title: Inhibition of Kv7/M Channel Currents by the Local Anesthetic Chloroprocaine.
abstract: BACKGROUND
  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.
  
  
  METHODS
  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.
  
  
  RESULTS
  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.
  
  
  CONCLUSIONS
  Taken together, the findings indicate that chloroprocaine concentration dependently inhibited Kv7/M channel currents.
authors.affiliation: The Key Laboratory of New Drug Pharmacology and Toxicology, Department of Pharmacology, Hebei Medical University, Shijiazhuang, China.
authors.forename: Fan
authors.initials: F
authors.lastname: Zhang
authors.forename: Yanxin
authors.initials: Y
authors.lastname: Cheng
authors.forename: Hong
authors.initials: H
authors.lastname: Li
authors.forename: Qingzhong
authors.initials: Q
authors.lastname: Jia
authors.forename: Hailin
authors.initials: H
authors.lastname: Zhang
authors.forename: Senming
authors.initials: S
authors.lastname: Zhao
mesh_terms: D000779:Anesthetics, Local / Q000494:pharmacology*; D000818:Animals; D002219:Carbamates / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D005727:Ganglia, Spinal / Q000187:drug effects; D057809:HEK293 Cells; D006801:Humans; D051658:KCNQ2 Potassium Channel / Q000187:drug effects*; D051659:KCNQ3 Potassium Channel / Q000187:drug effects*; D008564:Membrane Potentials / Q000187:drug effects; D009474:Neurons / Q000187:drug effects; D018408:Patch-Clamp Techniques; D010655:Phenylenediamines / Q000494:pharmacology; D026902:Potassium Channel Blockers / Q000494:pharmacology*; D011343:Procaine / Q000031:analogs & derivatives* / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley; D012640:Seizures / Q000139:chemically induced
chemical_list: D000779:Anesthetics, Local; D002219:Carbamates; D051658:KCNQ2 Potassium Channel; D051659:KCNQ3 Potassium Channel; D010655:Phenylenediamines; D026902:Potassium Channel Blockers; C101866:ezogabine; D011343:Procaine; C004616:chloroprocaine