| Size | Price | |
|---|---|---|
| Other Sizes |
| Targets |
Histamine H1 receptor (antihistamine activity). Dioxopromethazine also has anti-inflammatory and local anesthetic properties.
|
|---|---|
| ln Vitro |
Dioxopromethazine is an orally bioactive antihistamine with antitussive, expectorant, and local anesthetic properties. It suppresses asthma symptoms and has anti-inflammatory effects and the ability to relieve smooth muscle spasms.
|
| ln Vivo |
In vivo, dioxopromethazine is used for the treatment of cough and expectoration. It suppresses asthma symptoms and has local anesthetic effects. No detailed in vivo activity data are publicly available.
|
| Enzyme Assay |
In vitro receptor binding assays for dioxopromethazine are performed to evaluate its affinity for the H1 receptor. Radioligand binding studies using membrane preparations from cells or tissues expressing the H1 receptor are conducted. The compound's ability to displace a specific radiolabeled H1 ligand is measured to calculate its binding affinity.
|
| Cell Assay |
In vitro cell-based assays are conducted using cells expressing the H1 receptor. The cells are treated with dioxopromethazine, and receptor antagonism is measured by assessing its ability to block histamine-induced downstream signaling events.
|
| Animal Protocol |
In vivo animal studies are conducted in rodent models to evaluate the effects of dioxopromethazine on cough, asthma, and inflammation. The compound is typically administered orally, and its effects on cough reflex, airway resistance, and inflammatory markers are assessed.
|
| ADME/Pharmacokinetics |
No detailed pharmacokinetic data are publicly available for dioxopromethazine. As an orally bioactive compound, its ADME properties would be characterized in standard preclinical studies.
|
| Toxicity/Toxicokinetics |
No specific toxicity data are publicly available for dioxopromethazine. Studies have indicated that it has no toxicity to the liver, kidneys, or other organs. Teratogenicity studies have shown no harm to the fetus.
|
| References |
[1]. Bartsch R, et al. Zur Pharmakologie des neuen Antihistaminicums 9.9-Dioxopromethazin (Prothanon) [Pharmacology of the new antihistaminic 9,9-dioxopromethazine (Prothanon)]. Pharmazie. 1970;25(2):91-96.
|
| Additional Infomation |
See also: Dioxane hydrochloride (note moved to).
Dioxopromethazine (Prothanon) is an orally bioactive antihistamine with antitussive, expectorant, local anesthetic, and anti-inflammatory properties. It is used for the treatment of cough and expectoration and suppresses asthma symptoms. The compound is a research tool and is not widely approved for clinical use. |
| Molecular Formula |
C17H20N2O2S
|
|---|---|
| Molecular Weight |
316.42
|
| Exact Mass |
316.124
|
| CAS # |
13754-56-8
|
| PubChem CID |
63031
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.2±0.1 g/cm3
|
| Boiling Point |
478.5±34.0 °C at 760 mmHg
|
| Melting Point |
127-129ºC
|
| Flash Point |
243.2±25.7 °C
|
| Vapour Pressure |
0.0±1.2 mmHg at 25°C
|
| Index of Refraction |
1.606
|
| LogP |
2.18
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
22
|
| Complexity |
455
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CN(C(CN1C2=CC=CC=C2S(=O)(=O)C2=CC=CC=C12)C)C
|
| InChi Key |
FDXKCOBAFGSMDJ-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C17H20N2O2S/c1-13(18(2)3)12-19-14-8-4-6-10-16(14)22(20,21)17-11-7-5-9-15(17)19/h4-11,13H,12H2,1-3H3
|
| Chemical Name |
1-(5,5-dioxophenothiazin-10-yl)-N,N-dimethylpropan-2-amine
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| 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 | 3.1604 mL | 15.8018 mL | 31.6036 mL | |
| 5 mM | 0.6321 mL | 3.1604 mL | 6.3207 mL | |
| 10 mM | 0.3160 mL | 1.5802 mL | 3.1604 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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