title: Lidocaine effects on acetylcholine-elicited currents from mouse superior cervical ganglion neurons.
abstract: Lidocaine is a commonly used local anaesthetic that, besides blocking voltage-dependent Na(+) channels, has multiple inhibitory effects on muscle-type nicotinic acetylcholine (ACh) receptors (nAChRs). In the present study, we have investigated the effects of lidocaine on ACh-elicited currents (IAChs) from cultured mouse superior cervical ganglion (SCG) neurons, which mainly express heteromeric α3β4 nAChRs. Neurons were voltage-clamped by using the perforated-patch method and IAChs were elicited by fast application of ACh (100-300μM), either alone or in presence of lidocaine at different concentrations. IAChs were reversibly blocked by lidocaine in a concentration-dependent way (IC50=41μM; nH close to 1) and the inhibition was, at least partially, voltage-dependent, indicating an open-channel blockade. Besides, lidocaine blocked resting (closed) nAChRs, as evidenced by the increased inhibition caused by a 12s lidocaine application just before its co-application with the agonist, and also enhanced IAChs desensitisation, at concentrations close to the IC50. These results indicate that lidocaine has diverse inhibitory actions on neuronal heteromeric nAChRs resembling those previously reported for Torpedo (muscle-type) nAChRs (Alberola-Die et al., 2011). The similarity of lidocaine actions on different subtypes of heteromeric nAChRs differs with the specific effects of other compounds, restricted to particular subtypes of nAChRs.
authors: División de Fisiología, Departamento de Fisiología, Genética y Microbiología, Universidad de Alicante, E-03080 Alicante, Spain.
authors: Armando
authors: A
authors: Alberola-Die
authors: Antonio
authors: A
authors: Reboreda
authors: J Antonio
authors: JA
authors: Lamas
authors: Andrés
authors: A
authors: Morales
mesh_terms: D000109:Acetylcholine / Q000494:pharmacology*; D000818:Animals; D002478:Cells, Cultured; D015640:Ion Channel Gating / Q000187:drug effects*; D008012:Lidocaine / Q000037:antagonists & inhibitors / Q000494:pharmacology*; D051379:Mice; D009419:Nerve Tissue Proteins / Q000187:drug effects; D009474:Neurons / Q000187:drug effects*; D018408:Patch-Clamp Techniques; D011978:Receptors, Nicotinic / Q000145:classification / Q000187:drug effects*; D017783:Superior Cervical Ganglion / Q000187:drug effects*; D061567:Voltage-Gated Sodium Channel Blockers / Q000494:pharmacology*
chemical_list: D000109:Acetylcholine; D008012:Lidocaine; D009419:Nerve Tissue Proteins; D011978:Receptors, Nicotinic; D061567:Voltage-Gated Sodium Channel Blockers; C486720:Chrnb4 protein, mouse