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Search Results for " antinociceptive activity "

25

抑制剂 & 化合物

22

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
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。
TP1905	BW-180C (D-丙2,D-亮5)-脑啡肽,DADLE	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	BW-180C (DADLE) 是水溶性的多肽类δ-阿片受体激动剂，也对 μ-阿片受体显示活性，在体内表现出镇痛活性。
T39284	EST73502 HCl	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	EST73502 是 μ-阿片受体激动剂 (Ki = 64 nM) 激动剂和 σ1 受体拮抗剂 (Ki = 118 nM)。 EST73502 显示出镇痛活性。
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。
T11516	GV-196771A	NMDAR	Neuroscience
	GV-196771A 一种新型的NMDA受体甘氨酸位点拮抗剂，具有强大的抗痛觉过敏活性。
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。
TP1212	N-Boc-Phe-Leu-Phe-Leu-Phe Boc-FLFLF	Others	Others
	N-Boc-Phe-Leu-Phe-Leu-Phe (Boc-FLFLF) 是甲酰肽受体 1(FPR1)拮抗剂，能够增加疼痛作用，抑制膜联蛋白的抗疼痛活性。
T23331	SC 51089 SC 51089 free base	Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation
	SC 51089 是一种选择性的前列腺素受体 PGE2 拮抗剂，对前列腺素受体亚型具有选择性，具有抗伤害活性，可改善亨廷顿病 R6/1 小鼠模型中的运动缺陷并挽救记忆力下降。
T34081	Piromelatine NEU-P-11,NEU-P 11,NEU-P11	P2X Receptor; 5-HT Receptor; MT Receptor; Sodium Channel; TRP/TRPV Channel	GPCR/G Protein; Membrane transporter/Ion channel; Neuroscience
	Piromelatine 是褪黑激素 MT1/MT2 受体、5-HT1A 和 5-HT1D 的激动剂，也是 5-HT2B 的拮抗剂。Piromelatine 具有抗痛觉活性，对 P2X3、TRPV1 和 Nav1.7 通道有抑制作用，可用于促进睡眠、缓解疼痛、抗神经退行性疾病和抗抑郁疾病的研究。
T10572	BMT-124110	AAK1 (AP2 associated kinase 1)	Neuroscience
	BMT-124110是一种具有选择性的AAK1抑制剂(IC50: 0.9 nM)，具有抗伤害感受活性。BMT-090605抑制BMP -2诱导蛋白激酶BIKE,其IC50为 17 nM。BMT-090605抑制细胞周期蛋白 G 相关激酶GAK，其IC50:为99 nM。
T4436	RO1138452 CAY10441	Others; Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation; Others
	RO1138452 (CAY10441) 是一种选择性和可口服的前列环素受体拮抗剂，pKi 为8.3。它拮抗卡前列环素诱导的人神经母细胞瘤腺苷酸环化酶的激活，以剂量依赖性方式阻断环 AMP 积累，具有镇痛活性。
T27363	FR 64822 FR-64822,FR64822
	FR64822(N-(4-pyridylcarbamoyl)amino 1,2,3,6,-tetrahydropyridine), a novel non-opioid antinociceptive compound, displays antinociceptive activities in a variety of assays with mice and rats. It has a strong antinociceptive activity in the acetic acid writh
T27968	M-5011 T-3788,S-MTPPA,M 5011,M-5011C
	M-5011 is a non-steroidal anti-inflammatory drug and immunomodulator potentially for the treatment of inflammation and pain. M-5011 had an effective antinociceptive activity (ED50 value) of 0.63 mg/kg. M-5011 partially inhibits the generalized bone loss a
T68206	Arbortristoside A
	Arbortristoside A is an anti-inflammatory and antinociceptive. This activity may be due to the inhibiting effect of prostaglandin, histamine and serotonin. Arbortristoside A has also been shown to act on ulcerations and may facilitate healing of peptic ulcers.
T72151	(D-Met2,Pro5)-Enkephalinamide
	(D-Met2,Pro5)-Enkephalinamide 是一种强效的阿片类激动剂，其具有抗痛活性。
T15165	DPI-3290 Org 41793	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	DPI-3290 is a specific agonist of opioid receptors (Ki: 0.18 nM, 0.46 nM, and 0.62 nM for δ-, μ-, and κ-opioid receptors, respectively) with potent antinociceptive activity. DPI-3290 is one of a series of novel centrally acting agents.
T14691	BMT-090605	Others	Others
	BMT-090605 is a potent, selective AAK1 inhibitor, with an IC50 of 0.6 nM. BMT-090605 inhibits BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK) with IC50s of 45 and 60 nM, respectively[1]. BMT-090605 shows antinociceptive activity
T72007	COR167
	COR167 is a CB2 agonist. It displayed potent immunomodulatory activity on immune cells from healthy subjects and patients with multiple sclerosis. It also showed protective effects on rat brain tissues toward ischemia and reperfusion-induced injury. COR167 has antinociceptive properties.
T37392	Purotoxin 1
	Purotoxin 1 可从狼蛛的毒液中分离出来，是一种 P2X3 受体抑制剂，在炎性疼痛动物模型中显示出抗伤害活性。
T37092	20-HEPE
	20-HEPE is a metabolite of eicosapentaenoic acid that is formed via ω-oxidation of EPA by cytochrome P450 (CYP) ω-oxidases, including human CYP4F3B. It activates peroxisome proliferator-activated receptor α (PPARα) in COS-7 cells expressing a luciferase reporter when used at a concentration of 10 μM. 20-HEPE also activates murine transient receptor potential vanilloid receptor 1 (mTRPV1) in vitro but lacks antinociceptive activity in rats.
T63231	LPA5 antagonist 1
	LPA5 antagonist 1 是选择性的、强效的 lysophosphatidic acid receptor 5(LPA5) 拮抗剂，IC50 值为32 nM。LPA5 antagonist 1 具有高脑渗透性和抗痛活性，能够用于研究炎症性和神经性疼痛。
T9669	EST73502 hydrochloride
	EST73502 hydrochloride 是一种选择性的，具有口服活性和血脑屏障渗透性的 μ-opioid 受体 (μ-opioid receptor/MOR) 激动剂和 σ1 受体(σ1R) 拮抗剂，对 MOR 和 σ1R 作用的Ki 值分别为 64 nM 和 118 nM。EST73502 hydrochloride 可用于缓解疼痛研究。
TP1901	Hemopressin(rat) Hemopressin (rat)
	Bioactive endogenous peptide substrate for endopeptidase 24.15 (ep24.15), neurolysin (ep24.16) and ACE. Ki values are 27.76, 3.43 and 1.87 μM respectively. Potent hypotensive in vivo. Also acts as a selective CB1 receptor inverse agonist. Displays antinoc
TP1900	Hemopressin (human, mouse)
	Bioactive endogenous peptide substrate for endopeptidase 24.15 (ep24.15), neurolysin (ep24.16) and ACE. Ki values are 27.76, 3.43 and 1.87 μM respectively. Potent hypotensive in vivo. Also acts as a selective CB1 receptor inverse agonist. Displays antinoc
T38210	Hodgkinsine B
	Hodgkinsine B is an alkaloid and isomer of hodgkinsine that has analgesic activity.1It increases the latency to tail withdrawal in the tail-flick test in mice when administered at a dose of 10 mg/kg. 1.Kodanko, J.J., Hiebert, S., Peterson, E.A., et al.Synthesis of all low-energy stereoisomers of the tris(pyrrolidinoindoline) alkaloid hodgkinsine and preliminary assessment of their antinociceptive activityJ. Org. Chem.72(21)7909-7914(2007)

化合物

Cat.No: T22733

Synonym: DL-2-氨基-5-膦酰基缬草酸

Target: NMDAR

Cat.No: TP1905

Synonym: (D-丙2,D-亮5)-脑啡肽,DADLE

Target: Opioid Receptor

Cat.No: T39284

Target: Opioid Receptor

Cat.No: T21380

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

Target: Cannabinoid Receptor

Cat.No: T11516

Target: NMDAR

Nociceptin (1-7) acetate

Cat.No: T23076L

Target: Opioid Receptor

N-Boc-Phe-Leu-Phe-Leu-Phe

Cat.No: TP1212

Synonym: Boc-FLFLF

Target: Others

Cat.No: T23331

Synonym: SC 51089 free base

Target: Prostaglandin Receptor

Cat.No: T34081

Synonym: NEU-P-11,NEU-P 11,NEU-P11

Target: P2X Receptor, 5-HT Receptor, MT Receptor, Sodium Channel, TRP/TRPV Channel

Cat.No: T10572

Target: AAK1 (AP2 associated kinase 1)

Cat.No: T4436

Synonym: CAY10441

Target: Others, Prostaglandin Receptor

Cat.No: T27363

Synonym: FR-64822,FR64822

Cat.No: T27968

Synonym: T-3788,S-MTPPA,M 5011,M-5011C

Arbortristoside A

Cat.No: T68206

(D-Met2,Pro5)-Enkephalinamide

Cat.No: T72151

Cat.No: T15165

Synonym: Org 41793

Target: Opioid Receptor

Cat.No: T14691

Target: Others

Cat.No: T72007

Cat.No: T37392

Cat.No: T37092

LPA5 antagonist 1

Cat.No: T63231

EST73502 hydrochloride

Cat.No: T9669

Hemopressin(rat)

Cat.No: TP1901

Synonym: Hemopressin (rat)

Hemopressin (human, mouse)

Cat.No: TP1900

Cat.No: T38210

Cat. No.	Product Name	Target	Signaling Pathways
T5S1131	Ganoderic acid C6 灵芝酸C6	Others	Others
	Ganoderic acid C6 是醛糖还原酶活性的抑制剂。
T6S0743	Sesamoside	Others	Others
	Sesamoside 是分离自鸢尾叶的茎中的萜类，具有抗氧化和抗糖基化活性。
T20225	Dicentrine, (-)- L-Dicentrine,荷包牡丹碱,NSC 251699,NSC251699,NSC-251699	Others	Others
	Dicentrine, (-)- (NSC-251699) 是一种在几种植物物种中发现的非卟啉生物碱，在小鼠内脏痛的急性模型中显示出显著的镇痛活性。
T5783	Rosamultin 野蔷薇苷,罗莎白素	Antioxidant; HIV Protease	Microbiology/Virology; oxidation-reduction; Proteases/Proteasome
	Rosamultin 是从Potentilla anserina L 分离的 19 α-羟基型三萜。它抑制 HIV-1 蛋白酶，具有抗氧化、抗炎和镇痛作用。
TN2540	1-Hydroxybaccatin I	Others	Others
	1-Hydroxybaccatin I 对对苯醌诱导的腹部收缩具有显着的镇痛活性。
T8169	Decursinol	Others	Others
	Decursinol 是一种分离自Angelica gigas 的根中的、口服具有活性的抗伤害药物。它具有抗肿瘤和抗转移作用。
T6S0627	Mesaconitine 新乌碱,新乌头碱；中乌头碱	TNF	Apoptosis
	Mesaconitine 是乌头属植物的一种主要活性成分，通过循环 AMP 和刺激中枢 β-肾上腺素能系统具有镇痛活性，还有抗炎活性。
T5S0662	Gelsemine 钩吻碱,Gelsemin	Antioxidant	oxidation-reduction
	Gelsemine (Gelsemin) 是一种从中草药 Gelsemium elegans 中获得的生物碱，具有抗伤害和促进睡眠活性，可有效缓解慢性疼痛。
T3409	Plantamajoside Y0160,C10485,大车前苷,车前子甙	Others	Others
	Plantamajoside (Y0160) 是一种苯丙烷类糖苷，从车前Plantago asiaticaL.中分离出来得到。它对 LPS 诱导的急性肺损伤小鼠模型具有保护作用。它对肺部炎症具有潜在的研究价值。
T3981	Acacetin 4'-Methoxyapigenin,金合欢素,5,7-Dihydroxy-4'-methoxyflavone,Linarigenin	Apoptosis; IAP; COX; Autophagy	Apoptosis; Autophagy; Immunology/Inflammation; Neuroscience
	Acacetin (5,7-Dihydroxy-4'-methoxyflavone) 是一种来自狗舌草的口服有效类黄酮。它停在 PI3Kγ 的 ATP 结合口袋中，可导致癌细胞周期停滞，并诱导细胞凋亡和自噬。它有抗癌和抗炎活性，有潜力研究疼痛相关疾病。
T4S1990	Carvacrol 香荆芥酚,Karvakrol,O-Thymol,cymophenol,香芹酚	Apoptosis; Others; Gamma-secretase; Endogenous Metabolite; Antifungal	Apoptosis; Metabolism; Microbiology/Virology; Neuroscience; Others; Proteases/Proteasome; Stem Cells
	Carvacrol (O-Thymol) 是唇形科植物中的一种单萜酚类天然产物，具有镇痛、抗焦虑、抗抑郁、抗氧化、抗炎和抗癌作用。
T3834	8-Epideoxyloganic acid 8-表去氧马钱酸	ROS; Immunology/Inflammation related	Immunology/Inflammation
	8-Epideoxyloganic acid 是从 Incarvillea delavayi 中分离得到的一种环烯醚萜苷。它具有微弱的缓解疼痛活性。
T6S1579	Monotropein 水晶兰苷,Monotropeine	Others	Others
	Monotropein (Monotropeine) 是从Morinda officinalis 中获得，能够抑制硫酸葡聚糖硫酸钠诱导的结肠炎小鼠模型中炎性因子的表达。
T2S2362	Dehydrocorydaline nitrate 去氢延胡索甲素硝酸盐,硝酸脱氢紫堇碱	BCL; Others; PARP; p38 MAPK; Caspase; Parasite; Autophagy	Apoptosis; Autophagy; Chromatin/Epigenetic; DNA Damage/DNA Repair; MAPK; Microbiology/Virology; Others; Proteases/Proteasome
	Dehydrocorydaline nitrate 是生物碱。Dehydrocorydaline 调节 Bax，Bcl-2蛋白表达，激活 caspase-7，caspase-8，并使 PARP 失活。它能增强 p38 MAPK 活化，具有抗炎、抗癌、抗疟疾等功效。
T4S0969	Obtusifolin 决明蒽醌,决明蒽醌；美决明子素	Antioxidant; NF-κB	NF-κB; oxidation-reduction
	Obtusifolin 是分离自决明子的种子中，能够抑制NF-kB 通路，调节气道上皮细胞中 MUC5AC 粘蛋白的基因表达和产生。它通过靶向甲状旁腺激素相关蛋白来抑制邻苯二甲酸酯诱导的乳腺癌骨转移。
TCS2336	Evodine	P-gp	Membrane transporter/Ion channel; Neuroscience
	Evodine 是吴茱萸中的主要柠檬苦素，是P-gp 有效抑制剂，可通过保留抗氧化剂防御系统，针对谷氨酸诱导的毒性具有保护作用。
TN3476	Baccatin VI	Others	Others
	Baccatin VI 对对苯并醌诱发的腹部收缩具有显著的抗伤害活性。
TN5404	(+)-Conocarpan
	Conocarpan has antinociceptive effects. Conocarpan is quite active against S. aureus and B. subtilis with MIC of 6.25 micrograms/ml, it also shows activity against M. tuberculosis (MIC=15.6 ug/ml). Conocarpan shows considerable activity against epimastigo
TN3537	Braylin	IL Receptor; TNF; NF-κB	Apoptosis; Immunology/Inflammation; NF-κB
	Braylin has anti-inflammatory, antinociceptive and immunomodulatory effects, which possibly act through the glucocorticoid receptor activation and by inhibition of the transcriptional activity of NF-ÎºB. Braylin is also a phosphodiesterase-4 inhibitor, it could represent an ideal prototype of glucocorticoid receptor ligand, able to induce synergic immunomodulatory effects.
TN5147	Tilifodiolide	IL Receptor; TNF; GABA Receptor	Apoptosis; Immunology/Inflammation; Membrane transporter/Ion channel; Neuroscience
	Tilifodiolide exerts in vitro and in vivo anti-inflammatory activity and in vivo antinociceptive effects. Tilifodiolide exerted antidiarrheal activity by decreasing the intestinal fluid accumulation and vasorelaxant effects mediated by nitric oxide and cyclic guanosine monophosphate, it also showed anxiolytic and antidepressant effects by the partial involvement of gamma-Aminobutyric acid (GABA) receptors and the possible participation of α2-adrenoreceptors, respectively.
TMA0627	Taxiresinol	TNF	Apoptosis
	Taxiresinol shows anticancer, antinociceptive, and antiallergic activities, it shows inhibitory activity on induced histamine release from the human basophilic cell line, KU812. Taxiresinol can protect the hepatocytes from apoptosis via an inhibition of TNF- alpha production by activated macrophages and a direct inhibition of apoptosis induced by TNF- alpha in D-GalN/LPS-treated mice.
TN4776	Physalin D	TNF; Antifection	Apoptosis; Microbiology/Virology
	Physalin D shows antimalarial activity; it also exhibits a minimum inhibitory concentration value (MIC) against Mycobacterium tuberculosis H(37)Rv strain of 32 microg/mL. Physalin D displays considerable cytotoxicity against several cancer cell lines. It

天然产物

Ganoderic acid C6

Cat.No: T5S1131

Synonym: 灵芝酸C6

Target: Others

Cat.No: T6S0743

Target: Others

Dicentrine, (-)-

Cat.No: T20225

Synonym: L-Dicentrine,荷包牡丹碱,NSC 251699,NSC251699,NSC-251699

Target: Others

Cat.No: T5783

Synonym: 野蔷薇苷,罗莎白素

Target: Antioxidant, HIV Protease

1-Hydroxybaccatin I

Cat.No: TN2540

Target: Others

Cat.No: T8169

Target: Others

Cat.No: T6S0627

Synonym: 新乌碱,新乌头碱；中乌头碱

Target: TNF

Cat.No: T5S0662

Synonym: 钩吻碱,Gelsemin

Target: Antioxidant

Cat.No: T3409

Synonym: Y0160,C10485,大车前苷,车前子甙

Target: Others

Cat.No: T3981

Synonym: 4'-Methoxyapigenin,金合欢素,5,7-Dihydroxy-4'-methoxyflavone,Linarigenin

Target: Apoptosis, IAP, COX, Autophagy

Cat.No: T4S1990

Synonym: 香荆芥酚,Karvakrol,O-Thymol,cymophenol,香芹酚

Target: Apoptosis, Others, Gamma-secretase, Endogenous Metabolite, Antifungal

8-Epideoxyloganic acid

Cat.No: T3834

Synonym: 8-表去氧马钱酸

Target: ROS, Immunology/Inflammation related

Cat.No: T6S1579

Synonym: 水晶兰苷,Monotropeine

Target: Others

Dehydrocorydaline nitrate

Cat.No: T2S2362

Synonym: 去氢延胡索甲素硝酸盐,硝酸脱氢紫堇碱

Target: BCL, Others, PARP, p38 MAPK, Caspase, Parasite, Autophagy

Cat.No: T4S0969

Synonym: 决明蒽醌,决明蒽醌；美决明子素

Target: Antioxidant, NF-κB

Cat.No: TCS2336

Target: P-gp

Cat.No: TN3476

Target: Others

Cat.No: TN5404

Cat.No: TN3537

Target: IL Receptor, TNF, NF-κB

Cat.No: TN5147

Target: IL Receptor, TNF, GABA Receptor

Cat.No: TMA0627

Target: TNF

Cat.No: TN4776

Target: TNF, Antifection

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