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Search Results for " nociception "

33

抑制剂 & 化合物

1

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T7775	A2764 dihydrochloride	Potassium Channel	Membrane transporter/Ion channel
	A2764 dihydrochloride 是高选择性的TRESK (K2P18.1)抑制剂，对 TREK-1 和 TALK-1 有抑制作用。它相比基底 mTRESK 电流，对激活渠道更敏感 (IC50= 6.8 μM)。它可导致细胞去极化，增加细胞的兴奋性，在探索 TRESK 通道在偏头痛和痛觉中的作用中具有研究的价值。
T2024	A-803467 A 803467,A803467	Sodium Channel	Membrane transporter/Ion channel
	A-803467 是有效的、选择性的河豚毒素不敏感型Nav1.8 钠通道阻断剂。它在炎症性疼痛和神经性疼痛模型中有缓解疼痛作用。它通过与 ATP-binding cassette subfamily G member 2 (ABCG2) 转运蛋白的相互作用，增强了传统抗癌物的化疗敏感性。
T0692	Allopurinol Zyloric,别嘌醇,Zyloprim,Lopurin,别嘌呤醇	ROS; Xanthine Oxidase	Immunology/Inflammation; Metabolism
	Allopurinol (Zyloric) 是一种黄嘌呤氧化酶(XO)抑制剂，IC50=7.82±0.12 μM。
T6376	Allopurinol Sodium 1H-吡唑并[3,4-D]嘧啶-4-醇单钠盐,Allopurinol sodium salt,Sodium allopurinol	ROS	Immunology/Inflammation
	Allopurinol Sodium 是黄嘌呤氧化酶抑制剂，其IC50= 0.2~50 μM。它能够抗利什曼原虫，也可用于研究痛风以及高尿酸血症。
T1790	Fosaprepitant dimeglumine 福沙匹坦二甲葡胺,L785298,福沙吡坦二甲葡胺,MK-0517,Fosaprepitant dimeglumine salt	Neurokinin receptor	GPCR/G Protein; Neuroscience
	Fosaprepitant dimeglumine (MK-0517) 是 Aprepitant 的前药。它是一种神经激肽 1 受体拮抗剂，可用于预防化疗引起的恶心呕吐。
T7173	[Leu5]-Enkephalin 亮氨酸脑啡肽,Leucine enkephalin,Leucyl-enkephalin,Leu-enkephalin	Opioid Receptor; Endogenous Metabolite	Endocrinology/Hormones; GPCR/G Protein; Metabolism; Neuroscience
	[Leu5]-Enkephalin (Leu-enkephalin) 是一种参与伤害感受的内源性神经肽，是 δ-阿片和 μ-阿片受体的激动剂，Ki 值分别为 4.0 和 3.4 nM
T15192	Eact	Chloride channel	Membrane transporter/Ion channel
	Eact 是一种选择性和有效的 TMEM16A 激活剂，可直接激活感觉伤害感受器中的 TRPV1 通道，还会产生瘙痒、急性伤害感受和热过敏。
T39529	AT-121 hydrochloride	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	AT-121 hydrochloride 是一种 nociception 和 mu 阿片受体 (mu opioid receptor)的双重激动剂，Ki 值分别为 3.67 和 16.49 nM。AT-121 hydrochloride 是一种安全、无成瘾性且科缓解疼痛的化合物，具有抗伤害和止痛活性。
T7173L	[Leu5]-Enkephalin acetate(58822-25-6 free base) 亮氨酸脑啡肽,Leucine enkephalin,Leu-enkephalin,Leucyl-enkephalin	Opioid Receptor; Endogenous Metabolite	Endocrinology/Hormones; GPCR/G Protein; Metabolism; Neuroscience
	[Leu5]-Enkephalin acetate(58822-25-6 free base) 是一种参与伤害感受的内源性神经肽，是 δ-opioid 和 μ-opioid 受体的激动剂(Kis 分别为 4.0 和 3.4 nM)
T9955	EX-A5758	NOS	Immunology/Inflammation
	EX-A5758是一种新型推定的小分子 nNOS-NOS1 AP 抑制剂，可抑制炎症性伤害感受和化疗引起的神经性疼痛，并与紫杉醇协同降低肿瘤细胞活力
T3690	A-740003 A 740003	P2X Receptor	Membrane transporter/Ion channel; Neuroscience
	A-740003 (A 740003) 是一种选择性和竞争性的P2X7 受体拮抗剂，抑制大鼠和人的 P2X7 受体，IC50值分别为 18 和 40 nM。
T68141	Seganserin	5-HT Receptor	GPCR/G Protein; Neuroscience
	Seganserin 是一种非选择性5-羟色胺2-HT 受体拮抗剂，可逆转了氟西汀和喹帕嗪对黄体酮诱导的食欲亢进，抑郁和痛觉的抑制作用，逆转氟西汀和喹帕嗪诱导的抗抑郁和镇痛作用。
TP1083L	Neuromedin U (rat) acetate	Others	Others
	Neuromedin U (rat) acetate 是一种 23 个氨基酸的脑肠肽。 Neuromedin U (NMU) 通过其在中枢神经系统中的同源受体 NMUR2 调节几种重要的生理功能，包括能量平衡、压力反应和伤害感受。
TP2015L	HS 014 acetate(207678-81-7 free base)	Melanocortin Receptor	GPCR/G Protein; Neuroscience
	HS 014 acetate(207678-81-7 free base) 是一种有效的选择性黑皮质素 MC4 受体拮抗剂（克隆的人 MC4、MC1、MC3 和 MC5 受体的 Ki 值分别为 3.16、108、54.4 和 694 nM）。体内中枢给药后增加大鼠的食物摄入和小鼠的伤害感受。还抑制室旁下丘脑中 IL-1β 诱导的 Fos 表达。
T30239	Axomadol hydrochloride
	Axomadol hydrochloride has an effect on pupil diameter and nociception in healthy subjects.
TP1083	Neuromedin U, rat Rat neuromedin U-23,Neuromedin U (rat)
	Neuromedin U,a 23-amino acid brain-gut peptide, regulates several important physiological functions through its cognate receptor NMUR2 in the central nervous system, including energy balance, stress response, and nociception.
T26475	A-286501
	A-286501 is an orally active adenosine kinase inhibitor (IC50=0.47 nM). A-286501 effectively attenuates nociception by a non-opioid, non-non-steroidal anti-inflammatory drug ADO, receptor mediated mechanism.
T39527	Se-DMC
	Se-DMC effectively reduces the inflammatory response, nociception, and neurobehavioral deficits induced by complete Freund's adjuvant (CFA) in mice.
TP2015	HS014 HS 014
	Potent and selective melanocortin MC4 receptor antagonist (Ki values are 3.16, 108, 54.4 and 694 nM for cloned human MC4, MC1, MC3 and MC5 receptors respectively). Increases food intake in rats and nociception in mice following central administration in v
T61130	SSTR4 agonist 3
	SSTR4 agonist 3 is a potent compound that activates the SSTR4 receptor. The SSTR4 receptor is highly expressed in the hippocampus and neocortex, which are regions associated with memory, learning, and Alzheimer's disease pathology. SSTR4 agonists demonstrate strong efficacy in rodent models of pain, both acute and chronic, by reducing peripheral nociception and inflammation. Considering its potential application in pain research, SSTR4 agonist 3 is of interest[1].
T76484	[Tyr8,Nle11] Substance P
	[Tyr8,Nle11] Substance P 是 Substance P 的类似物。Substance P 是一种主要由神经元分泌的肽，参与许多生物学过程，包括痛觉和炎症。
T60305	ZLc-002
	ZLc-002 是一种选择性的 nNOS-Capon 偶联小分子抑制剂。ZLc-002 抑制炎症和化疗引起的神经性疼痛。ZLc-002 可用于焦虑和炎症研究。
T36719	D-NAME (hydrochloride)
	N(G)-Nitro-D-arginine methyl ester (D-NAME) is the less active enantiomer of the nitric oxide (NO) synthase inhibitor N(G)-nitro-L-arginine methyl ester . D-NAME was initially thought to be inactive and was often used as a negative control for L-NAME. Later studies showed that D-NAME (40 mg/kg/day in rats) can have similar but less pronounced effects as L-NAME (40 mg/kg/day in rats) in the cardiovascular system, particularly at long-term timepoints. D-NAME (3-10 &#181g/mouse) had no effect on no...
T78004	Neuromedin U, rat TFA Rat neuromedin U-23 TFA,Neuromedin U (rat) (TFA)
	Neuromedin U, rat TFA 是一脑肠肽类化合物，含23个氨基酸，主要通过中枢神经系统内的NMUR2同源受体，调控多项生理功能，如能量平衡、应激反应及伤害感知。
T37610	AT-121	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	AT-121 是一种双重μ-阿片和神经肽受体部分激动剂（Kis 分别为 16.49 和 3.67 nM）。它能刺激[35S]GTPγS 与表达μ-阿片受体或神经肽受体的细胞膜结合（EC50s 分别为 19.6 和 34.7 nM）。AT-121（0.003-0.03 mg/kg）能以剂量依赖的方式降低辣椒素诱导的热异感，但不会增加恒河猴的搔抓活动。在恒河猴药物自我给药试验中，AT-121 每次注射剂量为 0.3 至 10 μg/kg，它缺乏强化作用（一种潜在的滥用标志），不能减少食物颗粒的强化作用。AT-121（0.01 或 0.03 毫克/千克）不会诱发恒河猴的超痛觉，超痛觉是产生耐受性的标志。AT-121 是一种安全、无成瘾性的缓解疼痛药，具有抗伤害和止痛作用。
T78734	Sigma-1 receptor antagonist 5	Sigma receptor	GPCR/G Protein
	Sigma-1 receptor antagonist 5 (compound 12) 是一种 4-吡啶衍生物，既有镇痛活性也是 sigma 受体 (Ki=4.5 nM (σ1R)，10 nM (σ2R)) 及组胺 H3 (hH3R，Ki=7.7 nM，IC50=215 nM) 的拮抗剂。它能够抑制辣椒素引起的痛觉，并展现出对伤害性和神经性疼痛模型的显著疗效。
T38077	TLQP-21 TFA
	TLQP-21 TFA, a VGF-derived peptide endowed of endocrine and extraendocrine properties, is a potent G-protein-coupled receptor complement-3a receptor1 (C3aR1) agonist (EC50: mouse TLQP-21=10.3 μM; human TLQP-21=68.8μM). TLQP-21 TFA activates C3aR1 to induce an increase of intracellular Ca2+. TLQP-21 TFA is used for the research in regulation of nociception and other relevant physiologic functions[1][2]. TLQP-21 TFA is a peptide of 21 amino acids. At a dose of 3 μM TLQP-21 induces up to ~69% of th...
T80168	Scorpion toxin Tf2	Sodium Channel	Membrane transporter/Ion channel
	Scorpion toxin Tf2为一种在Tityus fasciolatus的毒液中首次发现的β-蝎毒素。作为Nav1.3激活剂，该毒素与神经元的电压门控钠（Nav）亚型相关，此亚型与癫痫和伤害感受密切相关。Scorpion toxin Tf2作用于hNav1.3，能够增强其激活电压，并且能够在静息膜电位下开启该通道。
T35598	Neuromedin U-25 (human) (trifluoroacetate salt)
	Neuromedin U (NMU) is a neuropeptide first demonstrated to drive smooth muscle contraction.1Translated as a 174 amino acid propeptide, NMU is cleaved to different lengths in different animals. It has diverse receptor-mediated rolesin vivo, as it regulates feeding, vasoconstriction, nociception, and bone remodeling and contributes to obesity, cancer and septic shock.2,2NMU-25 is the active form of NMU in humans. It binds with high affinity to receptors on human left ventricle and coronary artery ...
T35597	Neuromedin U-23 (rat) (trifluoroacetate salt)
	Neuromedin U-23 (NMU-23) is a neuropeptide involved in diverse biological processes, including smooth muscle contraction, energy homeostasis, and nociception.1It is an agonist of neuromedin-U receptor 1 (NMUR1; EC50= 0.17 nM for the human receptor in a calcium mobilization assay using HEK293 cells) and NMUR2 (EC50= ~1.4-2 nM for arachidonic acid release in CHO cells expressing the human receptor).2,3NMU-23 (1 μM) induces contractions in isolated rat colon smooth muscle strips.4It decreases body ...
T83674	K 41498 TFA
	K 41498 是一种针对皮质酮释放因子受体2α（CRF2α）和CRF2β的肽拮抗剂，其在表达人类受体的HEK293细胞中的Ki值分别为0.66和0.62 nM。它对CRF2α和CRF2β具有选择性，与CRF1相比（在表达人类受体的HEK293细胞中Ki值为425 nM）。K 41498 (1.84 µg/动物, 静脉注射) 能够阻止大鼠由于尿催肾上腺皮质激素引发的低血压。通过脊髓内给药，K 41498 (0.075-0.5 µmol/动物) 能降低完全弗氏佐剂引起的大鼠模型中机械性爪撤回阈值。
T36376	SB-612111
	SB-612111 is a novel and potent human opiate receptor-like orphan receptor (ORL-1) antagonist with a high affinity for hORL-1 (Ki=0.33 nM). SB-612111 exhibits selectivity for μ-, κ- and δ-receptors with Ki values of 57.6 nM, 160.5 nM and 2109 nM, respecticely. SB-612111 effectively antagonizes the pronociceptive action of Nociceptin in an acute pain model[1]. [1]. Paola F Zaratin, et al. Modification of Nociception and Morphine Tolerance by the Selective Opiate Receptor-Like Orphan Receptor Anta...
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

A2764 dihydrochloride

Cat.No: T7775

Target: Potassium Channel

Cat.No: T2024

Synonym: A 803467,A803467

Target: Sodium Channel

Cat.No: T0692

Synonym: Zyloric,别嘌醇,Zyloprim,Lopurin,别嘌呤醇

Target: ROS, Xanthine Oxidase

Allopurinol Sodium

Cat.No: T6376

Synonym: 1H-吡唑并[3,4-D]嘧啶-4-醇单钠盐,Allopurinol sodium salt,Sodium allopurinol

Target: ROS

Fosaprepitant dimeglumine

Cat.No: T1790

Synonym: 福沙匹坦二甲葡胺,L785298,福沙吡坦二甲葡胺,MK-0517,Fosaprepitant dimeglumine salt

Target: Neurokinin receptor

[Leu5]-Enkephalin

Cat.No: T7173

Synonym: 亮氨酸脑啡肽,Leucine enkephalin,Leucyl-enkephalin,Leu-enkephalin

Target: Opioid Receptor, Endogenous Metabolite

Cat.No: T15192

Target: Chloride channel

AT-121 hydrochloride

Cat.No: T39529

Target: Opioid Receptor

[Leu5]-Enkephalin acetate(58822-25-6 free base)

Cat.No: T7173L

Synonym: 亮氨酸脑啡肽,Leucine enkephalin,Leu-enkephalin,Leucyl-enkephalin

Target: Opioid Receptor, Endogenous Metabolite

Cat.No: T9955

Target: NOS

Cat.No: T3690

Synonym: A 740003

Target: P2X Receptor

Cat.No: T68141

Target: 5-HT Receptor

Neuromedin U (rat) acetate

Cat.No: TP1083L

Target: Others

HS 014 acetate(207678-81-7 free base)

Cat.No: TP2015L

Target: Melanocortin Receptor

Axomadol hydrochloride

Cat.No: T30239

Neuromedin U, rat

Cat.No: TP1083

Synonym: Rat neuromedin U-23,Neuromedin U (rat)

Cat.No: T26475

Cat.No: T39527

Cat.No: TP2015

Synonym: HS 014

SSTR4 agonist 3

Cat.No: T61130

[Tyr8,Nle11] Substance P

Cat.No: T76484

Cat.No: T60305

D-NAME (hydrochloride)

Cat.No: T36719

Neuromedin U, rat TFA

Cat.No: T78004

Synonym: Rat neuromedin U-23 TFA,Neuromedin U (rat) (TFA)

Cat.No: T37610

Target: Opioid Receptor

Sigma-1 receptor antagonist 5

Cat.No: T78734

Target: Sigma receptor

Cat.No: T38077

Scorpion toxin Tf2

Cat.No: T80168

Target: Sodium Channel

Neuromedin U-25 (human) (trifluoroacetate salt)

Cat.No: T35598

Neuromedin U-23 (rat) (trifluoroacetate salt)

Cat.No: T35597

Cat.No: T83674

Cat.No: T36376

L-AP4 monohydrate

Cat.No: T37127

Synonym: L-AP4 monohydrate

Cat. No.	Product Name	Target	Signaling Pathways
T3S0870	Paederosidic acid methyl ester 鸡屎藤苷酸甲酯,紫草酸甲酯	ATPase; Potassium Channel; NO Synthase	Immunology/Inflammation; Membrane transporter/Ion channel
	Paederosidic acid methyl ester 是 ATP 敏感的 K+channel 通道激活剂，分离自 P. scandens。它通过激活脑中和脊髓水平中 ATP 敏感型 K+通道提高了痛觉阈值，表现出显著的中枢缓解疼痛活性。

天然产物

Paederosidic acid methyl ester

Cat.No: T3S0870

Synonym: 鸡屎藤苷酸甲酯,紫草酸甲酯

Target: ATPase, Potassium Channel, NO Synthase

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