Referenced in: none

Automatically associated channels: Kv7.2 , Kv7.3 , Slo1

Title: Inhibition of Kv7/M Channel Currents by the Local Anesthetic Chloroprocaine.

Authors: Fan Zhang, Yanxin Cheng, Hong Li, Qingzhong Jia, Hailin Zhang, Senming Zhao

Journal, date & volume: Pharmacology, 2015 , 96, 124-30

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/26202459

Abstract
Chloroprocaine is a local ester anesthetic, producing excellent sensory block in clinical use. The Kv7/M potassium channel plays an important role in the control of neuronal excitability. In this study, we investigated the effects of the local anesthetic chloroprocaine on Kv7/M channels as well as the effect of retigabine on chloroprocaine-induced seizures.A perforated whole-cell patch technique was used to record Kv7 currents from HEK293 cells and M-type currents from rat dorsal root ganglion (DRG) neurons.Chloroprocaine produced a number of effects on Kv7.2/Kv7.3 currents, including a lowering of current amplitudes, a rightward shift in the voltage-dependent activation curves, and a slowing of channel activation. Chloroprocaine had a more selective inhibitory effect on the homomeric Kv7.3 and heteromeric Kv7.2/Kv7.3 channels than on the homomeric Kv7.2 channel. Chloroprocaine also inhibited native M channel currents and induced a depolarization of the DRG neuron membrane potential.Taken together, the findings indicate that chloroprocaine concentration dependently inhibited Kv7/M channel currents.