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Search Results for " ganglion "

33

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T2026	CYM5442	S1P Receptor; LPL Receptor	GPCR/G Protein
	CYM5442 是高选择性和口服活性的鞘氨醇 1-磷酸受体激动剂，EC50为 1.35 nM。它激活依赖 S1P1的 p42/p44-MAPK 磷酸化，具有视网膜神经保护作用，可轻松穿过中枢神经系统。
T7748	Dermorphin TFA 皮啡肽三氟乙酸盐	Others; Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience; Others
	Dermorphin TFA 是在两栖类皮肤中发现的天然七肽，是 μ-阿片受体激动剂，可用于抑制神经痛。
T22733	DL-AP5 DL-2-氨基-5-膦酰基缬草酸	NMDAR	Neuroscience
	DL-AP5 是选择性 N-甲基-D-天冬氨酸 (NMDA) 受体拮抗剂的外消旋形式，具有抗惊厥作用。
T7404	Dermorphin 皮啡肽	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	Dermorphin 是在两栖类皮肤中发现的天然七肽，是 μ-阿片受体激动剂，可用于抑制神经痛。
TP1283L	VIP(6-28)(human, rat, porcine, bovine) acetate	Others	Others
	VIP(6-28)(human, rat, porcine, bovine) acetate 是外源性血管活性肠肽 (VIP) 受体对颈上神经节 (SCG) 中 cAMP 作用的拮抗剂。
T5913	Sulbutiamine 舒布硫胺,Bisibuthiamine	Antioxidant	oxidation-reduction
	Sulbutiamine (Bisibuthiamine) 是合成的维生素 B1 类似物，可用于研究无力症。
T72662	NMDAR/TRPM4-IN-2	ERK; TRP/TRPV Channel; NMDAR; iGluR	MAPK; Membrane transporter/Ion channel; Neuroscience
	NMDAR/TRPM4-IN-2 是一种有效的 NMDAR/TRPM4 相互作用界面抑制剂。NMDAR/TRPM4-IN-2 保护小鼠免受 MCAO 诱导的脑损伤和 NMDA 诱导的视网膜神经节细胞丢失。NMDAR/TRPM4-IN-2 具有神经保护活性，可预防 NMDA 诱导的海马神经元细胞死亡和线粒体功能障碍，其 IC50 值为 2.1 μM。
TP2393	Neurotensin-related hexapeptide Lant-6
	Neurotensin-related hexapeptide exists in retinal ganglion cells and in their central projections in pigeons and may be utilized as a neuroactive substance by the central terminals of numerous retinal ganglion cells in birds.
T28987	TN-871 HCl TN-871 dihydrochloride,TN871,TN 871,TN-871
	TN-871 is a potassium and calcium channel antagonist. TN-871 modulates transmitter release from preganglionic nerve terminals without changing the postsynaptic sensitivity of the ganglion cells to ACh.
T28431	PNU109291 PNU-109291,PNU 109291
	PNU109291, a potent and selective agonist of the 5-HT1D receptor, effectively mitigates dural plasma extravasation induced by trigeminal ganglion stimulation.
T3289L	Amifostine Hydrate
	Amifostine Hydrate is a radiation protective agent that induces splenic vasodilation and blocks autonomic ganglion.
TP1934	L-R4W2
	Vanilloid TRPV1 (VR1) receptor antagonist peptide (IC50 ~ 0.1 μM); blocks Ca2+ currents in dorsal root ganglion neurons. Analgesic in vivo.
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.
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.
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.
T68811	Trimetaphan camsilate
	Trimetaphan camsilate is a drug that counteracts cholinergic transmission at the ganglion type of nicotinic receptors of the autonomic ganglia and therefore blocks both the sympathetic nervous system and the parasympathetic nervous system. It acts as a non-depolarizing competitive antagonist at the nicotinic acetylcholine receptor, is short-acting, and is given intravenously.
T35889	PB2
	PB2, a tris(2-carboxyethyl)phosphine (TCEP) analogue, enhances the survival of retinal ganglion cells (RGCs) following axotomy in vitro. Even at nanomolar and picomolar concentrations, PB2 demonstrates pronounced efficacy in promoting RGC survival. Notably, PB2 exhibits superior permeability compared to TCEP. Serving as a potent reducing agent, PB2 provides robust neuroprotection for RGCs[1].
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。
T80443	ω-Conotoxin MVIID SNX-238	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	ω-Conotoxin MVIID (SNX-238) 是芋螺肽，能抑制ω-Conotoxin-GVIA敏感的高阈值Ca2+电流于鱼类视网膜神经节细胞。
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
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。
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]。
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。
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。
T35888	PB1
	PB1 is a highly-effective intracellular disulfide reducing agent with notable attributes such as excellent cell permeability, the capacity to generate a substantial intracellular concentration gradient, and remarkable stability. It serves as a borane-protected TCEP (tris(2-carboxyethyl)phosphine) analogue. PB1 demonstrates the potential to enhance the survival of retinal ganglion cells following axotomy in vitro at concentrations in the nanomolar and picomolar range. Consequently, PB1 has proven...
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。
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...
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。
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。
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。

化合物

Cat.No: T2026

Target: S1P Receptor, LPL Receptor

Cat.No: T7748

Synonym: 皮啡肽三氟乙酸盐

Target: Others, Opioid Receptor

Cat.No: T22733

Synonym: DL-2-氨基-5-膦酰基缬草酸

Target: NMDAR

Cat.No: T7404

Synonym: 皮啡肽

Target: Opioid Receptor

VIP(6-28)(human, rat, porcine, bovine) acetate

Cat.No: TP1283L

Target: Others

Cat.No: T5913

Synonym: 舒布硫胺,Bisibuthiamine

Target: Antioxidant

NMDAR/TRPM4-IN-2

Cat.No: T72662

Target: ERK, TRP/TRPV Channel, NMDAR, iGluR

Neurotensin-related hexapeptide

Cat.No: TP2393

Synonym: Lant-6

Cat.No: T28987

Synonym: TN-871 dihydrochloride,TN871,TN 871,TN-871

Cat.No: T28431

Synonym: PNU-109291,PNU 109291

Amifostine Hydrate

Cat.No: T3289L

Cat.No: TP1934

Cat.No: T25110

Synonym: AS-1069562,AS 1069562

Cat.No: TP2070

Cat.No: T37296

Cat.No: T37086

Trimetaphan camsilate

Cat.No: T68811

Cat.No: T35889

Jingzhaotoxin-34

Cat.No: T80428

Target: Sodium Channel

ω-Conotoxin MVIID

Cat.No: T80443

Synonym: SNX-238

Target: Calcium Channel

Cat.No: T16135

Target: Others

6-Iodoamiloride

Cat.No: T79246

Target: Sodium Channel

Hainantoxin-III

Cat.No: T80186

Target: Sodium Channel

ω-Conotoxin CVIB

Cat.No: T80455

Target: Sodium Channel

CSD-CH2(1,8)-NH2

Cat.No: T80421

Target: Opioid Receptor

Cat.No: T35888

Cat.No: T80495

Target: Sodium Channel

Cat.No: T37201

Jingzhaotoxin-V

Cat.No: T80425

Target: Sodium Channel

Cat.No: T80066

Target: Potassium Channel

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

Cat. No.	Product Name	Target	Signaling Pathways
T62265	(+)-Sparteine sulfate pentahydrate
	(+)-sparteine (sulfate pentahydrate) 是一种神经节阻断剂，可以竞争性阻断神经元中烟碱乙酰胆碱受体。
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...
T38179	C16 3'-sulfo Galactosylceramide (d18:1/16:0) C16 3'-sulfo Galactosylceramide (d18:1/16:0)	Others	Others
	C16 3'-sulfo Galactosylceramide (d18:1/16:0)是硫酸盐类糖脂的一种。C16 3'-sulfo Galactosylceramide (d18:1/16:0)是在猪脑和血浆中发现的一种比较丰富的硫化物，在小鼠的整个发育过程中会有所减少。C16 3'-sulfo Galactosylceramide (d18:1/16:0)在体外可抑制视网膜神经节细胞生长。C16 3'-sulfo Galactosylceramide (d18:1/16:0)已被用作量化大鼠小脑和多发性硬化症患者分离的白质中的硫化物的参照物。

天然产物

(+)-Sparteine sulfate pentahydrate

Cat.No: T62265

N-Palmitoyl Glycine

Cat.No: T37219

C16 3'-sulfo Galactosylceramide (d18:1/16:0)

Cat.No: T38179

Synonym: C16 3'-sulfo Galactosylceramide (d18:1/16:0)

Target: Others

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