Molecular mechanism of modulation of nociceptive neuron membrane excitability by a tripeptide

Using the whole-cell patch-clamp method, the ability of arginine-containing tripeptide Ac-RER-NH₂, dipeptide Ac-RR-NH₂, and free Arg molecule to modulate the membrane excitability of nociceptors was studied. Extracellular Ac-RER-NH₂ upon interaction with the outer membrane of the nociceptive neuron decreases the Z_eff value of the activation gating system of Na_v1.8 channels. Thus, the tripeptide Ac-RER-NH₂ can be considered as a new effective and safe analgesic.