| Size | Price | Stock | Qty |
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| 100mg |
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| 500mg |
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| Other Sizes |
| Targets |
The primary target is voltage-gated sodium channels in nerve cell membranes. Dimethocaine functions by binding to and blocking these channels, preventing the propagation of action potentials and thus the transmission of pain signals. It is structurally a derivative of cocaine, acting as a sodium channel blocker.
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| ln Vitro |
In vitro, Dimethocaine shows anesthetic potency by inhibiting sodium currents in neuronal preparations. Studies have also characterized its metabolism using liver microsomes (P450 enzymes and NAT2). It shows weaker potency than cocaine as an anesthetic but also exhibits mild euphoric and stimulant effects.
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| ln Vivo |
In vivo, Dimethocaine produces local anesthesia upon topical or injectable administration. It also has stimulant properties, leading to its use as a recreational drug. In research models, it has been used to study the correlation between structure and anesthetic activity, as well as its impact on the central nervous system.
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| Enzyme Assay |
Non-cellular binding assays are used to study sodium channel interaction. Radio-labeled Batrachotoxin (BTX) or other sodium channel ligands are incubated with rat brain synaptosomes or purified sodium channels. Dimethocaine hydrochloride is added at varying concentrations, and displacement of the radioactive ligand is measured to calculate the IC50 for receptor binding.
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| Cell Assay |
A cell-free enzyme assay is used to study its metabolism. Human or rat liver microsomes (containing CYP450 enzymes) are incubated with Dimethocaine hydrochloride (10-100 uM) and an NADPH-regenerating system. After 30-60 minutes, the reaction is terminated with acetonitrile, and metabolites (e.g., hydroxylated and N-dealkylated products) are analyzed and identified via LC-MS/MS.
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| Animal Protocol |
Anesthetic efficacy is evaluated in the rat tail-flick or hot plate test. Dimethocaine hydrochloride (typically 0.5-2% solution) is injected locally (subcutaneously) into the tail. The latency for the rat to withdraw its tail from a heat source is measured at baseline and at multiple time points post-injection (5-60 minutes). A prolonged latency compared to baseline indicates a local anesthetic effect.
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| ADME/Pharmacokinetics |
Pharmacokinetic data indicates that Dimethocaine is rapidly absorbed following administration. It is primarily metabolized in the liver by cytochrome P450 enzymes (particularly CYP3A4 and CYP2D6) and NAT2, producing inactive metabolites that are excreted renally. The plasma half-life is relatively short (approximately 1-2 hours in animal models), similar to other short-acting anesthetics.
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| Toxicity/Toxicokinetics |
Adverse reactions can occur, including potential for addiction, cardiovascular issues (tachycardia, hypertension), and central nervous system stimulation. As a “new psychoactive substance” (NPS), it is often sold without any safety testing. Overdose can lead to seizures, arrhythmias, and respiratory depression. It is considered a controlled substance in many jurisdictions.
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| References |
[1]. Meyer MR, et al. Dimethocaine, a synthetic cocaine derivative: studies on its in vitro metabolism catalyzed by P450s and NAT2. Toxicol Lett. 2014;225(1):139-146.
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| Additional Infomation |
Clinically, Dimethocaine (Larocaine) was historically used as a local anesthetic, but its use has declined. Currently, it appears in the gray market as a recreational stimulant. The hydrochloride salt is water-soluble. It has an FDA Unique Ingredient Identifier of Z768GH360Q. It is not commonly used in modern medicine due to the availability of safer alternatives like lidocaine.
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| Molecular Formula |
C16H27CLN2O2
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|---|---|
| Molecular Weight |
314.85
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| Exact Mass |
314.176
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| CAS # |
553-63-9
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| Related CAS # |
94-15-5 (Parent)
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| PubChem CID |
120286
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.035g/cm3
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| Boiling Point |
403.5ºC at 760 mmHg
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| Melting Point |
196-197ºC
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| Flash Point |
197.8ºC
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| LogP |
4.176
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
21
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| Complexity |
293
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCN(CC)CC(C)(C)COC(=O)C1=CC=C(C=C1)N.Cl
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| InChi Key |
WWTWKTDXBNHESE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H26N2O2.ClH/c1-5-18(6-2)11-16(3,4)12-20-15(19)13-7-9-14(17)10-8-13;/h7-10H,5-6,11-12,17H2,1-4H3;1H
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| Chemical Name |
[3-(diethylamino)-2,2-dimethylpropyl] 4-aminobenzoate;hydrochloride
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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 and light. |
| 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: 250 mg/mL (794.03 mM)
H2O: 100 mg/mL (317.61 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.61 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 20.8 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: ≥ 2.08 mg/mL (6.61 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 20.8 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: ≥ 2.08 mg/mL (6.61 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 | 3.1761 mL | 15.8806 mL | 31.7612 mL | |
| 5 mM | 0.6352 mL | 3.1761 mL | 6.3522 mL | |
| 10 mM | 0.3176 mL | 1.5881 mL | 3.1761 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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