货号:A728009
同义名:
(S)-(-)-Dropropizine; DF-526
Levodropropizine 是一种组胺受体抑制剂,作为有效且耐受性良好的外周镇咳化合物,通过调节神经肽和抑制外围感觉神经末端的活化作用来减轻咳嗽。


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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 2HCl | ✔ | 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 | ✔ | 96% | |||||||||||||||||
| Betahistine |
+
Histamine H3 receptor, IC50: 1.9 μM |
99% | |||||||||||||||||
| Ciproxifan maleate |
+++
Histamine H3 receptor, IC50: 9.2 nM |
99%+ | |||||||||||||||||
| S 38093 |
++
rat H3 receptor, Ki: 1.44 μM human H3 receptor, Ki: 1.2 μM |
98% | |||||||||||||||||
| JNJ-7777120 |
++++
Histamine H4 receptor, Ki: 4.5 nM |
99% | |||||||||||||||||
| Azelastine HCl | ✔ | 98% | |||||||||||||||||
| Epinastine HCl | ✔ | 99% | |||||||||||||||||
| Levodropropizine | ✔ | 97% | |||||||||||||||||
| Cyproheptadine HCl | ✔ | 98% | |||||||||||||||||
| Hesperetin | ✔ | 97% | |||||||||||||||||
| Olopatadine HCl | ✔ | 98% | |||||||||||||||||
| Mianserin HCl | ✔ | 99+% | |||||||||||||||||
| Buclizine 2HCl | ✔ | 95% | |||||||||||||||||
| Latrepirdine 2HCl | ✔ | GluR | 99% | ||||||||||||||||
| 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。 | |||||||||||||||||||
| 靶点 |
|
| 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]. |
| 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 << |
| 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 |
|
| CAS号 | 99291-25-5 |
| 分子式 | C13H20N2O2 |
| 分子量 | 236.31 |
| SMILES Code | OC[C@@H](O)CN1CCN(C2=CC=CC=C2)CC1 |
| MDL No. | MFCD00866852 |
| 别名 | (S)-(-)-Dropropizine; DF-526; Levotuss; (–)-(S)-Dropropizine |
| 运输 | 蓝冰 |
| InChI Key | PTVWPYVOOKLBCG-ZDUSSCGKSA-N |
| Pubchem ID | 65859 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry,2-8°C |
| 溶解方案 |
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 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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