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Levodropropizine

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Chemical Structure| 99291-25-5 同义名 : (S)-(-)-Dropropizine;DF-526;Levotuss;(–)-(S)-Dropropizine
CAS号 : 99291-25-5
货号 : A728009
分子式 : C13H20N2O2
纯度 : 97%
分子量 : 236.31
MDL号 : MFCD00866852
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
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：
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].
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 Phase 3 Withdrawn - -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 <<
实验方案
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
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