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Search Results for " hyperalgesia "

31

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T22518	5-BDBD	P2X Receptor	Membrane transporter/Ion channel; Neuroscience
	5-BDBD 是选择性P2X4受体拮抗剂，抑制 rP2X4R 介导的电流，IC50为0.75μM。它可完全阻断硝酸甘油诱导的基础性和急性痛觉过敏。
T9685	DS-1971a	Sodium Channel	Membrane transporter/Ion channel
	DS-1971a 是选择性、口服有效的 NaV1.7抑制剂，对 hNaV1.7 和 mNaV1.7 的 IC50分别为 22.8 和 59.4 nM。DS-1971a 在缓解疼痛方面有研究价值。
T23498	UNC3230 UNC 3230	Others	Others
	UNC3230 是一种 ATP 竞争性的磷脂酰肌醇 4 磷酸 5 激酶 1C 型 (PIP5K1C) 选择性抑制剂，其IC50约为 41 nM。它还可抑制PIP4K2C，但对其他调节磷酸肌醇水平的脂质激酶无抑制作用。它具有缓解疼痛和抗癌特性。
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)。
T21976	ONO-8130	Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation
	ONO-8130 是前列腺素 EP1 受体选择性拮抗剂，口服有活力，能够阻断 L6 脊髓中ERK 的磷酸化。它可缓解环磷酰胺致膀胱炎小鼠的膀胱疼痛，可用于研究间质性膀胱炎。
T6950	PNU-120596 NSC 216666	AChR	Neuroscience
	PNU-120596 (NSC-216666) 是一种选择性α7 nAChR 阳性变构调节剂，EC50为 216 nM，可用于精神病和神经疾病的研究。
T21983L	PKI 14-22 amide, myristoylated Acetate PKI 14-22 amide, myristoylated Acetate(201422-03-9 Free base)	PKA	Tyrosine Kinase/Adaptors
	PKI 14-22 amide, myristoylated Acetate 抑制 cAMP 依赖性蛋白激酶 (PKA) 并阻断脊髓给药 8-溴-cAMP 产生的痛觉过敏。
T4236	AR-M 1000390 hydrochloride ARM390 Hydrochloride,ARM-390 HCl	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	AR-M 1000390 hydrochloride (ARM-390 HCl) 是选择性 δ 阿片受体激动剂，EC50为 7.2±0.9 nM。
T12632	(R)-Mirtazapine (R)-Org3770,(R)-6-Azamianserin	5-HT Receptor	GPCR/G Protein; Neuroscience
	(R)-Mirtazapine ((R)-Org3770) 是 Mirtazapine 的 R(-)-对映体，在急性热痛觉动物模型中具有抗伤害感受的特性。(R)-Mirtazapine 是 5-HT3 受体的拮抗剂，是一种潜在的镇痛剂。
T23076L	Nociceptin (1-7) acetate	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	Nociceptin (1-7) acetate 是一种有效的阿片受体样受体 1 (ORL1) 受体激动剂。 Nociceptin (1-7) 与 nociceptin 结合可降低痛觉过敏并具有镇痛活性。
TP1904L	FSLLRY-NH2 TFA(245329-02-6 free base)	Protease-activated Receptor	GPCR/G Protein
	FSLLRY-NH2 TFA(245329-02-6 free base) 是一种蛋白酶激活受体 2 (PAR2) 抑制剂。在 ICR 小鼠中逆转紫杉醇诱导的机械异常性疼痛、热痛觉过敏和 PKC 激活。阻断分离的心脏成纤维细胞中的 ERK 活化和胶原蛋白生成。还可以减轻皮肤癣菌相关瘙痒小鼠模型的症状。
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。
T80500	Jingzhaotoxin-X JZTX-X	Potassium Channel	Membrane transporter/Ion channel
	Jingzhaotoxin-X (JZTX-X) is a selective inhibitor of Kv4.2 and Kv4.3 potassium channels, inducing persistent mechanical hyperalgesia.
TP2276	Nocistatin (bovine)	Others	Others
	endogenous peptide used to block nociceptin-induced allodynia and hyperalgesia
T15167	Draflazine R-75231	Others	Others
	Draflazine is an ENT1 inhibitor. It completely reverses the hypersensitivity in the complete Freund’s adjuvant (CFA) model of mechanical hyperalgesia. Draflazine also completely reverses the hypersensitivity of the carrageenan inflammation model of therma
TQ0002L	A-317491 sodium A-317491,A 317491,A317491
	A-317491 is an effective selective non-nucleotide antagonist of P2X3 and P2X2/3 receptors, which reverses inflammatory mechanical hyperalgesia and relieves chronic inflammation and neuropathic pain in rats by acting on peripheral receptors.
T23076	Nociceptin(1-7) Nociceptin (1-7)	Others	Others
	Bioactive metabolite of nociceptin, antagonist of nociceptin-induced hyperalgesia
TP2277	Nocistatin(human) Nocistatin (human)	Others	Others
	Blocker of nociceptin-induced allodynia and hyperalgesia
T21393	Ethopropazine Hydrochloride Lysivane,Parphezein,Dibutil,Parfezin,Profenamine HCl,Pardisol
	Ethoproprazine hydrochloride is an butyrylcholinesterase inhibitor. It reduces extrapyramidal motor effects and used as an antidyskinetic, characteristic of Parkinson′s disease. It also alleviates thermal hyperalgesia in rats.
T81658	Nocistatin(human) TFA
	Nocistatin (human) TFA 可以抑制因疼痛刺激而引发的痛觉过敏与异常，并可减轻由前列腺素prostaglandin E2所致的疼痛。
T11700	J-2156	Others	Others
	The ED50 of J-2156 in rats for the relief of mechanical allodynia and mechanical hyperalgesia in the ipsilateral hindpaws was 3.7 and 8.0 mg/kg, respectively. J-2156 is a high potent, selective somatostatin receptor type 4 (SST4 receptor) agonist with IC5
T75594	Harpactira Baviana Venom
	Harpactira Baviana Venom (Baboon Tarantula Venom) 是一种蜘蛛毒液，能够从皇帝巴布蜘蛛蜘蛛中获得。Harpactira Baviana Venom 可以调节 NaV1.8和诱导痛觉过敏。
TP1904	FSLLRY-NH2
	Selective PAR2 peptide antagonist. Reverses taxol-induced mechanical allodynia, heat hyperalgesia and PKC activation in ICR mice. Blocks ERK activation and collagen production in isolated cardiac fibroblasts. Also reduces symptoms in a mouse model of derm
T76003	MSG606 TFA
	MSG606 TFA, a potent antagonist of the human MC1 receptor (IC50 = 17 nM), functions as a partial agonist at the human MC3 and MC5 receptors (EC50 values of 59 and 1300 nM, respectively). It demonstrates binding affinity for A375 melanoma cells in vitro and selectively reverses induced hyperalgesia in female mice without affecting male mice.
T75908	Nociceptin(1-7) TFA
	Nociceptin(1-7) 是 Nociceptin 的 N 端生物活性片段。Nociceptin(1-7) 是一种有效的ORL1(NOP)受体激动剂，具有缓解疼痛活性。Nociceptin(1-7) 联合 Nociceptin 可降低体内对痛觉的敏感。
T76420	Nocistatin
	Nocistatin 是一种神经肽，是孤儿类阿片受体的内源性配体。 Nocistatin 还是神经肽伤害感受肽或孤啡肽 FQ (Noc/OFQ) 的功能性拮抗剂。Nocistatin 通过 Gi/o 蛋白介导途径抑制 5-HT 释放。Nocistatin 阻断 Nociceptin 诱导的异常性疼痛和痛觉过敏。
T82470	Endokinin C
	Endokinin C作为内皮激肽系列中的肽类成分，在疼痛途径中扮演神经递质或调节剂的角色。该化合物的预处理能有效抑制endokinin A/B引发的小鼠划痕行为以及对热的过敏反应。
T64113	J-2156 TFA
	J-2156 TFA 是一种选择性的、高效的生长抑素受体 4 型 (SST4) 激动剂，能够作用于人 SST4 受体 (IC50: 0.05 nM) 和大鼠 SST4 受体 (IC50: 0.07 nM)。J-2156 TFA 表现出抗炎活性，能够缓解大鼠同侧后爪的机械性异常性疼痛和机械性痛觉过敏。
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...
T37182	AX 048
	The group IVA phospholipase A2 (PLA2), known as calcium-dependent cytosolic PLA2 (cPLA2), selectively releases arachidonic acid from membrane phospholipids, playing a central role in initiating the synthesis of prostaglandins and leukotrienes. AX 048 is a potent group IVA cPLA2 inhibitor that demonstrates 50% inhibition of the enzyme at a mole fraction (XI(50)) of 0.022. Pretreatment with AX 048 (ED50 = 1.2 mg/kg) dose-dependently reduces thermal hyperalgesia evoked by carrageenan injection of r...
T69451	R-130823
	R-130823 is a ighly selective inhibition against mitogen-activated protein kinase p38alpha (IC50=22 nM). The release of tumor necrosis factor-alpha, interleukin-1beta, -6 and -8 was inhibited in lipopolysaccharide-stimulated human blood pretreated by R-130823 , with IC50 values of 0.089, 0.066, 0.95 and 0.16 microM, respectively. R-130823 reduced the established hind paw swelling in rat adjuvant-induced arthritis, while methotrexate showed no suppression. In the same model, R-130823 ameliorated ...

化合物

Cat.No: T22518

Target: P2X Receptor

Cat.No: T9685

Target: Sodium Channel

Cat.No: T23498

Synonym: UNC 3230

Target: Others

Cat.No: T21543

Target: TRP/TRPV Channel

Cat.No: T21976

Target: Prostaglandin Receptor

Cat.No: T6950

Synonym: NSC 216666

Target: AChR

PKI 14-22 amide, myristoylated Acetate

Cat.No: T21983L

Synonym: PKI 14-22 amide, myristoylated Acetate(201422-03-9 Free base)

Target: PKA

AR-M 1000390 hydrochloride

Cat.No: T4236

Synonym: ARM390 Hydrochloride,ARM-390 HCl

Target: Opioid Receptor

(R)-Mirtazapine

Cat.No: T12632

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

Target: 5-HT Receptor

Nociceptin (1-7) acetate

Cat.No: T23076L

Target: Opioid Receptor

FSLLRY-NH2 TFA(245329-02-6 free base)

Cat.No: TP1904L

Target: Protease-activated Receptor

Cat.No: T37610

Target: Opioid Receptor

Jingzhaotoxin-X

Cat.No: T80500

Synonym: JZTX-X

Target: Potassium Channel

Nocistatin (bovine)

Cat.No: TP2276

Target: Others

Cat.No: T15167

Synonym: R-75231

Target: Others

A-317491 sodium

Cat.No: TQ0002L

Synonym: A-317491,A 317491,A317491

Nociceptin(1-7)

Cat.No: T23076

Synonym: Nociceptin (1-7)

Target: Others

Nocistatin(human)

Cat.No: TP2277

Synonym: Nocistatin (human)

Target: Others

Ethopropazine Hydrochloride

Cat.No: T21393

Synonym: Lysivane,Parphezein,Dibutil,Parfezin,Profenamine HCl,Pardisol

Nocistatin(human) TFA

Cat.No: T81658

Cat.No: T11700

Target: Others

Harpactira Baviana Venom

Cat.No: T75594

Cat.No: TP1904

Cat.No: T76003

Nociceptin(1-7) TFA

Cat.No: T75908

Cat.No: T76420

Cat.No: T82470

Cat.No: T64113

Cat.No: T71955

Cat.No: T37182

Cat.No: T69451

Cat. No.	Product Name	Target	Signaling Pathways
T3S2312	Poncirin 枸橘苷,Isosakuranetin-7-neohesperidoside	Apoptosis; Others	Apoptosis; Others
	Poncirin (Isosakuranetin-7-neohesperidoside) 是从三叶草中分离出来的一种天然产物，具有抗炎活性。它防止脂肪生成，增强间充质干细胞中的成骨细胞分化，增加骨矿物质密度，改善小梁微结构，可能反映 GIO 小鼠的骨形成增加和骨吸收减少。
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。
T4484	1,7-Dihydroxy-2,3-methylenedioxyxanthone	Prostaglandin Receptor; Antifection	GPCR/G Protein; Immunology/Inflammation; Microbiology/Virology
	1,7-Dihydroxy-2,3-methylenedioxyxanthone has antiulcerogenic, anti-oxidation, and antihyperalgesic activities, it can inhibit the carrageenan-induced hyperalgesia.

天然产物

Cat.No: T3S2312

Synonym: 枸橘苷,Isosakuranetin-7-neohesperidoside

Target: Apoptosis, Others

Cat.No: T3S2259

Synonym: 4-allylveratrole,eugenyl methyl ether,O-methyleugenol,Eugenol Methyl ether,丁香酚甲醚,丁子香酚甲醚

Target: GABA Receptor

1,7-Dihydroxy-2,3-methylenedioxyxanthone

Cat.No: T4484

Target: Prostaglandin Receptor, Antifection

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