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| Other Sizes |
| Targets |
Risocaine targets voltage-gated sodium channels in neuronal membranes. By blocking these channels, it inhibits the influx of sodium ions, preventing the generation and propagation of action potentials in nerve fibers. This blockade of nerve impulses temporarily inhibits the sensation of pain in the localized area where it is applied. Its mechanism is characteristic of ester-type local anesthetics.
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| ln Vitro |
In vitro, risocaine acts as a local anesthetic by blocking voltage-gated sodium channels. Its activity is confirmed in electrophysiological assays measuring sodium channel currents in neuronal cells. Its anesthetic potency and duration of action are evaluated in isolated nerve preparations. It is a white crystalline solid with a melting point of 72–75°C.
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| ln Vivo |
In vivo, risocaine is used for its numbing properties in minor surgical procedures, dental work, and other medical interventions to provide local anesthesia. It temporarily inhibits pain sensation in the area of application. Its localized action provides pain relief without systemic effects. It is an ester-type local anesthetic.
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| Enzyme Assay |
Cell-free assays for risocaine are not standard because it is a local anesthetic. Its ability to block sodium channels can be studied using patch-clamp techniques on isolated membranes or cells expressing sodium channels. Its physicochemical properties, such as solubility and melting point, are determined by standard methods. Its purity is confirmed by HPLC.
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| Cell Assay |
Cellular assays for risocaine are performed using neuronal cell lines expressing voltage-gated sodium channels. Cells are treated with varying concentrations of risocaine, and sodium currents are measured using patch-clamp electrophysiology. Its ability to inhibit action potential generation is assessed. Cell viability is evaluated using MTT assays.
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| Animal Protocol |
In vivo animal experiments for risocaine are conducted in animal models of local anesthesia. The compound is applied topically or injected locally, and the duration and intensity of anesthesia are measured by response to painful stimuli. Its pharmacokinetics and systemic absorption are also studied. These studies confirm its local anesthetic efficacy.
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| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
This study investigated the brain uptake of local anesthetics in rats following steady-state plasma concentrations and/or intravenous bolus administration. All tested ester anesthetics, such as ethyl para-aminobenzoic acid (PABA) esters (Et), propylparaben (Pr), butylparaben (Bu), and procaine, were rapidly cleared from plasma in a dose-dependent manner. The plasma concentration profiles of these compounds were well explained by a two-compartment model with a Michaelis elimination process that begins in the central compartment. …The extent of brain uptake (brain-plasma partition coefficient, Kp value) of these drugs was determined at three different steady-state plasma concentrations (1–15 μM). The Kp values for each drug were similar at the three different steady-state plasma concentrations. The Kp values increased in the following order: procaine (1.1) < PABA-Et (1.9), < lidocaine (2.2), < PABA-Pr (2.7), < PABA-Bu (3.6). In the n-heptane/water or n-octanol/water partition systems, there is a linear relationship between the Kp value and the logarithm of the partition coefficient. Metabolism/Metabolites Orally or subcutaneously administered PABA esters are rapidly hydrolyzed in mammals to alcohols and free acids. /PABA esters/ Risocaine has a molecular weight of 179.22 g/mol and a molecular formula of C10H13NO2. It is a white crystalline solid. It has a melting point of 72–75°C and water solubility of 842 mg/L at 37°C. It is soluble in DMSO. It has a purity of ≥95%. It should be stored under recommended conditions. |
| Toxicity/Toxicokinetics |
Interactions
A 28-year-old white male underwent endotracheal intubation for respiratory distress, during which he received a citacaine (benzocaine, buprofen, and tetracaine) inhaler and benzocaine ointment. Ninety minutes later, despite ventilation, the patient developed cyanosis with methemoglobin levels at 29% of total hemoglobin. /buprofen/ Non-human toxicity values The intraperitoneal LD50 in mice was 126 mg/kg. The toxicological profile of risocaine is consistent with ester-type local anesthetics. It is generally safe for topical use but may cause allergic reactions in some individuals. Systemic toxicity can occur with high doses, including CNS and cardiovascular effects. It should be used with caution. Its safety has been established through clinical use. |
| Additional Infomation |
Therapeutic Uses
Propyl para-aminobenzoate is used as a local anesthetic and antipruritic. Risocaine is a local anesthetic agent belonging to the ester-type class. It is also known as propyl 4-aminobenzoate, Risocaina, Raythesin, and Propylcain. It acts by blocking voltage-gated sodium channels. It is used for localized pain relief in medical settings. It is a research compound and is not widely used as a modern local anesthetic. |
| Molecular Formula |
C10H13NO2
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|---|---|
| Molecular Weight |
179.22
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| Exact Mass |
179.095
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| CAS # |
94-12-2
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| PubChem CID |
7174
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| Appearance |
Prisms
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| Density |
1.102g/cm3
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| Boiling Point |
323.3ºC at 760 mmHg
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| Melting Point |
75-80 °C
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| Flash Point |
174.3ºC
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| Index of Refraction |
1.546
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| LogP |
2.416
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
13
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| Complexity |
162
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C1C=CC(N)=CC=1)OCCC
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| InChi Key |
NBFQYHKHPBMJJV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H13NO2/c1-2-7-13-10(12)8-3-5-9(11)6-4-8/h3-6H,2,7,11H2,1H3
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| Chemical Name |
propyl 4-aminobenzoate
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| Synonyms |
Raythesin; Propylcain; Risocaine
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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 (~557.97 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (13.95 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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 (13.95 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.5797 mL | 27.8987 mL | 55.7973 mL | |
| 5 mM | 1.1159 mL | 5.5797 mL | 11.1595 mL | |
| 10 mM | 0.5580 mL | 2.7899 mL | 5.5797 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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