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Search Results for " nociceptive "

36

抑制剂 & 化合物

14

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)。
T10466	BAY-1797	P2X Receptor	Membrane transporter/Ion channel; Neuroscience
	BAY-1797 是具有口服活性的选择性P2X4高效拮抗剂，对人 P2X4 的IC50为 211 nM，具有抗伤害和抗炎作用。
T9244	σ1 Receptor antagonist-1	Sigma receptor	GPCR/G Protein
	σ1 Receptor antagonist-1 是高选择性的 sigma 1受体拮抗剂，pKi 为10.28。它抑制细胞生长，在 G0/G1 期阻滞细胞周期并诱导 MCF-7/ADR 细胞凋亡。
T9461	AZ194	Sodium Channel	Membrane transporter/Ion channel
	CRMP2-Ubc9-NaV1.7 inhibitor 194 是一流的CRMP2-Ubc9相互作用抑制剂及NaV1.7抑制剂 (IC50=1.2 μM)，口服有活性，具有抗伤害作用。AZ194 阻断 CRMP2 的 SUMOylation 以选择性地减少表面表达 NaV1.7 的量。
T4552	Fursultiamine Diteftin,呋喃硫胺,Judolor,Alinamin F	Others	Others
	Fursultiamine (Alinamin F) 是维生素 B1衍生物，具有抗伤害和抗肿瘤作用。它可用于研究维生素 B1缺乏病、骨关节炎和癌症。
T2525	Alosetron hydrochloride Lotronex,盐酸阿洛司琼,GR 68755C,GR 68755,GR 68755X	5-HT Receptor	GPCR/G Protein; Neuroscience
	Alosetron hydrochloride (GR 68755) 是一种高选择性的 5-HT3 受体拮抗剂，可减轻清醒或麻醉犬直肠扩张的内脏伤害性效应，具有抗炎活性，用于肠易激综合征的研究。它阻断 5HT3 介导的豚鼠肌间和粘膜下神经元的快速去极化，IC50约为 55 nM。
T9132	Emorfazone 依莫法宗,PH011085	Others	Others
	Emorfazone (PH011085) 具有抗伤害作用。
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。
T12632L	(S)-Mirtazapine (S)-6-Azamianserin,(S)-Org3770	5-HT Receptor	GPCR/G Protein; Neuroscience
	(S)-Mirtazapine ((S)-Org3770) 是 Mirtazapine 的 S(+)-对映体。(S)-Mirtazapine 是一种选择性 5-HT2 受体拮抗剂,具有促痛觉作用,常与Mirtazapine 的 R(-)-对映体混合使用来研究抑郁症。
T8341	QX 314 QX-314	Others	Others
	QX 314 (Lidocaine N-ethyl bromide) 是一种非膜渗透性阻滞剂，可抑制酸诱导的食管伤害性 C 纤维神经元活化。
T21380	Pravadoline WIN 48098-6,WIN48098-6,普拉朵林,WIN-48098-6	Cannabinoid Receptor	GPCR/G Protein
	Pravadoline (WIN48098-6) 是一种 cannabinoid 受体激动剂。 Pravadoline 抑制小鼠大脑中的 PGs 合成，并在受到各种热、化学和机械伤害性刺激的啮齿动物中显示出镇痛活性。
T7675	Substance P (1-7) 2TFA(68060-49-1(free base))	Others	Others
	Substance P (1-7) 2TFA(68060-49-1(free base)) 是速激肽P（SP）蛋白水解降解后形成的主要生物活性代谢物，具有抗炎、抗伤害和抗痛觉过敏作用。
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。
T83212	AC-099 hydrochloride	Neuropeptide Y Receptor	GPCR/G Protein; Neuroscience
	AC-099 hydrochloride 是一种神经肽 FF2 受体 NPFF2R 的选择性全激动剂（EC50=1189 nM）和神经肽 FF1 受体 NPFF1R的部分激动剂功能（EC50=2370 nM），可逆转阿片类化合物诱导的痛觉过敏，可用于研究神经系统疾病。
T19723	AMTB hydrochloride AMTB	TRP/TRPV Channel	Membrane transporter/Ion channel
	AMTB hydrochloride (AMTB HCl) 是TRPM8通道的选择性阻滞剂。它抑制 icilin 诱导的 TRPM8 通道激活，pIC50为 6.23。它在膀胱过度活动和膀胱疼痛综合征中有研究的价值。它是电压门控钠通道的非选择性抑制剂 (NaV)。
TP1559L	Ziconotide Acetate (107452-89-1 free base) 醋酸齐考诺肽,Prialt,Ziconotide Acetate	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	Ziconotide Acetate (107452-89-1 free base) (Prialt) 是一种镇痛剂，已用于治疗神经性和非神经性疼痛。 Ziconotide 通过与位于伤害感受通路初级传入神经元末端部分的 N 型钙通道结合起作用，因此通过有效的镇痛作用减少突触传递。
T1092	Zolmitriptan 佐米曲普坦,311C90,BW-311C90	5-HT Receptor	GPCR/G Protein; Neuroscience
	Zolmitriptan (311C90) 是一种5-HT1B/1D 受体部分激动剂，可用于偏头痛的研究，对 5-HT1B、5-HT1D、5-HT1F 受体的Ki 分别为 5.01、0.63 和 63.09 nM。
T25843	N(G)-Nitroarginine-4-nitroanilide NAPNA,N(omega)-Nitro-L-arginine p-nitroanilide,L-Napna
	N(G)-Nitroarginine-4-nitroanilide is an anti-nociceptive in mice.
T27243	Efipladib PLA-902,PLA 902,PLA902
	Efipladib is a phospholipase inhibitor. Efipladib decreases nociceptive responses without affecting PGE2 levels in the cerebral spinal fluid.
T35087	VVZ-149 VVZ 149
	VVZ-149 is an antagonist of both serotonin receptor 2A (5HT2A) and glycine transporter type 2 (GlyT2), with potential anti-nociceptive activity.
T23237	RLLFT-NH2	Others	Others
	TFLLR-NH2, reversed amino acid sequence control peptide, is a PAR1 selective agonist that significantly increases the nociceptive threshold.
TP2119	Sarafotoxin S6a
	Endothelin receptor agonist (EC50 values are 7.5 and > 150 nM for contraction of pig coronary artery and guinea pig aorta respectively). Nociceptive in vivo.
TP2118	SNX-482 SNX 482
	Potent and selective, voltage-dependent R-type CaV2.3 calcium channel blocker (IC50 = 30 nM). Antinociceptive; inhibits nociceptive C-fibre and Aδ-fibre-evoked neuronal responses.
TP1994	M871
	Selective galanin GAL2 receptor antagonist (Ki values are 13.1 and 420 nM for GAL2 and GAL1 receptors respectively). Blocks the pro-nociceptive effect of GAL2 receptor agonists.
TP1471	Ziconotide TFA (107452-89-1 free base) Ziconotide TFA
	Ziconotide TEA acts by binding to N-type calcium channels situated on the terminal part of primary afferent neurons of the nociceptive pathway therefore reducing synaptic transmission with potent antinociceptive effects.
T7396	Substance P(1-7) Substance P 1-7	Others; Neurokinin receptor	GPCR/G Protein; Neuroscience; Others
	Substance P(1-7) (Substance P 1-7) 是神经肽P 物质的片段，可对孤束核产生抑制和缓和作用，具有抗炎、抗伤害和抗痛觉过敏的作用。
T78559	PDE7-IN-3
	PDE7-IN-3（例2）是一种具有潜在镇痛活性的PDE7磷酸二酯酶抑制剂，可用于探究炎性、神经性、内脏性及伤害性疼痛。
T76274	Dolcanatide
	Dolcanatide为一种对GC-C(鸟苷酸环化酶-C)具有口服活性的激动剂，展现出通便、抗痛及抗炎效果，适用于炎症性肠病研究。
T60784	SSTR4 agonist 2
	SSTR4 agonist 2 是有效的生长抑素受体亚型 4 (SSTR4) 激动剂，在 SSTR4 相关的医学疾病研究中具有潜力。SSTR4 通路抑制痛觉和炎症。
T38055	Salvinorin A Propionate
	Salvinorin A propionate is a selective partial agonist at κ1-opioid receptors (KOR) with a Ki value of 32.6 nM. It inhibits adenylate cyclase (EC50 = 4.7 nM) in HEK293 cells transfected with human KOR. It is selective for KORs over μ, δ, and ORL-1 opioid receptors and has no effect at serotonin, dopamine, muscarinic, or adrenergic receptors. In mice, salvinorin A propionate (13 μg, i.c.v.) reduces nociceptive responses in a radiant heat tail-flick assay, though not as potently as salvinorin A .
T37389	NS 383
	ASIC blocker (IC50 values are 0.44, 2.1 μM and no effect at rat ASIC1a, ASIC3 and ASIC2a, respectively: IC50 value = 0.12 μM at human ASIC1a with no effect at ASIC2a or ASIC3). Inhibition was also observed at heteromeric ASIC channels (IC50 values are 0.79, 0.87 and 4.5 uM at rat ASIC1a+3, ASIC1a+2a and ASIC2a+3; IC5O values are 0.33 and 0.69 uM at human ASIC1a+2a and ASIC1a+3, with no effect at ASIC2a+3). Attenuates pathophysiological nociceptive behaviors in CFA-inflamed and CCI rats.
T71955	C3001a
	C3001a is a selective activator for TREK, against other two-pore domain K+(K2P) channels. C3001a binds to the cryptic binding site formed by P1 and TM4 in TREK-1. C3001a targets TREK channels in the peripheral nervous system to reduce the excitability of nociceptive neurons. In neuropathic pain, C3001a alleviated spontaneous pain and cold hyperalgesia. In a mouse model of acute pancreatitis, C3001a alleviated mechanical allodynia and inflammation. C3001a represents a lead compound which could a...
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。
T62805	SB-612111 hydrochloride
	SB-612111 hydrochloride 是一种高效的、新型的阿片受体孤儿受体 (ORL-1) 拮抗剂，对 hORL-1 具有较高的亲和力，Ki 值为 0.33 nM。SB-612111 hydrochloride 能够作用于 μ-receptor (Ki: 57.6 nM)，κ-receptor (Ki: 160.5 nM) 和 δ-receptor (Ki: 2109 nM)。SB-612111 hydrochloride 能有效拮抗 Nociceptin 在急性疼痛模型中的造成的痛觉作用。
T60911	SSTR4 agonist 4
	SSTR4 agonist 4 是一种有效的SSTR4激动剂，具有用于疼痛研究的潜力。SSTR4 激动剂在与急性和慢性相关的抗外周伤害感受和抗炎活性相关疼痛的啮齿动物模型中有效。SSTR4 在海马和新皮质、记忆和学习区域以及阿尔茨海默病病理学中的表达水平相对较高。
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 ...

化合物

Cat.No: T21543

Target: TRP/TRPV Channel

Cat.No: T10466

Target: P2X Receptor

σ1 Receptor antagonist-1

Cat.No: T9244

Target: Sigma receptor

Cat.No: T9461

Target: Sodium Channel

Cat.No: T4552

Synonym: Diteftin,呋喃硫胺,Judolor,Alinamin F

Target: Others

Alosetron hydrochloride

Cat.No: T2525

Synonym: Lotronex,盐酸阿洛司琼,GR 68755C,GR 68755,GR 68755X

Target: 5-HT Receptor

Cat.No: T9132

Synonym: 依莫法宗,PH011085

Target: Others

Cat.No: T30824

Synonym: Cgp29030A,Cgp-29030A

Target: Others

(S)-Mirtazapine

Cat.No: T12632L

Synonym: (S)-6-Azamianserin,(S)-Org3770

Target: 5-HT Receptor

Cat.No: T8341

Synonym: QX-314

Target: Others

Cat.No: T21380

Synonym: WIN 48098-6,WIN48098-6,普拉朵林,WIN-48098-6

Target: Cannabinoid Receptor

Substance P (1-7) 2TFA(68060-49-1(free base))

Cat.No: T7675

Target: Others

Cat.No: T14384

Synonym: KAN-0440567,KAND567

Target: CXCR

AC-099 hydrochloride

Cat.No: T83212

Target: Neuropeptide Y Receptor

AMTB hydrochloride

Cat.No: T19723

Synonym: AMTB

Target: TRP/TRPV Channel

Ziconotide Acetate (107452-89-1 free base)

Cat.No: TP1559L

Synonym: 醋酸齐考诺肽,Prialt,Ziconotide Acetate

Target: Calcium Channel

Cat.No: T1092

Synonym: 佐米曲普坦,311C90,BW-311C90

Target: 5-HT Receptor

N(G)-Nitroarginine-4-nitroanilide

Cat.No: T25843

Synonym: NAPNA,N(omega)-Nitro-L-arginine p-nitroanilide,L-Napna

Cat.No: T27243

Synonym: PLA-902,PLA 902,PLA902

Cat.No: T35087

Synonym: VVZ 149

Cat.No: T23237

Target: Others

Sarafotoxin S6a

Cat.No: TP2119

Cat.No: TP2118

Synonym: SNX 482

Cat.No: TP1994

Ziconotide TFA (107452-89-1 free base)

Cat.No: TP1471

Synonym: Ziconotide TFA

Substance P(1-7)

Cat.No: T7396

Synonym: Substance P 1-7

Target: Others, Neurokinin receptor

Cat.No: T78559

Cat.No: T76274

SSTR4 agonist 2

Cat.No: T60784

Salvinorin A Propionate

Cat.No: T38055

Cat.No: T37389

Cat.No: T71955

Sigma-1 receptor antagonist 5

Cat.No: T78734

Target: Sigma receptor

SB-612111 hydrochloride

Cat.No: T62805

SSTR4 agonist 4

Cat.No: T60911

Neuromedin U-23 (rat) (trifluoroacetate salt)

Cat.No: T35597

Cat. No.	Product Name	Target	Signaling Pathways
TN6791	Palvanil Hexadecanamide	TRP/TRPV Channel	Membrane transporter/Ion channel
	Palvanil (Hexadecanamide) 是一种快速脱敏的 TRPV1 激动剂。它可能是治疗 IBS 的有前途的药物，因为它可以调节肠道蠕动并减轻内脏疼痛。
T8249	Hexahydrofarnesyl acetone 植酮,Phytone	Others; Antibacterial	Microbiology/Virology; Others
	Hexahydrofarnesyl acetone (Phytone) 是从Launaea mucronata 中分离得到的倍半萜，具有抗菌和抗炎活性，可研究缓解疼痛。
TN6729	Azadiradione AZD	Others	Others
	Azadiradione (AZD) 是 HSF1的一种，是由印楝树中提取得到，具有一定生物活性的柠檬苦素。
T2786	Oxysophocarpine 氧化槐树碱,氧卡地平	Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation
	Oxysophocarpine 是提取自海藻的生物碱。它抑制口腔鳞状细胞癌的生长和转移。它对中枢神经系统和周围神经系统具有神经保护作用和抗伤害感受作用。
T6S1369	Vitexin 牡荆素,Apigenin-8-C-glucoside	Antioxidant	oxidation-reduction
	Vitexin 是一种存在于多种药用植物（如榕树、螺旋藻）中的 c-糖基化的黄酮。它具有广泛的药理作用，包括抗氧化，抗癌，抗炎，抗痛觉过敏和神经保护作用。
T4S0536	Bullatine A	Apoptosis; P2X Receptor	Apoptosis; Membrane transporter/Ion channel; Neuroscience
	Bullatine A 是一种有效的 P2X7拮抗剂，可抑制 ATP 诱导的细胞凋亡和 P2X 受体介导的炎症反应。它是乌头属的二萜生物碱，能缓解过敏反应，具有抗风湿、抗炎和抗伤害作用，可用于治疗关节炎等神经退行性疾病。
T8846	beta-Escin B-escin,AESCINE,beta-七叶素	Immunology/Inflammation related	Immunology/Inflammation
	beta-Escin 是七叶树种子的主要活性成分。它可抑制碱性成纤维细胞生长因子所诱导的增殖、迁移、管形成以及体内 CAM 血管生成。它具有研究抗血管生成作用的分子机制的潜力。
T2163	Dihydrocapsaicin CCRIS1589,二氢辣椒素,6,7-Dihydrocapsaicin,8-Methyl-N-vanillylnonanamide	Others; TRP/TRPV Channel	Membrane transporter/Ion channel; Others
	Dihydrocapsaicin (CCRIS1589) 是一种天然来源的辣椒素，是TRPV1的选择性激动剂，同时可以增加 p-Akt 水平。它可以增强低温诱导的神经保护。
T2860	Vanillyl Alcohol 4-Hydroxy-3-methoxybenzenemethanol,3-Methoxy-4-hydroxybenzyl alcohol,4-Hydroxy-3-methoxybenzyl alcohol,香兰醇,Vanillin alcohol,Vanillic alcohol	Apoptosis; Others	Apoptosis; Others
	Vanillyl Alcohol (3-Methoxy-4-hydroxybenzyl alcohol) 是一种酚类醇，具有抗血管生成、抗惊厥、抗炎、抗氧化、神经保护和抗伤害活性。它由香兰素衍生而来，在食品和饮料中用作调味剂。
T10109	3-Carene Delta-3-Carene	COX; Antifungal	Immunology/Inflammation; Microbiology/Virology; Neuroscience
	3-Carene（Delta-3-Carene）是西部落叶松和花旗松中提取的双环单萜烯，可做为植物杀菌剂。3-Carene 对痛觉刺激引起的炎症浸润和 COX-2 过表达有抑制作用。3-Carene 具有抗伤害作用，能促进成骨细胞分化的早期标志物碱性磷酸酶的活性和表达。
T3S0209	Vincristine	ERK; p38 MAPK; NF-κB; Akt; JNK; mTOR	Cytoskeletal Signaling; MAPK; NF-κB; PI3K/Akt/mTOR signaling
	Vincristine 与微管蛋白结合并抑制微管的形成，从而抑制癌细胞的有丝分裂。 Vincristine 可用作微管去稳定剂，用于研究治疗血液系统癌症，如白血病和淋巴瘤以及儿童肉瘤的相关研究。
T6677	Sophocarpine	ERK; p38 MAPK; NF-κB; TLR; COX; HER; JNK; STAT	Angiogenesis; Immunology/Inflammation; JAK/STAT signaling; MAPK; Neuroscience; NF-κB; Stem Cells; Tyrosine Kinase/Adaptors
	Sophocarpine 是一种从传统草药苦参中提取的重要生物碱。苦参具有抗病毒、抗肿瘤和抗炎等多种药理作用。它通过多种机制显著抑制癌细胞的生长，具有抗肿瘤活性。
T13953	Umbellulone	Others	Others
	Umbellulone is a natural product isolated from Umbellularia californica, and stimulates the TRPA1 channel in a subset of peptidergic, nociceptive neurons, activating the trigeminovascular system via this mechanism.
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

Cat.No: TN6791

Synonym: Hexadecanamide

Target: TRP/TRPV Channel

Hexahydrofarnesyl acetone

Cat.No: T8249

Synonym: 植酮,Phytone

Target: Others, Antibacterial

Cat.No: TN6729

Synonym: AZD

Target: Others

Oxysophocarpine

Cat.No: T2786

Synonym: 氧化槐树碱,氧卡地平

Target: Prostaglandin Receptor

Cat.No: T6S1369

Synonym: 牡荆素,Apigenin-8-C-glucoside

Target: Antioxidant

Cat.No: T4S0536

Target: Apoptosis, P2X Receptor

Cat.No: T8846

Synonym: B-escin,AESCINE,beta-七叶素

Target: Immunology/Inflammation related

Dihydrocapsaicin

Cat.No: T2163

Synonym: CCRIS1589,二氢辣椒素,6,7-Dihydrocapsaicin,8-Methyl-N-vanillylnonanamide

Target: Others, TRP/TRPV Channel

Vanillyl Alcohol

Cat.No: T2860

Synonym: 4-Hydroxy-3-methoxybenzenemethanol,3-Methoxy-4-hydroxybenzyl alcohol,4-Hydroxy-3-methoxybenzyl alcohol,香兰醇,Vanillin alcohol,Vanillic alcohol

Target: Apoptosis, Others

Cat.No: T10109

Synonym: Delta-3-Carene

Target: COX, Antifungal

Cat.No: T3S0209

Target: ERK, p38 MAPK, NF-κB, Akt, JNK, mTOR

Cat.No: T6677

Target: ERK, p38 MAPK, NF-κB, TLR, COX, HER, JNK, STAT

Cat.No: T13953

Target: Others

N-Palmitoyl Glycine

Cat.No: T37219

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