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Search Results for " bronchoconstriction "

Targets Recommended: Leukotriene Receptor

31

抑制剂 & 化合物

2

天然产物

1

重组蛋白

2

同位素标记化合物

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Cat. No.	Product Name	Target	Signaling Pathways
T26519	Ablukast Ro 23-3544,阿鲁司特	Leukotriene Receptor	GPCR/G Protein
	Ablukast (Ro 23-3544) 是白三烯受体的选择性拮抗剂，也是LTD4受体拮抗剂。可改善 LTC4 和抗原诱导的支气管狭窄。
T6397	Atracurium besylate Tracrium,51W89,BW-33A,苯磺酸阿曲库铵	AChR	Neuroscience
	Atracurium besylate (51W89) 是一种神经肌肉阻断剂，ED95为0.2 mg/kg。
T1682	Methacholine Chloride 醋甲胆碱,Mecholyl chloride,氯化乙酰甲胆碱,Acetyl-β-methylcholine chloride	AChR	Neuroscience
	Methacholine Chloride (Acetyl-β-methylcholine chloride) 是副交感神经系统中的毒蕈碱-3 受体激动剂。它可用于测量气道高反应性，作为评估哮喘样症状和正常静息呼气流速的诊断辅助手段。它直接作用于平滑肌上的乙酰胆碱受体，引起收缩和气道狭窄。
T3148	MK-571 sodium L-660711 (sodium salt),L-660711 sodium salt,Verlukast sodium,L-660711,MK571,MK-571 sodium salt,Propanoic acid	Leukotriene Receptor; LTR	GPCR/G Protein; Immunology/Inflammation
	MK-571 sodium (L-660711 sodium salt) 是一种可口服的选择性白三烯 D4受体拮抗剂，在豚鼠和人肺膜的 Ki 分别为0.22 和 2.1 nM。
T22787	FPL 55712	LTR	Immunology/Inflammation
	FPL 55712 是白三烯受体和 SRS-A 拮抗剂，抑制支气管收缩，可用于研究哮喘和冠状动脉血栓。
T67957	Pipoxizine	Others	Others
	Pipoxizine 对组胺所致的支气管收缩具有拮抗作用，可用于研究哮喘疾病。
T68090	Laprafylline	Others	Others
	Laprafylline 是一种黄嘌呤化合物，对体内支气管收缩有抑制作用，且具有抗肿瘤活性。Laprafylline在低浓度时可充当竞争性血清素能拮抗剂，在高难度时抑制由hist引起的收缩。
T68094	Lodoxamide ethyl	Others	Others
	lodoxamide ethyl 是一种新的口服活性抗过敏化合物，可用于预防抗原诱导的支气管收缩和阻断皮肤过敏反应。
T11388	Gemilukast ONO-6950	Others	Others
	Gemilukast（ONO-6950）是一种具有口服活性和有效性的半胱氨酰白三烯 1 和 2 受体 (CysLT1 和CysLT2) 双重抑制剂，抑制 LTC 4 诱导的支气管收缩，对人 CysLT1 和 CysLT2 有抑制作用，可用于治疗哮喘。
T68173	ZD-2138 Ici-D2138	Lipoxygenase	Metabolism
	ZD-2138是一种有效且具有选择性的5-脂氧合酶（5-LOX）的特异性抑制剂，抑制了过敏原诱导的肺支气管收缩，可减少豚鼠孤立气道的神经诱发性快速激肽能收缩。ZD-2138可用来治疗哮喘疾病。
T1115	Doxylamine succinate 琥珀酸多西拉敏,Decapryn	Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Neuroscience
	Doxylamine succinate (Decapryn) 是一种吡啶衍生物组胺 H1 拮抗剂，具有明显的镇静特性。它竞争性阻断组胺 H1 受体并限制典型的过敏和过敏反应，可防止组胺引起的皮肤和粘膜疼痛和瘙痒。
T71412	S 9795	Others	Others
	S 9795 is a methylxanthine derivative and acts as a potent inhibitor of bronchoconstriction in vivo.
T26811	BI-L 239 BIL239,Enofelast,BI-L-239	Others	Others
	BI-L 239 is an inhibition of 5-lipoxygenase products that cause bronchoconstriction.
T71541	ASP9133	Others	Others
	ASP9133 is a long-acting muscarinic antagonist (LAMA) which shows more selective inhibition of bronchoconstriction against salivation and more rapid onset of action than tiotropium bromide.
T68723	FPL-59257	Others	Others
	FPL-59257 is a leukotriene antagonist that has been shown to abolish cough response & partly inhibit bronchoconstriction produced by leukotrienes C & D.
T15415	GR 159897	Others	Others
	GR 159897 is a competitive, brain-penetrated non-peptide NK2 receptor antagonist with anti-tumor effects. GR 159897 inhibits binding of [3H]GR100679 to human NK2-CHO cells and rat colon membranes (pKis: 9.51 and 10, respectively). It can antagonize bronch
T36770	11-deoxy Prostaglandin E1 11-deoxy Prostaglandin E1	Others	Others
	11-deoxy Prostaglandin E1 是前列腺素 E1类似物，具有支气管扩张活性，可抑制组胺诱导的支气管收缩，引起离体豚鼠的气管条松弛。
T28015	Mequitamium iodide LG-30435,LG 30435,LG30435	Others	Others
	Mequitamium iodide is a platelet activating factor (PAF) inhibitor. Mequitamium inhibits PAF-acether induced platelet aggregation and bronchoconstriction. Mequitamium is capable of inhibiting platelet-mediated effects of PAF by interfering with secondary
TP1999	MEN 11270
	Peptide antagonist of the B2 bradykinin receptor (pKi = 10.3); conformationally constrained cyclized analog of HOE 140. Blocks hypotension and bronchoconstriction in vivo. Displays selectivity for B2 over 29 other receptors and ion channels (pIC50 < 5.5).
T75283	Atracurium	Others	Others
	Atracurium (BW-33A free acid)为高效的竞争性非去极化神经肌肉阻滞剂，兼具AChR受体拮抗作用。该化合物能够诱导支气管收缩及实现神经肌肉阻滞，并促进星形胶质细胞分化[5]。
T36214	16,16-dimethyl Prostaglandin E1 16,16-dimethyl Prostaglandin E1	Others	Others
	16,16-dimethyl Prostaglandin E1 是 PGE1 (T1626) 类似物，可诱导支气管收缩和血管平滑肌收缩，并抑制吲哚美辛诱导的细胞伸长。
T21951	CDP 840 hydrochloride	Others	Others
	CDP-840 (GR259653X) 是一种有效的、选择性和口服活性的phosphodiesterase IV (PDE IV)抑制剂。CDP-840 抑制有意识的松鼠猴中抗原诱导的早期和晚期支气管收缩。
T38157	Ricinelaidic Acid	Others	Others
	Ricinelaidic acid is a 12-hydroxy fatty acid and an antagonist of leukotriene B4 (LTB4) receptors (Ki = 2 μM in porcine neutrophil membranes). It inhibits chemotaxis and calcium flux induced by LTB4 in isolated human neutrophils (IC50s = 10 and 7 μM, respectively). Ricinelaidic acid (1 mg/kg, i.v.) inhibits bronchoconstriction induced by LTB4 in rats by 46%.
T70377	BAY 61-3606 HCl	Others	Others
	BAY 61-3606 HCl is a cell-permeable, reversible inhibitor of spleen tyrosine kinase. BAY 61-3606 HCl can inhibit degranulation and block cytokine release from mast cells. Oral administration of BAY 61-3606 to rats was shown to suppress antigen-induced passive cutaneous anaphylactic reaction, bronchoconstriction, and bronchial edema. It can also sensitize MCF-7 breast cancer cells to TNF-related apoptosis-inducing ligand (TRAIL)-mediated apoptosis by inhibiting Cdk9. This compound has been used i...
T70376	CHF-6366	Others	Others
	CHF-6366是一种高效的M3毒蕈碱拮抗剂和β2肾上腺素能受体激动剂，具有pKi值分别为10.4和11.4。同时，CHF-6366作为一种弱钙离子通道抑制剂，其IC50约为50μM。该化合物能够抑制豚鼠的支气管收缩，适用于慢性阻塞性肺疾病研究。
T37620	Leukotriene C4 methyl ester	Others	Others
	Leukotriene C4 (LTC4) is the parent cysteinyl-leukotriene produced by the LTC4 synthase-catalyzed conjugation of glutathione to LTA4. LTC4 is produced by neutrophils, macrophages, and mast cells, and by transcellular metabolism in platelets. It is one of the constituents of slow-reacting substance of anaphylaxis (SRS-A) and exhibits potent smooth muscle contracting activity. LTC4-induced bronchoconstriction and enhanced vascular permeability contribute to the pathogenesis of asthma and acute all...
T70456	Nolpitantium Free Base	Others	Others
	Nolpitantium Free Base is a highly selective nonpeptide antagonist of neurokinin-1 (NK1) receptor. Nolpitantium potently, selectively and competitively inhibited substance P binding to NK1 receptors from various animal species, including humans. In vitro, it was a potent antagonist in functional assays for NK1 receptors such as [Sar9, Met(O2)11]substance P-induced endothelium-dependent relaxation of rabbit pulmonary artery and contraction of guinea-pig ileum. Up to 1 mkM, Nolpitantium had no eff...
T60332	Methacholine bromide	Others	Others
	Methacholine (Acetyl-β-methylcholine) bromide 是一种有效的muscarinic-3 (M3)激动剂。Methacholine bromide 直接作用于平滑肌上的乙酰胆碱受体，导致支气管收缩和气道变窄。Methacholine bromide 对识别支气管高反应性 (BHR) 显示出高灵敏度，BHR 是哮喘的重要特征。Methacholine bromide 可用于测量气道高反应性 (AHR)，作为评估具有哮喘样症状和正常静息呼气流速的个体的诊断辅助[2]。
T37728	Methoctramine (hydrate)	Others	Others
	Methoctramine is a selective antagonist of M2 muscarinic acetylcholine receptors (IC50 = 6.1 nM in CHO-K1 cell membranes).[1] It is selective for M2 over M1, M3, M4, and M5 receptors (IC50s = 92, 770, 260, and 217 nM, respectively). In vitro, methoctramine inhibits acetylcholine-induced reductions in isolated guinea pig tracheal tube contractions when used at a concentration of 1 μM.[2] In vivo, methoctramine inhibits bradycardia and bronchoconstriction induced by acetylcholinein guinea pigs wit...
T83906	Tirzepatide sodium LY3298176
	Tirzepatide 是一种glucagon-like peptide 1 receptor (GLP-1R) 和 G protein-coupled receptor 119 (GPR119)的激动剂。它在表达人类GLP-1R或GPR119的HEK293细胞中诱导cAMP的产生（EC50s分别为6.54和1.01 nM）。Tirzepatide（100 nM）在表达人类GLP-1R或GPR119的HEK293细胞中诱导受体内化。在体内，Tirzepatide（每天10 nmol/kg）降低高脂饮食诱导的肥胖小鼠模型的体重、食物摄入量、血浆leptin、三酸甘油酯和free fatty acids (FFAs)水平、肝脏三酸甘油酯和血糖水平。它通过每三天给药50 nmol/kg的剂量，阻止A. alternata诱导的A. alternata挑战小鼠的支气管肺泡灌洗液（BALF）中嗜酸性粒细胞和淋巴细胞数量的增加。Tirzepatide（每三天50 nmol/kg）抑制由毒蕈碱受体激动剂methacholine (acetyl-β-methylcholine)导致的在糖尿病诱导的哮喘...
T36618	Rupatadine	Others	Others
	Rupatadine (UR-12592) is a potent dual PAF/H1 antagonist with Ki of 0.55/0.1 uM(rabbit platelet membranes/guinea pig cerebellum membranes).IC50 value:Target: PAF/H1 antagonistin vitro: Rupatadine competitively inhibited histamine-induced guinea pig ileum contraction (pA2 = 9.29 +/- 0.06) without affecting contraction induced by ACh, serotonin or leukotriene D4 (LTD4). It also competitively inhibited PAF-induced platelet aggregation in washed rabbit platelets (WRP) (pA2 = 6.68 +/- 0.08) and in hu...

化合物

Cat.No: T26519

Synonym: Ro 23-3544,阿鲁司特

Target: Leukotriene Receptor

Atracurium besylate

Cat.No: T6397

Synonym: Tracrium,51W89,BW-33A,苯磺酸阿曲库铵

Target: AChR

Methacholine Chloride

Cat.No: T1682

Synonym: 醋甲胆碱,Mecholyl chloride,氯化乙酰甲胆碱,Acetyl-β-methylcholine chloride

Target: AChR

Cat.No: T3148

Synonym: L-660711 (sodium salt),L-660711 sodium salt,Verlukast sodium,L-660711,MK571,MK-571 sodium salt,Propanoic acid

Target: Leukotriene Receptor, LTR

Cat.No: T22787

Target: LTR

Cat.No: T67957

Target: Others

Cat.No: T68090

Target: Others

Lodoxamide ethyl

Cat.No: T68094

Target: Others

Cat.No: T11388

Synonym: ONO-6950

Target: Others

Cat.No: T68173

Synonym: Ici-D2138

Target: Lipoxygenase

Doxylamine succinate

Cat.No: T1115

Synonym: 琥珀酸多西拉敏,Decapryn

Target: Histamine Receptor

Cat.No: T71412

Target: Others

Cat.No: T26811

Synonym: BIL239,Enofelast,BI-L-239

Target: Others

Cat.No: T71541

Target: Others

Cat.No: T68723

Target: Others

Cat.No: T15415

Target: Others

11-deoxy Prostaglandin E1

Cat.No: T36770

Synonym: 11-deoxy Prostaglandin E1

Target: Others

Mequitamium iodide

Cat.No: T28015

Synonym: LG-30435,LG 30435,LG30435

Target: Others

Cat.No: TP1999

Cat.No: T75283

Target: Others

16,16-dimethyl Prostaglandin E1

Cat.No: T36214

Synonym: 16,16-dimethyl Prostaglandin E1

Target: Others

CDP 840 hydrochloride

Cat.No: T21951

Target: Others

Ricinelaidic Acid

Cat.No: T38157

Target: Others

BAY 61-3606 HCl

Cat.No: T70377

Target: Others

Cat.No: T70376

Target: Others

Leukotriene C4 methyl ester

Cat.No: T37620

Target: Others

Nolpitantium Free Base

Cat.No: T70456

Target: Others

Methacholine bromide

Cat.No: T60332

Target: Others

Methoctramine (hydrate)

Cat.No: T37728

Target: Others

Tirzepatide sodium

Cat.No: T83906

Synonym: LY3298176

Cat.No: T36618

Target: Others

Cat. No.	Product Name	Target	Signaling Pathways
T25687	Leukotriene C4 LTC4,Leukotriene C	Endogenous Metabolite	Metabolism
	Leukotriene C4 (LTC4) 是一种类花生酸脂质介质，可调节炎症部位白细胞的募集和功能。Leukotriene C4 是支气管收缩、粘液分泌过多和嗜酸性粒细胞增多的介质，在荨麻疹中具有介导作用。
T2520	Desloratadine Sch34117,地氯雷他定,NSC 675447	Endogenous Metabolite; Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Metabolism; Neuroscience
	Desloratadine (Sch34117) 是非镇静H1抗组胺药 Loratadine 的主要口服代谢物，可减少对支气管平滑肌、毛细血管和胃肠道平滑肌中 H1 受体的典型组胺能作用，包括血管舒张、支气管收缩、血管通透性增加、疼痛、瘙痒和胃肠道平滑肌的痉挛性收缩。它是一种选择性H1受体拮抗剂，具有抗过敏和抗炎活性。

天然产物

Cat.No: T25687

Synonym: LTC4,Leukotriene C

Target: Endogenous Metabolite

Cat.No: T2520

Synonym: Sch34117,地氯雷他定,NSC 675447

Target: Endogenous Metabolite, Histamine Receptor

Species：

Expression System：

Tag：

Cat. No.	Product Name	Species	Expression System
TMPH-03749	CYSLTR1 Protein, Human, Recombinant (His) Cysteinyl leukotriene receptor 1,G-protein coupled receptor ...	Human	E. coli
	Receptor for cysteinyl leukotrienes mediating bronchoconstriction of individuals with and without asthma. Stimulation by LTD4 results in the contraction and proliferation of smooth muscle, edema, eosinophil migration and damage to the mucus layer in the lung. This response is mediated via a G-protein that activates a phosphatidylinositol-calcium second messenger system. The rank order of affinities for the leukotrienes is LTD4 >> LTE4 = LTC4 >> LTB4.

重组蛋白

CYSLTR1 Protein, Human, Recombinant (His)

Cat.No: TMPH-03749

Species: Human

Expression System: E. coli

Cat. No.	Product Name	Target	Signaling Pathways
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 ...
TMIJ-0202	Desloratadine-d5
	Desloratadine-d5 是 Desloratadine 的氘代化合物。Desloratadine 的 CAS 号为 100643-71-8。Desloratadine 是非镇静H1抗组胺药 Loratadine 的主要口服代谢物，可减少对支气管平滑肌、毛细血管和胃肠道平滑肌中 H1 受体的典型组胺能作用，包括血管舒张、支气管收缩、血管通透性增加、疼痛、瘙痒和胃肠道平滑肌的痉挛性收缩。它是一种选择性H1受体拮抗剂，具有抗过敏和抗炎活性。

同位素标记化合物

Cat.No: T71141

Desloratadine-d5

Cat.No: TMIJ-0202

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