Propoxycaine hydrochloride targets voltage-gated sodium channels. As a local anesthetic of the ester type, it binds to and inhibits voltage-gated sodium channels, preventing the initiation and propagation of nerve impulses. This modulates nerve impulses and induces sensory loss. The compound is a para-aminobenzoic acid ester. Its mechanism of action is characteristic of ester-type local anesthetics.

In vitro, Propoxycaine hydrochloride inhibits voltage-gated sodium channels, modulates nerve impulses, and induces sensory loss. It modulates the flow of lipid bilayers in SPMVs. The compound is an ester local anesthetic. Its sodium channel inhibition has been characterized in various electrophysiological assays. Propoxycaine hydrochloride has a rapid onset and longer duration of action than procaine.

In vivo, Propoxycaine hydrochloride is a local anesthetic used to control the pain of intramuscular injections of penicillin as well as in dentistry. It was used beginning in the 1950s during dental procedures. The compound has been combined with procaine to accelerate its onset of action and provide longer-lasting anesthetic effect. This drug was removed from the US market in 1996.

In vitro sodium channel assays for Propoxycaine hydrochloride involve measuring inhibition of voltage-gated sodium channels. Sodium channel activity is assessed using patch-clamp electrophysiology in cells expressing sodium channels. The compound is added at varying concentrations, and IC50 values are calculated from dose-response curves. For lipid bilayer studies, the compound's effect on membrane fluidity is assessed using fluorescence anisotropy or other methods. Assays are performed in appropriate buffer systems with positive controls such as known local anesthetics (e.g., lidocaine).

Propoxycaine hydrochloride cell-based assays are conducted in neuronal cell lines or primary neurons. Cells are cultured in appropriate media at 37°C with 5% CO2 and treated with the compound at varying concentrations. Sodium channel activity is assessed by measuring action potential firing using patch-clamp electrophysiology or by measuring sodium influx using fluorescent dyes. Cell viability is assessed by standard assays. Experiments are performed in triplicate with appropriate positive (e.g., lidocaine) and negative (vehicle) controls.

Propoxycaine hydrochloride in vivo studies are conducted in animal models for local anesthetic efficacy evaluation. Animals are treated with the compound via local injection. Anesthetic onset and duration are assessed by measuring sensory or motor block. For dental pain models, animals are subjected to dental procedures and pain response is assessed. Pharmacokinetic parameters are determined from blood samples. Animals are monitored for clinical signs. Studies are conducted in accordance with institutional animal care guidelines.

Absorption, Distribution and Excretion
Kidneys: Primarily through renal hydrolysis. Metabolism/Metabolites: This drug is hydrolyzed by plasma esterases in both plasma and liver.
Propoxycaine hydrochloride (MW 330.85 g/mol, C16H26N2O3·HCl) is an ester local anesthetic. It appears as white, odorless crystals with a melting point of 148-150°C. The compound is very soluble in water, slightly soluble in alcohol and chloroform, and practically insoluble in ether. It discolors upon prolonged exposure to light and air. Pharmacokinetic parameters such as half-life, bioavailability, and tissue distribution have been characterized in clinical studies.

Propoxycaine hydrochloride is generally well-tolerated at therapeutic doses. The compound is a local anesthetic with established safety profiles. No significant adverse effects have been reported in the available literature at research-use concentrations. The compound is intended for research use only. Standard safety precautions should be followed when handling. Comprehensive toxicological evaluation is available from clinical use data.

Prooxycaine is a benzoic acid ester. Prooxycaine is an ester-based local anesthetic with a rapid onset of action and a longer duration of action than procaine hydrochloride. It was withdrawn from the US market in 1996. Although no longer sold in the US, it was used in combination with procaine as an adjunct to dental anesthesia. When used in combination with procaine, it was the only dental local anesthetic available in cartridge form. Prooxycaine is a para-aminobenzoic acid ester with local anesthetic activity. Prooxycaine binds to and inhibits the activity of voltage-gated sodium channels, thereby inhibiting the ion flow required for nerve impulse initiation and conduction. This results in loss of sensation. An ester-based local anesthetic with a rapid onset of action and a longer duration of action than procaine hydrochloride. (Excerpt from Martindale Pharmacopoeia, 30th edition, p. 1017)

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Drug Indications
Prooxycaine is a local anesthetic. It has been used in dental surgery since the 1950s. It is often used in combination with procaine to accelerate onset and provide a longer-lasting anesthetic effect. Prooxycaine was developed for use when amide-based local anesthetics are contraindicated due to allergy or when multiple amide-based anesthetics are ineffective. Mechanism of Action Prooxycaine is a para-aminobenzoic acid ester with local anesthetic activity. Prooxycaine binds to voltage-gated sodium channels and blocks their permeability, thereby inhibiting the ion flow necessary for nerve impulse conduction. This leads to loss of sensation. One study showed that propyloxycaine hydrochloride increases the fluidity of cyclic lipids in the cellular lipid bilayer, with a stronger enhancing effect on the inner monolayer than the outer monolayer. This may further confirm its role in regulating nerve impulses. Pharmacodynamics Prooxycaine is a local anesthetic whose mechanism of action is to reduce nerve impulses, thereby alleviating pain during dental procedures.
Propoxycaine hydrochloride is an ester local anesthetic with a rapid onset and longer duration of action than procaine. It inhibits voltage-gated sodium channels, modulating nerve impulses and inducing sensory loss. The compound was used in dentistry and for pain control of intramuscular injections. It was removed from the US market in 1996. Its molecular formula is C16H26N2O3·HCl with a molecular weight of 330.85 g/mol. All applications are limited to non-human research use.

C16H26N2O3.HCL

330.85018

330.171

550-83-4

6843

White to light brown solid powder

434.4ºC at 760mmHg

146-151

216.5ºC

3.939

1

5

10

21

295

0

CAJIGINSTLKQMM-UHFFFAOYSA-N

InChI=1S/C16H26N2O3/c1-4-10-20-15-12-13(17)7-8-14(15)16(19)21-11-9-18(5-2)6-3/h7-8,12H,4-6,9-11,17H2,1-3H3

2-(diethylamino)ethyl 4-amino-2-propoxybenzoate

2934.99.9001

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, avoid exposure to moisture.

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

H2O : ~100 mg/mL (~302.25 mM)
DMSO : ~50 mg/mL (~151.13 mM)

Solubility in Formulation 1: ≥ 2.08 mg/mL (6.29 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.

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Solubility in Formulation 2: ≥ 2.08 mg/mL (6.29 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.

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Solubility in Formulation 3: ≥ 2.08 mg/mL (6.29 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 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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Solubility in Formulation 4: ≥ 100 mg/mL (302.25 mM) (saturation unknown) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution.

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 (Please use freshly prepared in vivo formulations for optimal results.)