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| Other Sizes |
| Targets |
Dropropizine acts on peripheral receptors and their afferent conductors in the respiratory tract. It is a peripheral antitussive that inhibits the cough reflex by modulating the activity of C-fibers and other sensory nerves. The compound does not act on the central nervous system, distinguishing it from opioids and other centrally acting antitussives. Its exact molecular target is not fully defined but is believed to involve specific receptors on peripheral sensory nerves.
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| ln Vitro |
In vitro, dropropizine has been shown to modulate the activity of sensory C-fibers. In cell-based assays using isolated nerve preparations or cultured sensory neurons, the compound reduces the firing rate of these neurons in response to irritant stimuli. This demonstrates its peripheral mechanism of action.
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| ln Vivo |
In vivo, dropropizine is effective in suppressing cough in animal models. In guinea pig models of cough induced by irritants such as citric acid or capsaicin, oral or inhaled administration of the compound significantly reduces the number of coughs. These effects are consistent with its peripheral mechanism of action.
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| Enzyme Assay |
In vitro enzyme or receptor binding (non-cell) assays for dropropizine are less common due to its peripheral mechanism of action, which may not involve a single well-defined receptor. However, binding studies can be performed using membrane preparations from lung tissue or sensory neurons to identify potential binding sites. These studies would involve incubating the membrane preparation with a radiolabeled ligand and measuring displacement by dropropizine.
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| Cell Assay |
In vitro cell-based assays for dropropizine are performed using primary cultures of sensory neurons or cell lines that express relevant receptors. Cells are treated with the compound, and neuronal activity is measured by monitoring calcium influx or electrical activity using patch-clamp techniques. The compound's ability to inhibit the response to capsaicin or other irritants is assessed.
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| Animal Protocol |
In vivo animal experiments for dropropizine are conducted using guinea pig or mouse models of cough. Cough is induced by exposing the animals to an irritant aerosol, such as citric acid or capsaicin. The compound is administered orally or by inhalation, and the number of coughs is counted over a set period. The reduction in cough frequency is used to assess the compound's antitussive efficacy.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of dropropizine indicate it is orally active. The compound has a molecular weight of 236.31 and a formula of C₁₃H₂₀N₂O₂. It is absorbed after oral administration and reaches systemic circulation. Specific PK parameters, such as half-life and bioavailability, are determined in preclinical studies via LC-MS/MS analysis of plasma samples.
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| Toxicity/Toxicokinetics |
Toxicology (toxicology) data for dropropizine indicate it is generally well-tolerated. As a non-opioid, peripheral antitussive, it has a low potential for central nervous system side effects such as sedation, respiratory depression, and addiction. Common side effects may include mild gastrointestinal disturbances.
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| References | |
| Additional Infomation |
3-(4-phenyl-1-piperazinyl)propane-1,2-diol is a member of the piperazine class of compounds.
Other information: Dropropizine is used as a cough suppressant in many countries. It is available as an over-the-counter medication for the symptomatic treatment of dry cough. The compound is also known by its synonym UCB-196. |
| Molecular Formula |
C13H20N2O2
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|---|---|
| Molecular Weight |
236.3101
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| Exact Mass |
236.152
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| CAS # |
17692-31-8
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| Related CAS # |
Levodropropizine;99291-25-5
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| PubChem CID |
3169
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
412.7±34.0 °C at 760 mmHg
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| Melting Point |
105-108ºC
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| Flash Point |
220.9±24.3 °C
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| Vapour Pressure |
0.0±1.0 mmHg at 25°C
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| Index of Refraction |
1.577
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| LogP |
0.46
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
17
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| Complexity |
212
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
PTVWPYVOOKLBCG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H20N2O2/c16-11-13(17)10-14-6-8-15(9-7-14)12-4-2-1-3-5-12/h1-5,13,16-17H,6-11H2
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| Chemical Name |
3-(4-phenylpiperazin-1-yl)propane-1,2-diol
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 41 mg/mL (~173.50 mM)
H2O : ≥ 33.33 mg/mL (~141.04 mM) |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.2317 mL | 21.1586 mL | 42.3173 mL | |
| 5 mM | 0.8463 mL | 4.2317 mL | 8.4635 mL | |
| 10 mM | 0.4232 mL | 2.1159 mL | 4.2317 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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