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Search Results for " allodynia "

24

抑制剂 & 化合物

1

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T7831	Nitecapone	Others; Transferase	Metabolism; Others
	Nitecapone 是一个具有口服活性的、短效的儿茶酚-O-甲基转移酶(COMT)的抑制剂。它具有胃肠道保护和抗氧化活性，能够清除活性氧和一氧化氮，防止脂质过氧化。
T4052	KML29	Lipase	Metabolism
	KML29 是一种口服具有活性的、高度选择性的不可逆 MAGL 抑制剂，其对小鼠、大鼠和人的 IC50值分别为15 nM、43 nM 和 5.9 nM。它对 FAAH 在内的其他中心和外周丝氨酸水解酶的交叉反应极小。
T16164	MY-5445 N-(3-chlorophenyl)-4-phenylphthalazin-1-amine	PDE	Metabolism
	MY-5445 (N-(3-chlorophenyl)-4-phenylphthalazin-1-amine) 是特异性的 cGMP 磷酸二酯酶 PDE5抑制剂，其 Ki=1.3 μM。它是一种 ABCG2转运蛋白调节剂，具有抗增殖活性。它能抑制人血小板凝集。
T4691	Asimadoline hydrochloride EMD-61753 hydrochloride,阿西马朵林盐酸盐	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	Asimadoline hydrochloride (EMD-61753 hydrochloride) 是一种 κ-阿片(κ-opioid)受体激动剂，对豚鼠和人重组 κ-opioid 的 IC50值分别为 5.6 和 1.2 nM。它可改善糖尿病大鼠的异常性疼痛，具有外周抗炎作用，并有用于肠易激综合征的研究潜力。
T8505	SC-236 4-(5-(4-氯苯基)-3-(三氟甲基)-1H-,Sc 236	Apoptosis; COX; PPAR	Apoptosis; DNA Damage/DNA Repair; Immunology/Inflammation; Metabolism; Neuroscience
	SC-236 (Sc 236) 是一种具有口服活性的COX-2特异性抑制剂和PPARγ激动剂。它可通过 c-Jun 氨基端抑制激活蛋白-1活性，在小鼠模型中通过抑制 ERK 的磷酸化发挥抗炎作用。
T4633	Asimadoline EMD-61753,阿西马朵林	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	Asimadoline (EMD-61753) 是一种 κ-阿片(κ-opioid)受体激动剂，对豚鼠和人重组 κ-opioid 的IC50值分别为 5.6 和 1.2 nM。它可改善糖尿病大鼠的异常性疼痛，具有外周抗炎作用，并有用于肠易激综合征的研究潜力。
T27405	GAT211 GAT-211,AZ-4,GAT 211,AZ 4,AZ4
	GAT211 is a CB1 positive allosteric modulator. GAT211 suppresses allodynia and produces synergistic antiallodynic effects with monoacylglycerol lipase and fatty acid amide hydrolase inhibitors in paclitaxel-treated mice.
T10381	AS2717638	Others	Others
	AS2717638 是一种具有口服生物活性的，选择性的溶血磷脂酸受体5 (LPA5) 的拮抗剂，其对 hLPA4 的 IC50值为38 nM。AS2717638 还能显著改善 PGE2、PGF2α以及 AMPA 诱导的异位疼痛。
TP2068L	Cyclotraxin B acetate(1203586-72-4 free base)	Trk receptor	Tyrosine Kinase/Adaptors
	Cyclotraxin B acetate(1203586-72-4 free base) 是 TrkB 受体的拮抗剂；抑制 BDNF 诱导的 TrkB 活性 (IC50 = 0.30 nM)。变构改变 TrkB 受体构象但不改变 BDNF 结合。防止 BDNF 引起的小鼠冷异常性疼痛。还显示在小鼠中表现出推定的抗焦虑特性。
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。
TP2276	Nocistatin (bovine)	Others	Others
	endogenous peptide used to block nociceptin-induced allodynia and hyperalgesia
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。
TP2277	Nocistatin(human) Nocistatin (human)	Others	Others
	Blocker of nociceptin-induced allodynia and hyperalgesia
T10209	A-887826	Others	Others
	A-887826 is a selective, orally bioavailable, and voltage-dependent Na(v1.8) channel blocker (IC50: 11 nM). It attenuates neuropathic tactile allodynia in vivo.
T41145	TASP 0277308
	TASP 0277308 is a potent and selective sphingosine 1-phosphate 1 (S1P1) receptor antagonist (IC50 = 7.8 nM). TASP 0277308 inhibits S1P-induced chemotaxis (IC50 = 1.1-1.6 nM), HUVEC cell proliferation (IC50 = 3-3.6 nM) and suppresses angiogenesisin vivo. TASP 0277308 also blocks VEGF-induced tube-formation of HUVECsin vitroand reverses or impairs the development of arthritis or mechano-allodynia.
T27752	KT109 KT-109,KT 109
	KT109 is a selective inhibitor of DAGLβ (IC50 = 42 nM). KT109-treated wild-type mice displayed reductions in LPS-induced allodyni as well as in DAGL-β (-/-) micea. Repeated KT109 administration prevented the expression of LPS-induced allodynia, without ev
T71206	Tiagabine-d6 hydrochloride
	Tiagabine-d6 is intended for use as an internal standard for the quantification of tiagabine by GC- or LC-MS. Tiagabine is an inhibitor of GABA transporter 1. It inhibits seizures induced by DMCM in mice. Tiagabine reduces allodynia in a rodent model of neuropathic pain when used at a dose of 72.8 µmol/kg, and it acts synergistically with gabapentin to delay pain responses in mice in the hot plate test. Formulations containing tiagabine have been used as adjunctive therapies in the treatment of ...
T27025	Cizolirtine citrate E-4018,E4018,E 4018
	Cizolirtine is a calcitonin gene-related peptide antagonist. Cizolirtine may be useful for alleviating some neuropathic somatosensory disorders, in particular cold allodynia, with a reduced risk of undesirable side effects. Cizolirtine inhibits the spinal
TP2068	Cyclotraxin B
	Antagonist of TrkB receptors; inhibits BDNF-induced TrkB activity (IC50 = 0.30 nM). Allosterically alters TrkB receptor conformation but does not alter BDNF binding. Prevents BDNF-induced cold allodynia in mice. Also shown to exhibit putative anxiolytic p
T61091	p38-α MAPK-IN-4
	p38-α MAPK-IN-4 (Compound 69) 是一种选择性的p38α MAPK 抑制剂，IC50为 1.5 μM。p38-α MAPK-IN-4 在体内可快速、强烈地抑制机械性触诱发痛 (mechanical allodynia) 的发生。
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
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
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...
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。

化合物

Cat.No: T7831

Target: Others, Transferase

Cat.No: T4052

Target: Lipase

Cat.No: T16164

Synonym: N-(3-chlorophenyl)-4-phenylphthalazin-1-amine

Target: PDE

Asimadoline hydrochloride

Cat.No: T4691

Synonym: EMD-61753 hydrochloride,阿西马朵林盐酸盐

Target: Opioid Receptor

Cat.No: T8505

Synonym: 4-(5-(4-氯苯基)-3-(三氟甲基)-1H-,Sc 236

Target: Apoptosis, COX, PPAR

Cat.No: T4633

Synonym: EMD-61753,阿西马朵林

Target: Opioid Receptor

Cat.No: T27405

Synonym: GAT-211,AZ-4,GAT 211,AZ 4,AZ4

Cat.No: T10381

Target: Others

Cyclotraxin B acetate(1203586-72-4 free base)

Cat.No: TP2068L

Target: Trk receptor

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

Cat.No: TP1904L

Target: Protease-activated Receptor

Nocistatin (bovine)

Cat.No: TP2276

Target: Others

Nocistatin(human) TFA

Cat.No: T81658

Nocistatin(human)

Cat.No: TP2277

Synonym: Nocistatin (human)

Target: Others

Cat.No: T10209

Target: Others

Cat.No: T41145

Cat.No: T27752

Synonym: KT-109,KT 109

Tiagabine-d6 hydrochloride

Cat.No: T71206

Cizolirtine citrate

Cat.No: T27025

Synonym: E-4018,E4018,E 4018

Cat.No: TP2068

p38-α MAPK-IN-4

Cat.No: T61091

Cat.No: T11700

Target: Others

Cat.No: TP1904

Cat.No: T71955

Cat.No: T76420

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。

天然产物

Cat.No: T3S2312

Synonym: 枸橘苷,Isosakuranetin-7-neohesperidoside

Target: Apoptosis, Others

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