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Search Results for " bronchoconstriction "

33

抑制剂 & 化合物

1

天然产物

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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
	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
	S 9795 is a methylxanthine derivative and acts as a potent inhibitor of bronchoconstriction in vivo.
T36770	11-deoxy Prostaglandin E1 11-deoxy Prostaglandin E1
	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。
T26811	BI-L 239 BIL239,Enofelast,BI-L-239
	BI-L 239 is an inhibition of 5-lipoxygenase products that cause bronchoconstriction.
T71541	ASP9133
	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.
T28015	Mequitamium iodide LG-30435,LG 30435,LG30435
	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
T68723	FPL-59257
	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
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
	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]。
T21951	CDP 840 hydrochloride
	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。
T36214	16,16-dimethyl Prostaglandin E1 16,16-dimethyl Prostaglandin E1
	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。
T38157	Ricinelaidic Acid
	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%.
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 ...
T70376	CHF-6366
	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。
T70377	BAY 61-3606 HCl
	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...
T70456	Nolpitantium Free Base
	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...
T37620	Leukotriene C4 methyl ester
	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...
T37728	Methoctramine (hydrate)
	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...
T60332	Methacholine bromide
	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]。
T38128	Leukotriene D4 Leukotriene D4 MaxSpec® Standard,LTD4
	Leukotriene D4 (LTD4) is one of the constituents of slow-reacting substance of anaphylaxis (SRS-A) produced by the metabolism of LTC4 by γ-glutamyl transpeptidase. It is the first cysteinyl-leukotriene metabolite of LTC4 . Like LTC4, LTD4-induced bronchoconstriction and enhanced vascular permeability contribute to the pathogenesis of asthma and acute hypersensitivity. LTD4 is equipotent to LTC4 in its biological activities, except that LTD4 is nearly 100-fold more effective in the contraction of...
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
	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

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

11-deoxy Prostaglandin E1

Cat.No: T36770

Synonym: 11-deoxy Prostaglandin E1

Cat.No: T26811

Synonym: BIL239,Enofelast,BI-L-239

Cat.No: T71541

Mequitamium iodide

Cat.No: T28015

Synonym: LG-30435,LG 30435,LG30435

Cat.No: T68723

Cat.No: T15415

Target: Others

Cat.No: TP1999

Cat.No: T75283

CDP 840 hydrochloride

Cat.No: T21951

16,16-dimethyl Prostaglandin E1

Cat.No: T36214

Synonym: 16,16-dimethyl Prostaglandin E1

Ricinelaidic Acid

Cat.No: T38157

Cat.No: T71141

Cat.No: T70376

BAY 61-3606 HCl

Cat.No: T70377

Nolpitantium Free Base

Cat.No: T70456

Leukotriene C4 methyl ester

Cat.No: T37620

Methoctramine (hydrate)

Cat.No: T37728

Methacholine bromide

Cat.No: T60332

Cat.No: T38128

Synonym: Leukotriene D4 MaxSpec® Standard,LTD4

Tirzepatide sodium

Cat.No: T83906

Synonym: LY3298176

Cat.No: T36618

Cat. No.	Product Name	Target	Signaling Pathways
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: T2520

Synonym: Sch34117,地氯雷他定,NSC 675447

Target: Endogenous Metabolite, Histamine Receptor

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