Drug intelligence / Profile preview

procaine

Development stage
Phase 3
Modality
Small Molecules
Administration
Intramuscular, Subcutaneous, Intravenous, Intrathecal, Infiltration
01

Overview

Procaine is a local anesthetic of the amino ester group, primarily used to produce local or regional anesthesia, especially in dental procedures and minor surgeries. It was first synthesized in 1905 by Alfred Einhorn and introduced under the trade name Novocain. Its mechanism of action involves blocking voltage-gated sodium channels on neuronal cell membranes, thereby inhibiting nerve impulse conduction and producing loss of sensation. In addition to its primary action as a sodium channel blocker, procaine has been shown to antagonize NMDA receptors, nicotinic acetylcholine receptors, serotonin receptor-ion channel complexes (notably 5-hydroxytryptamine receptor 3A), inhibit monoamine oxidase activity, block calcium-activated potassium channels, and inhibit DNA methyltransferases among other targets. It is metabolized by plasma esterases into para-amino benzoic acid (PABA) and excreted via the kidneys[1][5][7].

Brand names
NovocainNovocaineMericaine
Other names
2-Diethylaminoethyl p-aminobenzoate monohydrochlorideProcaïneProcaínaProcaine HydrochlorideChlorhydrate de Procaïne
02

Targets

SCN10A (Sodium channel protein type X alpha subunit)CHRNA2 (nAChR α2)KCNN1 (Small conductance calcium-activated potassium channel protein 1)HTR3A (5-hydroxytryptamine receptor 3A)GRIN3A (Glutamate receptor ionotropic, NMDA subunit 3A)DNMT3A (DNA methyltransferase 3 alpha)DAT (Dopamine plasma membrane transport protein)DNMT1 (DNA (cytosine-5)-methyltransferase 1)

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