Objective The present study was aimed to investigate the pharmacological modulatory effects of ropivacaine,an amide-type local anesthetic,on rat Nav1.2（rNav1.2）and rNav1.5,the two Na＋channel isoforms heterologously expressed in Xenopus oocytes and in HEK293t cell line,respectively.Methods Two-electrode voltage-clamp（TEVC）and whole-cell patchclamp recordings were employed to record the whole-cell currents.Results Ropivacaine induced tonic inhibition of peak Na＋ currents of both subtypes in a dose-and frequency-dependent manner.rNav1.5 appeared to be more sensitive to ropivacaine.In addition,for both Na＋channel subtypes,the steady-state inactivation curves,but not the activation curves,were significantly shifted to the hyperpolarizing direction by ropivacaine.Use-dependent blockade of both rNav1.2 and rNav1.5 channels was induced by ropivacaine through a high frequency of depolarization,suggesting that ropivacaine could preferentially bind to the 2 inactivated Na＋channel isoforms.Conclusion The results will be helpful in understanding the pharmacological modulation by ropivacaine on Nav1.2 subtype in the central nervous system,and on Nav1.5 subtype abundantly expressed in the heart.
