Lidocaine is a commonly used local anesthetic as well as an antiarrhythmic drug, which is a potent and selective blocker of Nav channels. It inhibits, for instance, human Nav1.5 channels expressed in Xenopus oocytes in a positive rate-dependent and concentration-dependent manner, with an IC50 value of 145.6 µM. Its block can be complex, exhibiting channel state-dependent and time-dependent elements.
产品描述
A State Dependent NaV Channel Inhibitor
产品形式
Voltage-gated Na+ channels (VGSC, Nav) are critically important for electrogenesis and nerve impulse conduction, and as targets for important clinically relevant analgesics such as Lidocaine. Certain NaV channel isoforms are predominantly expressed in peripheral sensory neurons associated with pain sensation, and the expression and functional properties of Nav channels in peripheral sensory neurons can be dynamically regulated following axonal injury or peripheral inflammation.
