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Search Results for " capsaicin "

32

抑制剂 & 化合物

13

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T1109	(Z)-Capsaicin Zucapsaicin,Civamide,cis-Capsaicin,珠卡赛辛,(Z)-辣椒素	TRP/TRPV Channel; HSV	Membrane transporter/Ion channel; Microbiology/Virology
	(Z)-Capsaicin (Zucapsaicin) 是天然辣椒素的合成顺式异构体，用于治疗膝骨关节炎。它是一种可口服的 TRPV1激动剂，可研究神经性疼痛。
T16014	Mavatrep JNJ-39439335	TRP/TRPV Channel	Membrane transporter/Ion channel
	Mavatrep (JNJ-39439335) 是一种特异性的 TRPV1 拮抗剂，Ki 为 6.5 nM，可用于炎症性疼痛的研究。
T23322	SB 452533	TRP/TRPV Channel	Membrane transporter/Ion channel
	SB 452533 是TRPV1的选择性拮抗剂，pKb 为 7.8。
T39349	Vocacapsaicin hydrochloride CA-008 hydrochloride	TRP/TRPV Channel	Membrane transporter/Ion channel
	Vocacapsaicin hydrochloride (CA-008 hydrochloride) 是非阿片类 TRPV1 激动剂，是辣椒素的原料，可用于缓解疼痛。
T39348	Vocacapsaicin CA-008,Vocacapsaicin
	Vocacapsaicin (CA-008), a prodrug of Capsaicin and a first-in-class non-opioid TRPV1 agonist, offers significant and enduring pain relief.
T6379	AMG 517 AMG517,N-[4-[[6-[4-(三氟甲基)苯基]-4-嘧啶基]氧基]-2-苯并噻唑基]乙酰胺,AMG-517	TRP/TRPV Channel	Membrane transporter/Ion channel
	AMG 517是一种有效的香草素受体-1 (TRPV1) 拮抗剂，IC50为0.5 nM。
T29522L	(S)-ABT 102	TRP/TRPV Channel	Membrane transporter/Ion channel
	N-[(1S)-5-tert-butyl-2,3-dihydro-1H-inden-1-yl]-N'-1H-indazol-4-ylurea 是一种有效的TRPV1拮抗剂，其IC50为123 nM，可阻断capsaicin 对TRPV1的激活。
T7102	BCTC N-(4-叔丁苯基)-4-(3-氯吡啶-2-基)哌嗪-1-甲酰胺	TRP/TRPV Channel	Membrane transporter/Ion channel
	BCTC 是有效的、特异性的瞬时受体阳离子通道M8(TRPM8)抑制剂。
T1356	4-Hydroxy-3-methoxybenzylamine hydrochloride 香兰素胺盐酸盐,N-Vanillylamine hydrochloride	Others	Others
	4-Hydroxy-3-methoxybenzylamine hydrochloride (N-Vanillylamine hydrochloride) 是一种生物碱，是capsaicin 生物合成的中间体。
T7189	AMG9810 (2E)-N-(2,3-二氢-1,4-苯并二噁英-6-基)-3-[4-(1,1-二甲基乙基)苯基]-2-丙酰胺	TRP/TRPV Channel	Membrane transporter/Ion channel
	AMG9810是高效的，竞争性的香草素受体1选择性拮抗剂，对人类和大鼠TRPV1的IC50分别为24.5 和 85.6 nM。
T4431	Olodanrigan PD-126055,EMA401	RAAS	Endocrinology/Hormones
	Olodanrigan (EMA401) 是具有口服活性、高选择性及外周受限的血管紧张素 Ⅱ 类型 2 受体(AT2R)拮抗剂。它的缓解疼痛的机制可能是：抑制增强的 AngII/AT2R 诱导的 p38 和 p42/p44 MAPK 激活，进而阻碍 DRG 神经元的过度兴奋性及 DRG 神经元的萌发。它可用于研究神经性疼痛。
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。
T37668	CAY10448 CAY10448
	Capsaicin is the primary active component of the heat and pain-eliciting lipid soluble fraction of the Capsicum pepper. Capsaicin signals are transduced by a heat-activated ion channel, the vanilloid receptor 1 (VR1), or transient receptor potential vanilloid 1 (TRPV1). CAY10448 is an iodinated nonivamide, a potent capsaicin receptor antagonist with an IC50 value of approximately 10 nM.
T38277	8-methyl Nonanoic Acid 8-methyl Nonanoic Acid,Isocapric Acid
	Capsaicin, the chemical that imparts the spicy-hot quality of chili peppers, is produced by the fruits of plants belonging to the Capsicum family. 8-methyl Nonanoic acid is an immediate precursor of capsaicin as well as a by-product of capsaicin degradation.[1] Addition of 5 mM of 8-methyl nonanoic acid significantly increases the yield of capsaicin in both immobilized and freely suspended cells of C. frutescens. [2] Capsaicin has reported antimicrobial properties, however isocapric acid can ac...
T68271	AZD1386
	AZD1386 is a TRPV1 antagonist. AZD1386 acts as a competitive antagonist at the channel's capsaicin binding site.
T23944	DA 5018 DA-5018,DA5018
	DA 5018 is a capsaicin derivative and is also a new non-narcotic analgesic. It has an antipruritic effect.
T74742	TRPV1 activator-2
	TRPV1 activator-2 (compound 9)为辣椒素类似物，特异性与脂-水通道残基相互作用。
T37732	AMG 21629
	Potent and selective TRPV1 antagonist. Blocks Ca2+ uptake by CHO cells expressing TRPV1 receptors and acid-induced Ca2+ uptake, respectively). Exhibits >4000-fold selectivity for TRPV1 over other TRP channels. Blocks capsaicin-induced flinch response and causes hyperthermia in rats. Orally available and non-CNS penetrant. Tamayo et al (2008) Design and synthesis of peripherally restricted transient receptor potential vanilloid 1 (TRPV1) antagonists. J.Med.Chem. 51 2744 PMID:18386885 \|Gavva et al...
T74741	TRPV1 activator-1
	TRPV1 activator-1 (compound 8)，一种颈部结构经过改变的辣椒素类似物，特异性与T551残基相互作用。
T61788	TRPV1 antagonist 3
	TRPV1 antagonist 3 (Compound 7q) is a highly potent antagonist of the TRPV1 receptor with an IC50 of 2.66 nM against capsaicin. It exhibits selectivity towards its mode of action and is orally bioavailable (with a bioavailability of 60%). Additionally, it can penetrate the central nervous system [1].
T37086	PDDHV
	PDDHV is a resiniferatoxin-type phorboid vanilloid with capsaicin-like selectivity for the cloned rat transient receptor potential cation channel subfamily V member 1 (TRPV1), formerly known as vanilloid receptor 1. It induces Ca2+-uptake by rat dorsal root ganglion neurons with an EC50 value of 70 nM.
T68904	GW-833972A free base
	GW833972 is a CB2 Agonist. GW 833972A inhibited capsaicin-induced depolarization of the human and guinea-pig and prostaglandin E(2) (PGE(2)) and hypertonic saline-induced depolarization of the guinea-pig isolated vagus nerve in vitro. GW 833972A also inhibited citric acid-induced cough but not plasma extravasation in the guinea-pig and this effect was blocked by a CB(2) receptor antagonist.
T81787	MitTx-beta
	MitTx-beta为一多肽，源自得克萨斯珊瑚蛇(Micrurus tener tener)之毒液。与MitTx-α配对，组成复合物MitTx，此复合物激活ASIC1通道，存在于辣椒素敏感神经纤维上。
T33789	Oleoyl proline N-Oleoyl-l-proline
	Oleoyl proline is an N-acyl amine that can be detected in bovine brain extracts and D. melanogaster larvae using mass spectrometry. In a preclinical model of pain, mice lacking fatty acid amide hydrolase (FAAH KO) had decreased N-oleoyl proline levels in
T21750	A 784168
	A-784168 是一种有效的、口服活性的香草素受体 1 型 (TRPV1) 抑制剂。香草素受体 1 型 (TRPV1) 是一种配体门控非选择性阳离子通道，被认为是各种疼痛刺激 (如内源性脂质、辣椒素、热和低 pH 值) 的重要整合剂。口服给药时，A-784168 具有良好的 CNS 渗透性。
T37670	CAY10568
	Most local anesthetics act by abolishing voltage gated sodium channel currents indiscriminately in all populations of neurons. Selective analgesia through TRPV1-mediated entry of a cationic lidocaine derivative, QX314, was recently reported. CAY10568 is a physically smaller, less hydrophobic version of QX314 designed to be even more permeable to TRPV1 ion channel when activated by agonists such as capsaicin and N-oleoyl dopamine. CAY10568 when given in combination with suitable TRPV1 agonists sh...
T36064	N-Oleoyl Glutamine
	N-Oleoyl glutamine is an endogenous N-acyl amine.1,2It is both formed and degraded by peptidase M20 domain-containing 1 (PM20D1), a factor secreted by thermogenic adipose cells. N-Oleoyl glutamine (50 μM) induces mitochondrial uncoupling to increase respiration in C2C12 cells by 64%.3It inhibits capsaicin-induced calcium flux in HEK293A cells co-transfected with transient receptor potential vanilloid 1 (TRPV1) and red fluorescent protein (RFP).2N-Oleoyl glutamine (100 mg/kg) reduces the number o...
T37167	Reduced Haloperidol
	Reduced haloperidol is an active metabolite of haloperidol . It is formed via reduction of haloperidol by ketone reductase. Reduced haloperidol inhibits radioligand binding to sigma-1 and dopamine D2 receptors (Kis = 1.4 and 31 nM, respectively) and stimulates brain-derived neurotrophic factor (BDNF) secretion from CCF-SSTG1 and U87MG astrocytic glial cells. It also inhibits norepinephrine, dopamine, and serotonin (5-HT) reuptake (Kis = 21, 25, and 33 μM, respectively, in COS-7 cells expressing ...
T36101	Psychotridine
	Psychotridine is an alkaloid that has been found inP. forsterianaand has diverse biological activities.1,2,3It inhibits ADP-, collagen-, or thrombin-induced aggregation of washed isolated human platelets with IC50values of 1.4, 1.4, and 3.9 μM, respectively.1Psychotridine (2.5 or 5 μM) is cytotoxic to HTC rat hepatocellular carcinoma cells.2It reduces paw licking induced by capsaicin in mice when administered at doses of 0.5, 2.5, or 5 mg/kg.3 1.Beretz, A., Roth-Georger, A., Corre, G., et al.Pol...
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。
T71141	Fenspiride-d5
	Fenspiride-d5 is intended for use as an internal standard for the quantification of fenspiride by GC- or LC-MS. Fenspiride is an antagonist of histamine H1 receptors and a non-steroidal anti-inflammatory drug (NSAID). It inhibits histamine-induced contraction of isolated guinea pig trachea but not histamine-induced inotropy of isolated guinea pig heart. It also inhibits phosphodiesterase 4 (PDE4), PDE5, and PDE3 (IC50s = 69, ~158, and 363 µM, respectively, in isolated human bronchi derived from ...
T83732	Tat-CBD3A6K TFA
	Tat-CBD3A6K是一种肽类化合物，为N型电压门控钙通道Cav2.2以及collapsin response mediator protein 2 (CRMP2) 蛋白-蛋白相互作用抑制剂Tat-CBD3的衍生物。Tat-CBD3A6K (10 mg/kg) 能够阻止由d4T (stavudine)引发的大鼠抗逆转录病毒神经病痛模型中爪撤回阈值的下降，并减少同一大鼠分离的背根神经节(DRG)神经元的动作电位数量。通过硬膜途径给予Tat-CBD3A6K (30 µM/animal) 能够减少由萜类生物碱辣椒素引发的大鼠硬脑膜血流增加。

化合物

(Z)-Capsaicin

Cat.No: T1109

Synonym: Zucapsaicin,Civamide,cis-Capsaicin,珠卡赛辛,(Z)-辣椒素

Target: TRP/TRPV Channel, HSV

Cat.No: T16014

Synonym: JNJ-39439335

Target: TRP/TRPV Channel

Cat.No: T23322

Target: TRP/TRPV Channel

Vocacapsaicin hydrochloride

Cat.No: T39349

Synonym: CA-008 hydrochloride

Target: TRP/TRPV Channel

Cat.No: T39348

Synonym: CA-008,Vocacapsaicin

Cat.No: T6379

Synonym: AMG517,N-[4-[[6-[4-(三氟甲基)苯基]-4-嘧啶基]氧基]-2-苯并噻唑基]乙酰胺,AMG-517

Target: TRP/TRPV Channel

Cat.No: T29522L

Target: TRP/TRPV Channel

Cat.No: T7102

Synonym: N-(4-叔丁苯基)-4-(3-氯吡啶-2-基)哌嗪-1-甲酰胺

Target: TRP/TRPV Channel

4-Hydroxy-3-methoxybenzylamine hydrochloride

Cat.No: T1356

Synonym: 香兰素胺盐酸盐,N-Vanillylamine hydrochloride

Target: Others

Cat.No: T7189

Synonym: (2E)-N-(2,3-二氢-1,4-苯并二噁英-6-基)-3-[4-(1,1-二甲基乙基)苯基]-2-丙酰胺

Target: TRP/TRPV Channel

Cat.No: T4431

Synonym: PD-126055,EMA401

Target: RAAS

Cat.No: T37610

Target: Opioid Receptor

Cat.No: T37668

Synonym: CAY10448

8-methyl Nonanoic Acid

Cat.No: T38277

Synonym: 8-methyl Nonanoic Acid,Isocapric Acid

Cat.No: T68271

Cat.No: T23944

Synonym: DA-5018,DA5018

TRPV1 activator-2

Cat.No: T74742

Cat.No: T37732

TRPV1 activator-1

Cat.No: T74741

TRPV1 antagonist 3

Cat.No: T61788

Cat.No: T37086

GW-833972A free base

Cat.No: T68904

Cat.No: T81787

Cat.No: T33789

Synonym: N-Oleoyl-l-proline

Cat.No: T21750

Cat.No: T37670

N-Oleoyl Glutamine

Cat.No: T36064

Reduced Haloperidol

Cat.No: T37167

Cat.No: T36101

Sigma-1 receptor antagonist 5

Cat.No: T78734

Target: Sigma receptor

Cat.No: T71141

Tat-CBD3A6K TFA

Cat.No: T83732

Cat. No.	Product Name	Target	Signaling Pathways
T1062	Capsaicin Qutenza,8-Methyl-N-vanillyl-trans-6-nonenamide,天然辣椒素,Vanilloid,辣椒素,(E)-Capsaicin,Zostrix	Apoptosis; TRP/TRPV Channel; Autophagy	Apoptosis; Autophagy; Membrane transporter/Ion channel
	Capsaicin ((E)-Capsaicin) 属于天然产物，提取自辣椒，是一种 TRPV1 激动剂 (EC50=0.29 μM)。Capsaicin 具有抗肿瘤、抗炎、抗氧化、神经保护等活性。
T39018	Capsaicin β-D-glucopyranoside
	Capsaicin β-D-glucopyranoside, a glucoside converted by Capsaicin, is the bioactive compound found in chili peppers responsible for their characteristic pungent flavor.
T3421	Nordihydrocapsaicin	Others	Others
	Nordihydrocapsaicin(诺地氢辣椒碱)是Capsaicin(辣椒素)的模拟物和同源物，属于在Capsicum(辣椒)中发现的Capsaicinoid(辣椒素类)化合物。
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。
TN1739	Homodihydrocapsaicin I 高二氢辣椒素,高二氢辣椒素I	Others	Others
	Homodihydrocapsaicin I 是一种辣椒素，分离自辣椒果实中。
T82187	Homocapsaicin II
	Homocapsaicin II, 提取自Capsicum annuum L果实，为一种辣椒素类化合物。
T7177	Capsazepine	Apoptosis; TRP/TRPV Channel	Apoptosis; Membrane transporter/Ion channel
	Capsazepine 是一种 TRPV1 受体的拮抗剂， IC50值为 562 nM。它可阻断由激活 TRPV1 离子通道的辣椒素引起的热痛感，是辣椒素拮抗剂。
T5S1389	Escin IB 七叶皂苷B,七叶皂苷 IB	5-HT Receptor; NO Synthase	GPCR/G Protein; Immunology/Inflammation; Neuroscience
	Escin IB 是一种皂苷，分离自马栗子种子的皮和胚乳中，能够抑制 pancreatic lipase 的活性。
T1321	Nonivamide Nonanoic acid vanillylamide,Pelargonic acid vanillylamide,辣椒素,Vanillyl-N-nonylamide,Pseudocapsaicin	TRP/TRPV Channel	Membrane transporter/Ion channel
	Nonivamide (Nonanoic acid vanillylamide) 具有激动活性，在静态毒性检测中，4d-EC50为 5.1 mg/L。
TN2429	Capsiate	Antioxidant; TRP/TRPV Channel	Membrane transporter/Ion channel; oxidation-reduction
	Capsiate 是一种具有口服活性的 TRPV1 激动剂，是非刺激性辣椒素类似物，可作为抗过敏剂，具有抗炎、抗氧、降糖和抑制血管生成活性。
T4513	Vanillyl butyl ether 4-(Butoxymethyl)-2-methoxyphenol,香兰醇丁醚,Butyl vanillyl ether,香草醇丁醚	Others	Others
	Vanillyl butyl ether (Butyl vanillyl ether) 是香草特有风味和香气的来源。它是辣椒素类似物，对人体有感官刺激作用。它是环保且无毒的物质。它是烷氧基取代的苄基衍生物，主要用作调味剂。
TL0018	Lobelin	AChR; Antifection	Microbiology/Virology; Neuroscience
	Inhalation challenge with capsaicin and rapid intravenous injection of Lobelin and alinamin indicated that peripheral c-fiber receptors were involved in the induction of coughing.
TN4440	Limonexic acid	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	Limonexic acid shows antinociceptive actions , it produces dose-related inhibition of glutamate- and capsaicin-induced pain. Limonexic acid can effectively protect hepatocyte against CCl4-induced injury.

天然产物

Cat.No: T1062

Synonym: Qutenza,8-Methyl-N-vanillyl-trans-6-nonenamide,天然辣椒素,Vanilloid,辣椒素,(E)-Capsaicin,Zostrix

Target: Apoptosis, TRP/TRPV Channel, Autophagy

Capsaicin β-D-glucopyranoside

Cat.No: T39018

Nordihydrocapsaicin

Cat.No: T3421

Target: Others

Dihydrocapsaicin

Cat.No: T2163

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

Target: Others, TRP/TRPV Channel

Homodihydrocapsaicin I

Cat.No: TN1739

Synonym: 高二氢辣椒素,高二氢辣椒素I

Target: Others

Homocapsaicin II

Cat.No: T82187

Cat.No: T7177

Target: Apoptosis, TRP/TRPV Channel

Cat.No: T5S1389

Synonym: 七叶皂苷B,七叶皂苷 IB

Target: 5-HT Receptor, NO Synthase

Cat.No: T1321

Synonym: Nonanoic acid vanillylamide,Pelargonic acid vanillylamide,辣椒素,Vanillyl-N-nonylamide,Pseudocapsaicin

Target: TRP/TRPV Channel

Cat.No: TN2429

Target: Antioxidant, TRP/TRPV Channel

Vanillyl butyl ether

Cat.No: T4513

Synonym: 4-(Butoxymethyl)-2-methoxyphenol,香兰醇丁醚,Butyl vanillyl ether,香草醇丁醚

Target: Others

Cat.No: TL0018

Target: AChR, Antifection

Cat.No: TN4440

Target: GABA Receptor

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