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Search Results for " antinociceptive effects "

25

抑制剂 & 化合物

20

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
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。
T28118	MSP3 MSP-3,MSP 3	TRP/TRPV Channel	Membrane transporter/Ion channel
	MSP3 是瞬时受体电位香草素 1 型的激动剂 (EC50 = 0.87 μM) ，具有镇痛和神经保护作用。
T10593	BPR1M97	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	BPR1M97 是一种具有血脑屏障渗透性和有效性的 mu 阿片受体（MOP）和神经肽-啡肽 FQ（NOP）受体激动剂，对 MOP 的 Kis 值为1.8 nM，对 NOP 的Kis 值为 4.2 nM。BPR1M97 具有抗伤害作用和抗痛觉作用。
T17309	(R)-(-)-Ibuprofen levibuprofen,(R)-Ibuprofen	NF-κB	NF-κB
	(R)-(-)-Ibuprofen ((R)-Ibuprofen) 是 Ibuprofen 的 R 型异构体，对 COX 无作用，可以抑制 NF-κB 的活化；(R)-(-)-Ibuprofen 具有抗炎作用，可用于缓解疼痛的研究。
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。
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。
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。
T8414	SNC 80 Snc-80,SNC80,NIH 10815	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	SNC 80 (NIH 10815) 是有效的，高度选择性的非肽类 δ 阿片 (δ-opioid) 受体激动剂，Ki 为1.78 nM，IC50 为 2.73 nM。SNC80 还以 EC50 为 52.8 nM 来选择性激活 HEK293 细胞中的 μ-δ 异聚体。SNC80 具有抗伤害性，抗痛觉过敏和抗抑郁样作用，并可用于多种头痛症的研究。
T11721L	JDTic dihydrochloride	JAK	Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells
	JDTic is a potent antagonist of kappa-opioid receptors (KOR), blocking the κ-agonist U50, 488-induced antinociception.
T61708	AZD 2066 hydrate
	AZD 2066 hydrate is a selective, orally active, and brain-penetrant antagonist of mGluR5. It exhibits antinociceptive effects [1].
T28516	ReN-1869 NNC-05-1869,NNC 05-1869,NNC-051869,ReN 1869
	ReN-1869 is a histamine H1 receptor antagonist. ReN 1869 is active against inflammation and neurogenic pain. ReN-1869 produces potent and selective antinociceptive effects on dorsal horn neurons after inflammation and neuropathy.
TP1529	Galanin (1-19), human
	Galanin (1-19), human, represents the fragment encompassing amino acids 1 to 19 of the human galanin neuropeptide. Galanin (GAL) is known for its extensive distribution and multifaceted biological roles, such as regulating hormone secretion, providing antinociceptive effects, and altering feeding behavior.
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
T73307	TrkA-IN-4
	TrkA-IN-4 是一种有效和具有口服活性的 TrkA 变构抑制剂，是TrkA-IN-3 的前药。TrkA-IN-4 显示出有效的抗伤害作用。
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.
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.
T73562	DALDA
	DALDA 是一种强效和高选择性μ-opioid receptor 激动剂，其Ki 为 1.69 nM。 DALDA 具有抗痛和呼吸作用。
T76439	DALDA acetate
	DALDA acetate 是一种强效和高选择性μ-opioid receptor 激动剂，其Ki 为 1.69 nM。DALDA acetate 具有抗痛和呼吸作用。
T40119	TC-2559 difumarate
	TC-2559 idifumarate is a CNS-selective, orally active α4β2 subtype of nicotinic acetylcholine receptor (nAChR) partial agonist with an EC 50 of 0.18 μM. It exhibits selectivity for α4β2 receptors over α2β4, α4β4, and α3β4 receptors, with EC 50 s ranging from 10 to 30 μM. TC-2559 difumarate also demonstrates antinociceptive effects.
T74651	L-Inosine
	L-Inosine 是 L-构型形式的 Inosine。Inosine 是一种由腺苷分解代谢产生的内源性嘌呤核苷。Inosine 具有抗炎免疫调节，抗伤害和神经保护作用。
T75799	Hemopressin(human, mouse) TFA	Cannabinoid Receptor	GPCR/G Protein
	Hemopressin TFA，一种衍生自血红蛋白α1链的九肽，最初自大鼠脑匀浆分离。作为口服活性且选择性的CB1大麻素受体反向激动剂，Hemopressin TFA在炎性疼痛模型中具有抗伤害感受效应。
T75798	Hemopressin(rat) TFA
	Hemopressin(rat) TFA，一种衍生自α1-珠蛋白九肽，最初分离自大鼠脑匀浆。该化合物通过口服能有效选择性地作为CB1大麻素受体的反向激动剂，并在炎性疼痛模型中表现出抗伤害感受活性。
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。
T62631	CB2 receptor antagonist 1
	己基间苯二酚衍生物29作为CB2选择性竞争性拮抗剂/反向激动剂，显示出优异的效力。另外，橄榄醇与5-（2-甲基辛烷-2-基）间苯二酚衍生物23和24均展现出显著的抗伤害感受活性，且化合物24能有效激活大麻素和TRPV1受体。
T73631	(Rac)-SNC80
	(Rac)-SNC80 是SNC80 的外消旋体。SNC80 (NIH 10815) 是一种有效的，高度选择性的非肽类 δ 阿片 (δ-opioid) 受体激动剂，Ki 为1.78 nM，IC50为 2.73 nM。SNC80 具有抗伤害性，抗痛觉过敏和抗抑郁样作用，并可用于多种头痛症的研究。

化合物

Cat.No: T9461

Target: Sodium Channel

Cat.No: T28118

Synonym: MSP-3,MSP 3

Target: TRP/TRPV Channel

Cat.No: T10593

Target: Opioid Receptor

(R)-(-)-Ibuprofen

Cat.No: T17309

Synonym: levibuprofen,(R)-Ibuprofen

Target: NF-κB

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

Cat.No: TP1212

Synonym: Boc-FLFLF

Target: Others

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

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: T8414

Synonym: Snc-80,SNC80,NIH 10815

Target: Opioid Receptor

JDTic dihydrochloride

Cat.No: T11721L

Target: JAK

AZD 2066 hydrate

Cat.No: T61708

Cat.No: T28516

Synonym: NNC-05-1869,NNC 05-1869,NNC-051869,ReN 1869

Galanin (1-19), human

Cat.No: TP1529

Cat.No: T27968

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

Cat.No: T73307

Cat.No: T72007

Ziconotide TFA (107452-89-1 free base)

Cat.No: TP1471

Synonym: Ziconotide TFA

Cat.No: T73562

Cat.No: T76439

TC-2559 difumarate

Cat.No: T40119

Cat.No: T74651

Hemopressin(human, mouse) TFA

Cat.No: T75799

Target: Cannabinoid Receptor

Hemopressin(rat) TFA

Cat.No: T75798

Sigma-1 receptor antagonist 5

Cat.No: T78734

Target: Sigma receptor

CB2 receptor antagonist 1

Cat.No: T62631

Cat.No: T73631

Cat. No.	Product Name	Target	Signaling Pathways
T8014	Epoxylinalool 氧化芳樟醇,2-(2-Hydroxy-2-Propyl)-5-Methyl-5-Vinyltetrahydrofuran	Others	Others
	Epoxylinalool (2-(2-Hydroxy-2-Propyl)-5-Methyl-5-Vinyltetrahydrofuran) 是一种天然存在的单萜醇，广泛用于香水和调味品的生产。
T7907	7-Methoxyflavone	Others	Others
	7-Methoxyflavone 是一种分离自 Zornia brasiliensis 的化合物。它能够抑制福尔马林疼痛反应神经源期的舔爪时间 (65.6%)，有外周镇痛活性，但不影响炎症期的伤害性反映。
T2757	Myricitrin 杨梅苷,Myricetrin,Myricitrine	PKC	Chromatin/Epigenetic; Cytoskeletal Signaling
	Myricitrin (Myricitrine) 是从杨梅根皮中分离出来的类黄酮化合物，具有镇痛作用。它是主要的抗氧化剂。
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。
TN1413	Atranorin 荔枝素，巴美灵,荔枝素	Endogenous Metabolite; NO Synthase; Ras	GPCR/G Protein; Immunology/Inflammation; MAPK; Metabolism
	Atranorin 是地衣的次生代谢产物，具有显着的抗伤害、抗炎和氧化还原活性，对 H(2)O(2) 诱导的氧化应激下的细胞具有细胞保护作用。
TN1377	α-Spinasterol Α-波菜甾醇,alpha-Spinasterol,菠甾醇	COX; Antibacterial; TRP/TRPV Channel	Immunology/Inflammation; Membrane transporter/Ion channel; Microbiology/Virology; Neuroscience
	α-Spinasterol 是一种从Spinacia oleracea 分离的瞬时受体电位香草酸 1 拮抗剂，具有抗菌、抗炎、抗抑郁、抗氧化和抗伤害作用。它抑制COX-1和COX-2活性，IC50值分别为 16.17 μM 和 7.76 μM。
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。
T3254	PHYTOL 植醇,trans-Phytol,(E)-Phytol	Antibacterial; PPAR; Parasite	DNA Damage/DNA Repair; Metabolism; Microbiology/Virology
	PHYTOL (trans-Phytol) 是一种从叶绿素中提取的二萜醇，广泛应用于食品添加剂和医药领域，具有很好的抗血吸虫特性。它具有抗伤害、抗氧化、抗炎、抗过敏等作用。它对结核分枝杆菌和金黄色葡萄球菌具有抗菌活性。
T5S2358	Dehydrocorydaline Dehydrocorydalin,脱氢紫堇碱,13-Methylpalmatine	BCL; PARP; p38 MAPK; Caspase; Parasite; Autophagy	Apoptosis; Autophagy; Chromatin/Epigenetic; DNA Damage/DNA Repair; MAPK; Microbiology/Virology; Proteases/Proteasome
	Dehydrocorydaline (13-Methylpalmatine) 是一种生物碱。它调节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、抗癌等功效。它具有强大的抗疟疾作用，并具低细胞毒性。
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。
TN1989	Niga-ichigoside F1 苦莓苷F1	Others; Nrf2	Immunology/Inflammation; Others
	Niga-ichigoside F1(NI) has anti-inflammatory, gastroprotective ,antinociceptive, and cytotoxic effects.
TN4149	Glyasperin F	Others	Others
	Glyasperin F has antinociceptive, and anti-inflammatory effects, it could inhibit NO production in RAW 264.7 macrophages to some extent. Glyasperin F displayed cytotoxic effects against the four tested cancer cell lines with IC50values below 85 μM.
TN1549	Damnacanthal 丹宁卡	IL Receptor; Akt; Syk	Angiogenesis; Cytoskeletal Signaling; Immunology/Inflammation; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors
	Damnacanthal possesses anti-cancer, immunomodulatory, antinociceptive and anti-inflammatory actions, it can treat or prevent hepatocellular carcinoma through its inhibitory effects on the HGF/c-Met axis.
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.
TN5019	Siegeskaurolic acid	TNF; NOS; NF-κB; COX; NO Synthase; Prostaglandin Receptor	Apoptosis; GPCR/G Protein; Immunology/Inflammation; Neuroscience; NF-κB
	Siegeskaurolic acid 是一种具有抗炎活性的天然产物。
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.
TN2072	Picroside IV	Others	Others
	Kutkoside is a mixture of iridoid glycosides namely, picroside II, Picroside IV and 6-ferulloylcatalpol, it may have antinociceptive and anti-inflammatory effects.
TN1080	Kaji-ichigoside F1 蔷薇苷
	Kaji-ichigoside F1 shows antiinflammatory/antinociceptive action in acetic acid-induced writhing and hot plate testing and in a carrageenan-induced paw edema model in mice and rats. Kaji-ichigoside F1 exhibits in vivo hepatoprotective effects, it inhibite
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
TN6570	Daturaolone
	Daturaolone has potency in reducing the harmful effects or in maintaining the normal hepatic physiological mechanisms in both acute and chronic hepato-toxic induced liver damage in rats. Daturaolone also possesses in vivo anti-inflammatory and antinocicep

天然产物

Cat.No: T8014

Synonym: 氧化芳樟醇,2-(2-Hydroxy-2-Propyl)-5-Methyl-5-Vinyltetrahydrofuran

Target: Others

7-Methoxyflavone

Cat.No: T7907

Target: Others

Cat.No: T2757

Synonym: 杨梅苷,Myricetrin,Myricitrine

Target: PKC

Cat.No: T4S1990

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

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

Cat.No: TN1413

Synonym: 荔枝素，巴美灵,荔枝素

Target: Endogenous Metabolite, NO Synthase, Ras

Cat.No: TN1377

Synonym: Α-波菜甾醇,alpha-Spinasterol,菠甾醇

Target: COX, Antibacterial, TRP/TRPV Channel

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: T3254

Synonym: 植醇,trans-Phytol,(E)-Phytol

Target: Antibacterial, PPAR, Parasite

Dehydrocorydaline

Cat.No: T5S2358

Synonym: Dehydrocorydalin,脱氢紫堇碱,13-Methylpalmatine

Target: BCL, 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

Niga-ichigoside F1

Cat.No: TN1989

Synonym: 苦莓苷F1

Target: Others, Nrf2

Cat.No: TN4149

Target: Others

Cat.No: TN1549

Synonym: 丹宁卡

Target: IL Receptor, Akt, Syk

Cat.No: TN3537

Target: IL Receptor, TNF, NF-κB

Siegeskaurolic acid

Cat.No: TN5019

Target: TNF, NOS, NF-κB, COX, NO Synthase, Prostaglandin Receptor

Cat.No: TN5147

Target: IL Receptor, TNF, GABA Receptor

Cat.No: TN2072

Target: Others

Kaji-ichigoside F1

Cat.No: TN1080

Synonym: 蔷薇苷

Cat.No: TN5404

Cat.No: TN6570

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