| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg | |||
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| Other Sizes |
| Targets |
Chlophedianol acts primarily as a centrally acting antitussive agent targeting the cough center in the medulla oblongata. It also blocks histamine receptors (antihistamine activity) and has mild local anesthetic properties that help suppress cough reflexes. At high doses, it may have anticholinergic effects via muscarinic receptor antagonism.
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| ln Vitro |
In vitro, Chlophedianol demonstrates antihistamine activity by competitively blocking histamine H1 receptors, reducing allergic reactions such as sneezing, itching, and runny nose. It also exhibits local anesthetic properties in neuronal preparations. The compound may show anticholinergic activity at high concentrations, as evidenced by muscarinic receptor binding assays. Detailed in vitro activity data including specific IC50 or EC50 values are limited in the published literature.
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| ln Vivo |
In both cats and rabbits, choledanol (Clofedanol) hydrochloride (0–162 mg/kg; oral or subcutaneous injection; once) decreases respiratory fluid production [1].
In vivo, Chlophedianol hydrochloride is effective as an antitussive agent in animal models of cough. It suppresses cough reflexes through central action on the cough center. The compound has been used clinically for the management of acute cough due to upper respiratory tract infections (URIs). Its antitussive efficacy has been demonstrated in various preclinical models, though specific in vivo data regarding cough suppression potency are limited in publicly available sources. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for Chlophedianol typically involve histamine H1 receptor binding assays using radiolabeled ligands such as [³H]mepyramine. Membranes prepared from cells expressing human H1 receptors are incubated with varying concentrations of the test compound. Specific binding is determined by subtracting non-specific binding (defined by excess unlabeled antihistamine). IC50 or Ki values are calculated from competition binding curves. Muscarinic receptor binding assays may also be performed to assess anticholinergic potential at high concentrations.
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| Cell Assay |
Cellular assays for Chlophedianol typically involve functional assays measuring histamine-induced calcium mobilization in cells expressing H1 receptors. Cells are pre-incubated with the compound at various concentrations, then stimulated with histamine, and intracellular calcium levels are measured using fluorescent indicators. The degree of inhibition of histamine response is used to calculate IC50 values. Cytotoxicity and cell viability assays may also be performed to assess safety margins.
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| Animal Protocol |
Animal/Disease Models: Healthy, adult, male rabbits and cats [1]
Doses: 2.0, 6.0, 18, 54 and 162 mg/kg (PO) or 1.0, 3.0, 9.0, 27 and 81 mg/kg (SC) Route of Administration: Administered orally or subcutaneously (sc) (sc), once. Experimental Results: A slight but significant decrease in respiratory fluid output for one to three hrs (hrs (hours)) after administration. Fewer animals develop mucus cotton in their respiratory tracts. In vivo animal studies for antitussive efficacy typically use guinea pig or mouse models of cough induced by aerosolized citric acid or capsaicin. Animals are administered Chlophedianol orally or intraperitoneally at various doses prior to cough challenge. The number of coughs is recorded over a defined observation period, and the percentage inhibition of cough reflex is calculated. Standard antitussive agents such as codeine or dextromethorphan are used as positive controls. |
| ADME/Pharmacokinetics |
Metabolism / Metabolites
Liver. Liver. Chlophedianol hydrochloride is orally active with good absorption following oral administration. As a small-molecule antitussive, it distributes to the central nervous system to exert its centrally acting cough suppressant effects. The compound is metabolized in the liver, and its metabolites are excreted primarily via the kidneys. Detailed PK parameters (half-life, bioavailability, protein binding) are not extensively published but are consistent with those of centrally acting antitussive agents. |
| Toxicity/Toxicokinetics |
Toxicity Summary
It inhibits the cough reflex by acting directly on the cough center in the medulla oblongata of the brain. Toxicity studies of Chlophedianol hydrochloride indicate that it has a reasonable safety margin at therapeutic doses. At high doses, anticholinergic side effects may occur, including dry mouth, blurred vision, and urinary retention. The compound is generally well-tolerated when used at recommended doses for short-term management of dry cough. Overdose may lead to central nervous system depression or excitation, depending on the dose. |
| References | |
| Additional Infomation |
Chlorpheniramine is a diarylmethane compound with the structure 2-chlorophenyl(phenyl)methane, where the carbon atoms of the methane are substituted with 2-(dimethylamino)ethyl. It is used to treat dry cough by inhibiting the cough reflex through direct action on the cough center in the medulla oblongata. It is a diarylmethane and tertiary amine compound and is the conjugate base of chlorpheniramine (1+). Chlorpheniramine is a centrally acting antitussive, marketed in Canada under the brand name Ulone. It is not marketed in the United States. Chlorpheniramine is only present in individuals who have used or taken this medication. Chlorpheniramine inhibits the cough reflex through direct action on the cough center in the medulla oblongata. Drug Indications: For the treatment of dry cough. Mechanism of Action: Inhibits the cough reflex through direct action on the cough center in the medulla oblongata.
Pharmacodynamics Chlorpheniramine (or chlorfenapyridine) is a centrally acting antitussive. It has local anesthetic and antihistamine effects, and at high doses may have anticholinergic effects. Chlophedianol hydrochloride is a centrally acting antitussive agent used clinically for the treatment of dry, non-productive cough, particularly associated with upper respiratory tract infections. It combines antitussive, antihistamine, and local anesthetic properties in a single molecule. The compound is available in various formulations including syrups and tablets. Its mechanism involves suppression of the cough reflex at the medullary cough center, with additional peripheral effects through histamine receptor blockade and local anesthesia. |
| Molecular Formula |
C17H20CLNO.HCL
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| Molecular Weight |
326.26
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| Exact Mass |
325.1
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| CAS # |
511-13-7
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| Related CAS # |
Chlophedianol;791-35-5
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| PubChem CID |
2795
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| Appearance |
White to off-white solid powder
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| Boiling Point |
429.8ºC at 760mmHg
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| Flash Point |
213.7ºC
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| LogP |
4.329
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
20
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| Complexity |
291
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
WRCHFMBCVFFYEQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H20ClNO/c1-19(2)13-12-17(20,14-8-4-3-5-9-14)15-10-6-7-11-16(15)18/h3-11,20H,12-13H2,1-2H3
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| Chemical Name |
1-(2-chlorophenyl)-3-(dimethylamino)-1-phenylpropan-1-ol
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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 : ~125 mg/mL (~383.13 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 | 3.0650 mL | 15.3252 mL | 30.6504 mL | |
| 5 mM | 0.6130 mL | 3.0650 mL | 6.1301 mL | |
| 10 mM | 0.3065 mL | 1.5325 mL | 3.0650 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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