| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 500mg | |||
| 1g | |||
| Other Sizes |
| Targets |
Mesoridazine Besylate targets dopamine receptors, particularly D2 and D4 subtypes. It has high affinity for the cloned rat dopamine D4 receptor (Ki 20 nM). By blocking dopamine receptors in the brain, it helps manage symptoms such as hallucinations, delusions, and agitation. It is a dopaminergic antagonist and belongs to the phenothiazine class of antipsychotics.
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| ln Vitro |
Mesoridazine inhibits human ether-a-go-go related gene (HERG) currents in a concentration-dependent manner (IC50 = 550 nM, 0 mV). The blocking action increases dramatically along the voltage range where HERG activation occurs, leading to maximal Saturable channel activity when HERG voltage is reached [1]. The total absorption rates of 15.94 ± 4.04% and 39.24 ± 5.11% of mesoridazine (15 mM; 24 hours) in nude mouse and pig skin, respectively, were reported [3].
In vitro, mesoridazine besylate is a potent phenothiazine dopamine receptor antagonist that inhibits D2DR and D4DR. It has high affinity for the dopamine D4 receptor. Mesoridazine (15 mM) shows strong action and persistent analgesia in preventing cutaneous discomfort. |
| ln Vivo |
Mesoridazine (15 mM) shows strong action and persistent analgesia in preventing cutaneous discomfort when applied topically once or once a day for seven days [3]. Mice in the nude were given a topical application of mesoridazine (15 mM) for six hours. The intradermal concentration of the drug was 0.34 - 0.74 nmol/mg [3].
In vivo, mesoridazine besylate is an orally active phenothiazine antipsychotic agent. It is a metabolite of thioridazine and is used as an antipsychotic medication. It acts by blocking dopamine receptors in the brain, helping to manage symptoms of psychosis. It is considered a second-line treatment due to its potential side effects. |
| Enzyme Assay |
In vitro enzyme/receptor binding studies for mesoridazine besylate typically involve radioligand binding assays using membrane preparations from cells expressing dopamine D2 and D4 receptors. Competitive binding experiments with labeled ligands such as [3H]-spiperone are performed to determine Ki values. Standard protocols involve incubating membranes with increasing concentrations of mesoridazine in the presence of a fixed concentration of radioligand.
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| Cell Assay |
In vitro cellular assays for mesoridazine besylate involve culturing cells expressing dopamine receptors in the presence of serial dilutions of the compound. Receptor-mediated signaling, such as cAMP accumulation or calcium mobilization, is measured. Cell viability is assessed using standard assays. Its effects on dopamine receptor signaling are characterized by its antagonist activity.
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| Animal Protocol |
Animal/Disease Models: 8weeks old female nude mice [3]
Doses: 15 mM Route of Administration: Topical administration, once (analgesic test) or one time/day for 7 days (stimulation test) Experimental Results:Shows analgesic effect. A slight increase in transepidermal water loss (TEWL) from 7.8 to 9.9 g/m2/h was observed. In vivo animal studies for mesoridazine besylate include models of psychosis, such as amphetamine-induced hyperactivity or conditioned avoidance response in rodents. Animals are treated with mesoridazine via oral or intraperitoneal administration. Endpoints include inhibition of hyperlocomotion or avoidance behavior. Standard protocols include dose-response assessment and comparison to reference antipsychotics. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of mesoridazine besylate include a molecular weight of 544.75 and a molecular formula of C₂₁H₂₆N₂OS₂·C₆H₆O₃S. It is the benzenesulfonate salt of mesoridazine. It is orally active. It is a metabolite of thioridazine. Detailed pharmacokinetic parameters such as half-life and bioavailability are available from clinical studies.
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| Toxicity/Toxicokinetics |
Toxicological data for mesoridazine besylate are similar to other phenothiazine antipsychotics. Common side effects include sedation, extrapyramidal symptoms, weight gain, and anticholinergic effects. It may cause QT prolongation and should be used with caution in patients with cardiac conditions. It is contraindicated in patients with severe cardiovascular disease, coma, or known hypersensitivity to phenothiazines.
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| References |
[1]. Zhi Su, et al. Mesoridazine: an open-channel blocker of human ether-a-go-go-related gene K+ channel. J Mol Cell Cardiol. 2004 Jan;36(1):151-60.
[2]. I S M Salih, et al. Comparison of the effects of thioridazine and mesoridazine on the QT interval in healthy adults after single oral doses. Clin Pharmacol Ther. 2007 Nov;82(5):548-54. [3]. Liu KS, et al. Topically applied mesoridazine exhibits the strongest cutaneous analgesia and minimized skin disruption among tricyclic antidepressants: The skin absorption assessment. Eur J Pharm Biopharm. 2016 Aug;105:59-68. |
| Additional Infomation |
Mesoridazine besylate is the benzylsulfonate salt of methoritizine, prepared from equimolar amounts of methoritizine and benzylsulfonic acid. It is a dopaminergic antagonist and belongs to the first generation of antipsychotic drugs. Its main component is methoritizine.
Mesoridazine Besylate is a phenothiazine antipsychotic agent and a metabolite of thioridazine. It is a potent dopamine receptor antagonist with high affinity for D2 and D4 receptors. It is used to manage symptoms of psychosis. It is considered a second-line treatment due to its potential side effects. It is not approved for human therapeutic use in many jurisdictions. |
| Molecular Formula |
C27H32N2O4S3
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|---|---|
| Molecular Weight |
544.74898
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| Exact Mass |
544.152
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| CAS # |
32672-69-8
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| Related CAS # |
Mesoridazine;5588-33-0
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| PubChem CID |
36207
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| Appearance |
Typically exists as solid at room temperature
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| Boiling Point |
570.5ºC at 760mmHg
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| Flash Point |
298.9ºC
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| LogP |
7.783
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
36
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| Complexity |
686
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=S(C(C=C1N2CCC3N(C)CCCC3)=CC=C1SC4=C2C=CC=C4)C.O=S(C5=CC=CC=C5)(O)=O
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| InChi Key |
CRJHBCPQHRVYBS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H26N2OS2.C6H6O3S/c1-22-13-6-5-7-16(22)12-14-23-18-8-3-4-9-20(18)25-21-11-10-17(26(2)24)15-19(21)237-10(8,9)6-4-2-1-3-5-6/h3-4,8-11,15-16H,5-7,12-14H2,1-2H31-5H,(H,7,8,9)
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| Chemical Name |
10-(2-(1-methylpiperidin-2-yl)ethyl)-2-(methylsulfinyl)-10H-phenothiazine benzenesulfonate
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| Synonyms |
Mesoridazine benzenesulfonate NC
123 CHEBI
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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) |
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
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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 | 1.8357 mL | 9.1785 mL | 18.3570 mL | |
| 5 mM | 0.3671 mL | 1.8357 mL | 3.6714 mL | |
| 10 mM | 0.1836 mL | 0.9179 mL | 1.8357 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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