Procaine

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Cat Number

CAS Number

59-46-1

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CAS Number

59-46-1

Storage

2-8 ℃

Molecular Formula

C13H20N2O2

Molecular Weight

236.31

Smiles

CCN(CC)CCOC(=O)C1=CC=C(C=C1)N

Appearance

Crystalline powder

Melting Point

61 ℃

Boiling Point

373.6±22.0 ℃ at 760 mmHg

Relative Density

1.1±0.1

General Description

Procaine is an ester-type local anesthetic valued for its rapid onset, moderate duration of action, and low toxicity — traits that have made it a staple in clinical practice. Clinically, it is most commonly formulated as procaine hydrochloride (Procaine HCl), which significantly improves its water solubility and stability. What’s more, procaine is quickly metabolized by plasma esterases in the body, rendering it especially well-suited for medical procedures that demand short-acting, controllable anesthesia.

Mechanism of Action

Procaine works by blocking voltage-gated sodium channels on neuronal cell membranes — that stops depolarization and keeps nerve impulses from traveling. By putting the brakes on action potential initiation and spread, it brings on reversible local anesthesia right where it’s needed.
As an ester-type anesthetic, plasma pseudocholinesterase breaks it down into para-aminobenzoic acid (PABA) and diethylaminoethanol (DEAE) — that’s why its effects don’t last long. This setup delivers solid pain relief while cutting down on systemic toxicity way more than older anesthetics did.

Application

Local Anesthesia: Perfect for dental work, minor surgeries, and diagnostic tests that need short-term numbing in a specific area.
Nerve Block Procedures: Temporarily shuts down peripheral nerves to ease pain and help with small-scale surgical jobs.
Procaine Penicillin Formulation: A key part of long-acting antibiotic injections — Procaine takes the sting out of the injection site while slowing penicillin release for longer-lasting effects.
Research and Laboratory Use: Frequently used in electrophysiology studies, ion channel research, and as a reference standard for looking into how anesthetics work.
Pain Management: Sometimes mixed into therapeutic injections for inflammatory or musculoskeletal pain, particularly in integrative medicine practices.

Voltage-gated sodium channels (VGSCs) are essential for the initiation and propagation of action potentials in peripheral nerves. When these channels open, sodium ions rapidly enter the neuron, leading to membrane depolarization and signal conduction. Local anesthetics, including Procaine, interrupt this process by blocking sodium influx, resulting in loss of sensation in the innervated area.
Procaine must first diffuse across the neuronal membrane in its non-ionized form. Inside the cytoplasm, the drug becomes ionized and binds to the intracellular portion of the sodium channel. This binding stabilizes the inactivated state of the channel and prevents its return to the resting, activatable form. As a result, action potentials cannot be generated or propagated.
According to Becker and Reed (2006), Procaine displays classical characteristics of local anesthetic pharmacology, including state-dependent binding and preferential inhibition of rapidly firing or damaged nerves. Its anesthetic effect is localized, reversible, and concentration-dependent.
The main mechanisms of Procaine’s sodium-channel–blocking effect include:
Penetrating the neuronal membrane in non-ionized form and becoming ionized intracellularly
Binding to the intracellular side of voltage-gated sodium channels
Stabilizing the inactivated state of the sodium channel
Preventing sodium influx and blocking action potential propagation
Preferentially inhibiting high-frequency nerve firing and inflamed tissues due to state-dependent affinity

Fig. 1 Local anesthetic action. An injected local anesthetic exists in equilibrium as a quaternary salt (BH+) and tertiary base (B). (Becker DE.; et al. 2006)

References

Becker DE, et al. Essentials of local anesthetic pharmacology.Anesth Prog, 2006 Fall;53(3):98-108.

Jungwirth et al. tested ProcCluster® (PC) — a procaine-based formulation — to see how it fights off Herpes Simplex Virus Type 1 (HSV-1). They checked out its antiviral activity, how it affects viral assembly, and its cytotoxicity in vitro, using several human cell lines: RPE-1, HaCaT, and Kelly neuroblastoma cells.
The study found that at millimolar doses that don’t harm cells, PC significantly blocks HSV-1 replication and stops viral progeny from being released. When cells were treated with PC, the intracellular trafficking of viral glycoprotein gD got thrown off — leading to gD piling up in Rab5-positive early endosomes and Rab11-positive recycling endosomes.
At the same time, PC prevented gD from moving on to Rab7-positive late endosomes or LAMP1-positive lysosomes. This wonky distribution means PC messes with HSV-1’s second envelopment process — a step that’s totally essential for the virus to mature and get released.
Compared to untreated cells or those treated just with solvent, PC cut viral titers way down. What’s more, using PC alongside acyclovir (ACV) made the antiviral effect even stronger — showing that the two work together to reduce HSV-1 replication more effectively.
These findings point to ProcCluster® being a host-directed antiviral. Instead of directly stopping viral DNA replication, it limits the formation and release of mature viral particles.

Fig. 2 ProcCluster® (PC) causes viral glycoproteins to accumulate in endosomes, blocking virus maturation and release. (Jungwirth J.; et al. 2025)

References

Jungwirth J, et al. The Procaine-Based ProcCluster® Impedes the Second Envelopment Process of Herpes Simplex Virus Type 1. International journal of molecular sciences, 2025, 26(15): 7185.