| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
5-HT2A Receptor ( Ki = 1.5 nM ); 5-HT2C Receptor ( Ki = 12 nM ); 5-HT3 Receptor ( Ki = 75 nM )
Cyamemazine targets multiple receptors. It acts as a D2 dopamine receptor antagonist. It also strongly antagonizes 5-HT3 and 5-HT2C serotonin receptors. Additionally, it acts as an α1-adrenergic, H1, and mACh antagonist. Its antipsychotic action is consistent with its high affinity for dopamine receptors. It has Ki values of 12 nM for 5-HT3, 1.5 nM for 5-HT2A, and 75 nM for 5-HT2C receptors. Its affinity for M1 (Ki = 13 nM), M2 (Ki = 42 nM), M3 (Ki = 321 nM), M4 (Ki = 12 nM), and M5 (Ki = 35 nM) receptors is consistent with its antagonist activity at muscarinic receptors. |
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| ln Vitro |
Cyamemazine's antipsychotic action is consistent with its high affinity for dopamine receptors. Cyamemazine's affinity for M1 (Ki = 13 nM), M2 (Ki = 42 nM), M3 (Ki = 321 nM), M4 (Ki = 12 nM), and M5 (Ki = 35 nM) receptors is consistent with its antagonist activity at muscarinic receptors[1].
Cyamemazine is an antagonist at D2 dopamine receptors and 5-HT3, 5-HT2A, and 5-HT2C serotonin receptors. It also acts as an antagonist at α1-adrenergic, H1, and mACh receptors. It has antipsychotic, anxiolytic, and sedative properties. |
| ln Vivo |
Cyamemazine functions as an antagonist at the 5-HT3, 5-HT2C, and 5-HT2A receptors in the rat brain membrane in the 5-HT2C-dependent phospholipase C stimulation, in the 5-HT3-dependent contraction of the isolated guinea pig ileum and bradycardic responses, and in the 5-HT2A-dependent contraction of the isolated rat aorta rings and the isolated guinea pig trachea. The antagonism of 5-HT3 and 5-HT2C receptors by cyamemazine is partly responsible for its therapeutic action against anxiety disorders. Low doses of cyclomazine administered acutely can lower metabolite and extracellular dopamine concentrations in the rat striatum[1].
Cyamemazine is used as an antipsychotic and anxiolytic agent. It has been used to reduce ethanol withdrawal symptoms. It is valuable for research into neuropsychiatric disorders, serotonin-dopamine interactions, and therapeutic strategies in CNS pharmacology. |
| Enzyme Assay |
Cyamemazine is evaluated in cell-free receptor binding assays to determine its affinity for dopamine, serotonin, muscarinic, adrenergic, and histamine receptors. Radioligand binding displacement assays are performed using membrane preparations expressing these receptors. Ki values are determined to quantify the potency of receptor antagonism.
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| Cell Assay |
Cyamemazine is assessed in cell-based assays to measure its antagonist activity at various receptors. Cells expressing dopamine, serotonin, muscarinic, adrenergic, or histamine receptors are treated with Cyamemazine, and receptor activity is measured by assessing downstream signaling pathways.
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| Animal Protocol |
Cyamemazine is administered in animal models to evaluate its antipsychotic, anxiolytic, and sedative effects. It has been studied in models of alcohol and benzodiazepine withdrawal syndrome. Efficacy is assessed using behavioral tests and physiological measurements.
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| ADME/Pharmacokinetics |
Cyamemazine has a molecular weight of 323.46 and a molecular formula of C19H21N3S. It has a CAS number of 3546-03-0. The compound is soluble in DMSO at ≥5 mg/mL. It should be stored as a powder at -20°C.
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| Toxicity/Toxicokinetics |
No detailed toxicity data is available for Cyamemazine beyond its known use as an antipsychotic. The compound is for research use only and is not intended for human therapeutic use. It has been shown to increase phototoxicity and lipid membrane peroxidation in cells and lysosomes.
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| References |
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| Additional Infomation |
Cymetrazine belongs to the phenothiazine class of drugs. Cymetrazine (trade name: Texacin), also known as cyanpromethazine, is a typical phenothiazine antipsychotic, primarily used to treat schizophrenia and psychotic-related anxiety disorders. Due to its potent anti-anxiety effect (5-HT2C receptor) and lack of extrapyramidal side effects (5-HT2A receptor), cyanmetrazine actually behaves like an atypical antipsychotic.
Cyamemazine is a phenothiazine derivative that acts as a D2 dopamine receptor antagonist. It has a CAS number of 3546-03-0. It is a typical antipsychotic drug of the phenothiazine class. It is not approved for clinical use. |
| Molecular Formula |
C19H21N3S
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|---|---|
| Molecular Weight |
323.45
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| Exact Mass |
323.145
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| Elemental Analysis |
C, 70.55; H, 6.54; N, 12.99; S, 9.91
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| CAS # |
3546-03-0
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| Related CAS # |
Cyamemazine-d6; 1216608-24-0
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| PubChem CID |
62865
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| Appearance |
Solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
479.0±45.0 °C at 760 mmHg
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| Melting Point |
204-205
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| Flash Point |
243.5±28.7 °C
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| Vapour Pressure |
0.0±1.2 mmHg at 25°C
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| Index of Refraction |
1.655
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| LogP |
4.62
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
23
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| Complexity |
443
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(CN(C)C)CN1C2=CC=CC=C2SC3=C1C=C(C=C3)C#N
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| InChi Key |
SLFGIOIONGJGRT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H21N3S/c1-14(12-21(2)3)13-22-16-6-4-5-7-18(16)23-19-9-8-15(11-20)10-17(19)22/h4-10,14H,12-13H2,1-3H3
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| Chemical Name |
10-[3-(dimethylamino)-2-methylpropyl]phenothiazine-2-carbonitrile
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| Synonyms |
Cyamepromazine; TercianCianatil; Cyamemazine
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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: ~100 mg/mL (~309.2 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.73 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (7.73 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.73 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0917 mL | 15.4583 mL | 30.9167 mL | |
| 5 mM | 0.6183 mL | 3.0917 mL | 6.1833 mL | |
| 10 mM | 0.3092 mL | 1.5458 mL | 3.0917 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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