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左羟丙哌嗪 /Levodropropizine {[allProObj[0].p_purity_real_show]}

货号:A728009 同义名: (S)-(-)-Dropropizine;DF-526

Levodropropizine is a histamine receptor inhibitor, and is an effective and very well tolerated peripheral antitussive drug.

Levodropropizine 化学结构 CAS号:99291-25-5
Levodropropizine 化学结构
CAS号:99291-25-5
Levodropropizine 3D分子结构
CAS号:99291-25-5
Levodropropizine 化学结构 CAS号:99291-25-5
Levodropropizine 3D分子结构 CAS号:99291-25-5
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Levodropropizine 纯度/质量文件 产品仅供科研

货号:A728009 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 H1 receptor H2 receptor H3 receptor H4 receptor Histamine receptor 其他靶点 纯度
Hydroxyzine 2HCl 99+%
Cyclizine 97%
Loratadine +

B(0)AT2, IC50: 4 μM

98%
Desloratadine ++

Histamine H1 receptor, IC50: 51 nM

98%
Doxylamine succinate 99%
Ebastine 98%
Tripelennamine HCl +

H1 receptor, IC50: 30 μM

98%
Meclizine dihydrochloride 98%
Chlorpheniramine maleate +++

Histamine H1 receptor, IC50: 12 nM

99%
Diphenhydramine HCl 99%
Alcaftadine ++++

H1 receptor, pKi: 8.5

++

H2 receptor, pKi: 7.2

99%+
Fexofenadine HCl ++

Histamine H1 receptor, IC50: 246 nM

99%+
Bilastine +++

H1 receptor, Ki: 44.15 nM

98%
Pemirolast potassium 98%
Bepotastine besilate +

Histamine H1 receptor, pIC50: 5.7

98%
Mizolastine +++

Histamine H1 receptor, IC50: 47 nM

98%
Brompheniramine maleate 98%
Carbinoxamine maleate salt 99+%
Clemastine fumarate ++++

Histamine H1 receptor, IC50: 3 nM

98%
Ketotifen fumarate salt 95%
Rupatadine Fumarate ++

Histamine H1 receptor, Ki: 102 nM

PAFR 98%
Famotidine 97%
Roxatidine Acetate HCl +

Histamine H2 receptor, IC50: 3.2 μM

98%
Lafutidine 99%
Cimetidine 98%
Nizatidine ++++

Histamine H2 receptor, IC50: 0.9 nM

AChE 98%
Ranitidine 98%
Betahistine +

Histamine H3 receptor, IC50: 1.9 μM

98%
Ciproxifan maleate +++

Histamine H3 receptor, IC50: 9.2 nM

99%+
S 38093 ++

human H3 receptor, Ki: 1.2 μM

rat H3 receptor, Ki: 1.44 μM

98%
JNJ-7777120 ++++

Histamine H4 receptor, Ki: 4.5 nM

98%
Azelastine HCl 98%
Epinastine HCl 98%
Levodropropizine 97%
Cyproheptadine hydrochloride 98%
Hesperetin 97%
Olopatadine HCl 98%
Mianserin hydrochloride 99+%
Buclizine 2HCl 97%
Latrepirdine 2HCl GluR 98%
Cetirizine 2HCl 98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Levodropropizine 生物活性

靶点
  • Histamine receptor

描述 Levodropropizine, a common antitussive drug, suppresses seizure activity in rats with PTZ-induced (pentylenetetrazol) status epilepticus[3]. Levodropropizine is commonly used as an antitussive drug for acute and chronic cough. It is a non-opioid agent with peripheral antitussive action via the modulation of sensory neuropeptide levels in the airways[4]. Moreover, the antitussive drug has a peripheral site of action by injecting the drug intracerebroventricularly (i.c.v.). In these experiments levodropropizine (40 micrograms/50 microliters i.c.v.) did not prevent electrically-induced cough. And levodropropizine failed to prevent the vagally elicited cough in neuropeptide-depleted animals[5]. Levodropropizine (10, 50 and 200 mg/kg) reduced in a dose-dependent manner the extravasation of Evans blue dye evoked by capsaicin. Levodropropizine inhibited also substance P-evoked extravasation, whereas it did not affect the extravasation evoked by platelet activating factor. Levodropropizine (10 and 100 microM) did not affect the contraction produced by [Sar9,Met(O2)11]substance P, a selective agonist for tachykinin NK1 receptors, in the rat urinary bladder in vitro[6].

Levodropropizine 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01416480 Acute Bronchitis Phase 3 Completed - Korea, Republic of ... 展开 >> Hallym University Medical Center Anyang, Gyeonggi-do, Korea, Republic of, 431-070 收起 <<
NCT01177852 Inflammation ... 展开 >>Cough Rhinitis 收起 << Phase 3 Withdrawn - -
NCT03489837 Evaluate the Efficacy and Safe... 展开 >>ty of Levotuss CR Tab. in Comparison With Levotuss Syrup in Patients With Cough Due to Acute or Chronic Bronchitis 收起 << Phase 3 Completed - Korea, Republic of ... 展开 >> Included Seoul national hospital,10sites Seoul, Korea, Republic of 收起 <<

Levodropropizine 参考文献

[1]Zanasi A, Lanata L, et al. Levodropropizine for treating cough in adult and children: a meta-analysis of published studies. Multidiscip Respir Med. 2015 May 31;10(1):19.

[2]Melillo G, Malandrino S, et al. General pharmacology of the new antitussive levodropropizine. Arzneimittelforschung. 1988 Aug;38(8):1144-50.

[3]Erdogan MA, Yusuf D, Erdogan A, Erbas O. Levodropropizine suppresses seizure activity in rats with pentylenetetrazol-induced epilepsy. Epilepsy Res. 2019 Feb;150:32-37

[4]Song JW, Jang YS, Jung MC, Kim JH, Choi JH, Park S, Hwang YI, Jang SH, Jung KS. Levodropropizine-Induced Anaphylaxis: Case Series and Literature Review. Allergy Asthma Immunol Res. 2017 May;9(3):278-280

[5]Lavezzo A, Melillo G, Clavenna G, Omini C. Peripheral site of action of levodropropizine in experimentally-induced cough: role of sensory neuropeptides. Pulm Pharmacol. 1992 Jun;5(2):143-7

[6]Yamawaki I, Geppetti P, Bertrand C, Huber O, Daffonchio L, Omini C, Nadel JA. Levodropropizine reduces capsaicin- and substance P-induced plasma extravasation in the rat trachea. Eur J Pharmacol. 1993 Oct 12;243(1):1-6

Levodropropizine 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.23mL

0.85mL

0.42mL

21.16mL

4.23mL

2.12mL

42.32mL

8.46mL

4.23mL

Levodropropizine 技术信息

CAS号99291-25-5
分子式C13H20N2O2
分子量 236.31
别名 (S)-(-)-Dropropizine;DF-526;Levotuss;(–)-(S)-Dropropizine
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Room temperature

溶解度

DMSO: 50 mg/mL(211.59 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 10 mg/mL(42.32 mM),配合低频超声助溶

动物实验配方
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