The quaternary lidocaine derivative QX-314 produces long-lasting intravenous regional anesthesia in rats

Background The lidocaine derivative, QX-314, produces long-lasting regional anesthesia in various animal models. We designed this study to examine whether QX-314 could produce long-lasting intravenous regional anesthesia (IVRA) in a rat model. Methods IVRA was performed on tail of rats. EC50 (median effective concentration) of QX-314 in IVRA was determined by up-and-down method. IVRA on tail of rats was evaluated by tail-flick and tail-clamping tests. For comparison between QX-314 and lidocaine, 60 Sprague-Dawley rats were randomly divided into 6 groups (n = 10/group), respectively receiving 0.5 ml of 0.5% lidocaine, 0.25% QX-314, 0.5% QX-314, 1.0% QX-314, 2.0% QX-314 and normal saline. To explore the role of TRPV1 channel in IVRA of QX-314, 20 rats were randomly divided into 2 groups (n = 10/group), respectively receiving 0.5 ml of 1% QX-314 and 1% QX-314+75 µg/ml capsazepine. Toxicities of QX-314 on central nervous system and cardiac system were measured in rats according to Racine's convulsive scale and by electrocardiogram, respectively. Results QX-314 could produce long-lasting IVRA in a concentration-dependent manner. EC50 of QX-314 in rat tail IVRA was 0.15±0.02%. At concentration of 0.5%, IVRA duration of QX-314 (2.5±0.7 hour) was significantly longer than that of 0.5% lidocaine (0.3±0.2 hour, P