Procaine hydrochloride (Novocaine HCl) is the hydrochloride salt form of procaine, a benzoic acid derivative with local anesthetic and antiarrhythmic properties. Procaine binds to and inhibits voltage-gated sodiumchannels, thereby inhibiting the ionic flux required for the initiation and conduction of impulses. In addition, this agent increases electrical excitation threshold, reduces rate of rise of action potential and slows nerve impulse propagation thereby causing loss of sensation.

5-HT3:1.7 μM(Kd), nAChR:45.5 μM, NMDAR:0.296 mM, Na+ channel:60 μM

在清醒的猫体内,Procaine（15 mg/kg）增加杏仁核腹侧海马体,腹内侧下丘脑,伏隔核和颞叶新皮质的细胞活性.Procaine是边缘系统细胞的兴奋剂.Procaine促进诱发的刺激活性从杏仁核到腹内侧下丘脑的传导.

Procaine具有结合或拮抗烟碱型乙酰胆碱受体和5-羟色胺受体-离子通道复合体与N-甲基-D-天冬氨酸受体的功能。Procaine主要通过抑制钠离子进而影响外周神经的神经元细胞膜上电压门控钠离子通道的内流来发挥作用。当钠离子内流被中断时,动作电位被阻断,信号传导也因此受到抑制。有研究认为受体部位是位于钠通道的细胞质(内部)部分。