| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
| Targets |
(±)-Levomepromazine acts by blocking a variety of receptors, including adrenergic, dopamine (D2), histamine (H1), muscarinic acetylcholine, and serotonin (5-HT2) receptors. This broad receptor antagonism underlies its diverse pharmacological effects, including antipsychotic, sedative, analgesic, and antiemetic actions. It is a low-potency antipsychotic, meaning that higher doses are typically required compared to high-potency agents, but it has a lower propensity for extrapyramidal side effects.
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| ln Vitro |
In vitro, (±)-Levomepromazine is characterized by its receptor binding profile, antagonizing dopaminergic, serotonergic, adrenergic, histaminergic, and muscarinic receptors. While specific IC₅₀ values for receptor binding are not provided in the available sources, its pharmacological activity is well-established through receptor binding assays. Its effects are similar to those of chlorpromazine. The compound is available as a racemic mixture.
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| ln Vivo |
In vivo, (±)-Levomepromazine is used clinically as an antipsychotic and for palliative care. It is administered orally and has potent sedative, analgesic, and antiemetic effects. Its use in palliative care is particularly notable for managing pain, nausea, and agitation in terminally ill patients. It has been in clinical use for many years, and its in vivo efficacy and safety profile are well established.
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| Enzyme Assay |
A cell-free assay for (±)-Levomepromazine would typically involve receptor binding assays to measure its affinity for various receptors, including dopaminergic, serotonergic, adrenergic, histaminergic, and muscarinic receptors. In these assays, membrane preparations containing the receptors are incubated with radiolabeled ligands and varying concentrations of the compound. The concentration required to displace 50% of the specific binding (IC₅₀) can be determined. However, specific IC₅₀ values are not provided in the available sources.
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| Cell Assay |
Cellular assays for (±)-Levomepromazine are not specifically described in the available sources. As a receptor antagonist, its effects can be evaluated in cell lines expressing the relevant receptors by measuring downstream signaling pathways. For example, its antagonism of dopamine D2 receptors can be assessed by measuring inhibition of cAMP accumulation or other second messenger responses. However, specific protocols are not detailed.
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| Animal Protocol |
In vivo animal experiments for (±)-Levomepromazine are not described in the available sources. As a clinically used drug, its efficacy and safety have been established in human studies. Preclinical studies in animal models likely contributed to its development, but specific protocols and data are not provided in the references cited.
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| ADME/Pharmacokinetics |
(±)-Levomepromazine is an orally administered drug. Its pharmacokinetic properties are consistent with those of other phenothiazine antipsychotics. It is well absorbed after oral administration and undergoes extensive metabolism in the liver. Its half-life and other PK parameters are not provided in the available sources. The compound is available in immediate-release formulations for oral use.
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| Toxicity/Toxicokinetics |
Toxicity data for (±)-Levomepromazine are not detailed in the available sources. As a clinically used drug, its safety profile is well established. Common adverse effects include sedation, hypotension, anticholinergic effects (dry mouth, constipation), and extrapyramidal symptoms (though less common than with high-potency antipsychotics). Specific toxicological information, such as LD₅₀ values, is not provided.
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| References | |
| Additional Infomation |
A phenothiazine drug with pharmacological activity similar to chlorpromazine and promethazine. It possesses the histamine antagonistic properties of antihistamines while also producing effects on the central nervous system similar to chlorpromazine. (From Martindale Pharmacopoeia, 30th edition, p. 604)
See also: Levopromethazine (note moved to). (±)-Levomepromazine (CAS: 851-68-3) is the racemate of Levomepromazine, a low-potency phenothiazine antipsychotic also known as Methotrimeprazine. It is used clinically for its antipsychotic, sedative, analgesic, and antiemetic properties, particularly in palliative care. The compound acts by blocking multiple CNS receptors, including adrenergic, dopamine, histamine, muscarinic acetylcholine, and serotonin receptors. It is also known by the brand name Tisercin. It is a first-generation typical antipsychotic. |
| Molecular Formula |
C19H24N2OS
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|---|---|
| Molecular Weight |
328.47166
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| Exact Mass |
328.161
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| CAS # |
851-68-3
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| Related CAS # |
(±)-Levomepromazine-d6;1189805-51-3;(Rac)-Levomepromazine-d3 hydrochloride;1216745-60-6;(±)-Levomepromazine-d3;1185071-29-7
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| PubChem CID |
3916
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.125g/cm3
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| Boiling Point |
468ºC at 760mmHg
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| Flash Point |
236.8ºC
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| Index of Refraction |
1.594
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| LogP |
4.56
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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 |
5
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| Heavy Atom Count |
23
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| Complexity |
378
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1C=CC2=C(N(C3=CC=CC=C3S2)CC(CN(C)C)C)C=1
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| InChi Key |
VRQVVMDWGGWHTJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H24N2OS/c1-14(12-20(2)3)13-21-16-7-5-6-8-18(16)23-19-10-9-15(22-4)11-17(19)21/h5-11,14H,12-13H2,1-4H3
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| Chemical Name |
3-(2-methoxyphenothiazin-10-yl)-N,N,2-trimethylpropan-1-amine
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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 : ~50 mg/mL (~152.22 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 | 3.0444 mL | 15.2221 mL | 30.4442 mL | |
| 5 mM | 0.6089 mL | 3.0444 mL | 6.0888 mL | |
| 10 mM | 0.3044 mL | 1.5222 mL | 3.0444 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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