| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Targets |
Mequitazine targets the histamine H1 receptor, acting as a potent antagonist. It selectively blocks H1 receptors. It competes with histamine for H1-receptor sites on effector cells in the gastrointestinal tract, blood vessels, and respiratory tract. It may also inhibit Ca²⁺ release from intracellular Ca stores of mast cells and stabilize the lipid bilayer of the cell membrane. It also exhibits bactericidal effects against clinical isolates including Ps. aeruginosa.
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| ln Vitro |
Strong H1 receptor-selective antihistamine mequitazine has been extensively researched and used to treat allergy conditions like urticaria and hay fever [1]. Mequitazidine exhibited notable bactericidal properties against every clinical isolate that was examined, including Ps. Aeruginosa pseudomonas. Its impact on strains that are Gram-positive is more noticeable [2].
In vitro, mequitazine is a potent H1-receptor selective antihistaminic drug. It demonstrates significant bactericidal effects against all tested clinical isolates including Pseudomonas aeruginosa. It may act to inhibit Ca²⁺ release from intracellular Ca stores of mast cells and stabilize the lipid bilayer of the cell membrane. |
| ln Vivo |
In the ileum of guinea pigs, mequitazine and clemizole competitively counteract the effects of histamine. In the rat duodenum, mequitazine of 107 caused a parallel change in the acetylcholine dose-response curve. The greatest doses of mequitazine have anticholinergic action [3]. Mequitazine prevents the rat aorta from contracting in response to KCl, 5-hydroxytryptamine (5-HT), phenylephrine (PE), and Ca2+ [4].
In vivo, mequitazine is a potent, nonsedative, and long-acting histamine H1 antagonist. It is used for allergic disorders such as hay fever and urticaria. It has been extensively researched and used to treat allergy conditions. Its nonsedative profile makes it preferable for daytime use compared to first-generation antihistamines. |
| Enzyme Assay |
In vitro enzyme/receptor binding studies for mequitazine typically involve radioligand binding assays using membrane preparations from cells expressing histamine H1 receptors. Competitive binding experiments with labeled ligands such as [3H]-mepyramine are performed to determine affinity (Ki). Standard protocols involve incubating membranes with increasing concentrations of mequitazine in the presence of a fixed concentration of radioligand.
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| Cell Assay |
In vitro cellular assays for mequitazine involve culturing cells expressing H1 receptors in the presence of serial dilutions of the compound. Histamine-induced calcium mobilization or other signaling readouts are measured. Its antibacterial activity is assessed by standard broth microdilution or agar diffusion methods against bacterial strains such as Pseudomonas aeruginosa.
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| Animal Protocol |
In vivo animal studies for mequitazine include models of allergy, such as histamine-induced bronchoconstriction or skin reactions in rodents. Animals are treated with mequitazine via oral administration. Endpoints include inhibition of histamine-induced responses. Its long-acting profile is assessed by measuring the duration of antihistaminic effect.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of mequitazine include a molecular weight of 322.47 and a molecular formula of C₂₀H₂₂N₂S. It has an ALogP of 4.6. It is a potent, long-acting antihistamine. It is nonsedative, indicating limited blood-brain barrier penetration. It is metabolized in the liver and has a long half-life, supporting once-daily dosing.
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| Toxicity/Toxicokinetics |
Toxicological data for mequitazine indicate that it is generally well-tolerated at therapeutic doses. Common side effects may include dry mouth, mild drowsiness in some individuals, and gastrointestinal upset. It is contraindicated in patients with known hypersensitivity to antihistamines. Overdose may cause severe anticholinergic effects, including seizures and cardiac arrhythmias.
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| References |
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| Additional Infomation |
Mequintazine belongs to the phenothiazine class of drugs. Mequintazine is a histamine H1 receptor antagonist (antihistamine). It competes with histamine for normal H1 receptor sites on effector cells in the gastrointestinal tract, blood vessels, and respiratory tract. It effectively and temporarily relieves symptoms such as sneezing, tearing, itchy eyes, and runny nose caused by hay fever and other upper respiratory tract allergies. Indications: Used to treat hay fever, urticaria, and allergic rhinitis. Mechanism of Action: Mequintazine binds to histamine H1 receptor sites on effector cells in the gastrointestinal tract, blood vessels, and respiratory tract. This blocks the action of endogenous histamine, thereby temporarily relieving histamine-induced adverse symptoms.
Mequitazine is a potent, nonsedative, and long-acting histamine H1 antagonist. It is used for allergic disorders such as hay fever and urticaria. It is also known as LM-209. It exhibits significant bactericidal effects against Pseudomonas aeruginosa. It is not approved for human therapeutic use in many jurisdictions. |
| Molecular Formula |
C20H22N2S
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|---|---|
| Molecular Weight |
322.47
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| Exact Mass |
322.15
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| CAS # |
29216-28-2
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| Related CAS # |
84992-84-7 (hydrochloride)
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| PubChem CID |
4066
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
469.4±24.0 °C at 760 mmHg
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| Melting Point |
143-145ºC
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| Flash Point |
237.7±22.9 °C
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| Vapour Pressure |
0.0±1.2 mmHg at 25°C
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| Index of Refraction |
1.707
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| LogP |
5.38
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
23
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| Complexity |
398
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
HOKDBMAJZXIPGC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H22N2S/c1-3-7-19-17(5-1)22(18-6-2-4-8-20(18)23-19)14-16-13-21-11-9-15(16)10-12-21/h1-8,15-16H,9-14H2
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| Chemical Name |
10-(1-azabicyclo[2.2.2]octan-3-ylmethyl)phenothiazine
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| Synonyms |
Mircol; Primalan; Mequitazine
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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 : ~16 mg/mL (~49.62 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 | 3.1011 mL | 15.5053 mL | 31.0106 mL | |
| 5 mM | 0.6202 mL | 3.1011 mL | 6.2021 mL | |
| 10 mM | 0.3101 mL | 1.5505 mL | 3.1011 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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