (d18:1/16:0)

Cat.No: T36859

Synonym: C16 Globotriaosylceramide (d18:1/16:0)

Cat.No: T37201

Neuropeptide Y (1-24) (human)

Cat.No: T76358

6-Iodoamiloride

Cat.No: T79246

Target: Sodium Channel

Cat.No: T80185

Synonym: HWTX-I

Target: Calcium Channel

Cat.No: T75944

Hainantoxin-III

Cat.No: T80186

Target: Sodium Channel

(d(CH2)51,Tyr(Me)2,Arg8)-Vasopressin

Cat.No: TP2136

CSD-CH2(1,8)-NH2

Cat.No: T80421

Target: Opioid Receptor

Jingzhaotoxin-V

Cat.No: T80425

Target: Sodium Channel

Cat.No: T83948

Cat.No: T80495

Target: Sodium Channel

C18 Globotriaosylceramide (d18:1/18:0)

Cat.No: T37439

Globotriaosylceramides (hydroxy) (porcine)

Cat.No: T36185

Globotriaosylceramides (porcine)

Cat.No: T36186

Cat.No: T80066

Target: Potassium Channel

Cat.No: T38042

Synonym: Resolvin D4,RvD4

Cat.No: T83701

Synonym: Transient Receptor Potential Vanilloid 1-Tat,736-745-Tat

6-hydroxy Buspirone

Cat.No: T83909

Synonym: BMY 28674,BMS-52821

Tat-CBD3A6K TFA

Cat.No: T83732

Tat-AKAP79 (326-336) TFA

Cat.No: T83728

Synonym: Tat-A-kinase Anchor Protein 79 (326-336)

Myr-Tat-CBD3 TFA

Cat.No: T83739

Synonym: Myr-Tat-Calcium Channel-binding Domain 3,N-myristate-Tat-CBD3

Cat.No: T83731

L-AP4 monohydrate

Cat.No: T37127

Synonym: L-AP4 monohydrate

Cat. No.	Product Name	Target	Signaling Pathways
T37219	N-Palmitoyl Glycine
	The acyl amides are a family of endogenous lipids that act as potent modulators of pain and inflammation. The best characterized members of this family are the arachidonoyl amides, which includes N-arachidonoyl ethanolamide (AEA; anandamide). N-palmitoyl glycine (PalGly) contains an 18-carbon saturated fatty acid that is amide-linked to glycine and is structurally similar to the phospholipid-derived N-acyl ethanolamines. Endogenously produced in rat skin and spinal cord, PalGly is present in 100...

天然产物

N-Palmitoyl Glycine

Cat.No: T37219

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