title: Lamotrigine is an open-channel blocker of the nicotinic acetylcholine receptor.
abstract: Lamotrigine is an antiepileptic drug employed in the treatment of partial epilepsies. We studied its possible interaction with channels other than its known therapeutic target, the voltage-gated sodium channel, using the adult muscle nicotinic acetylcholine receptor as a model system. At the single-channel level, lamotrigine caused a dose-dependent (a) diminution in mean open time, (b) increase in mean burst duration and (c) increase in the area of a new closed-time component. A simple linear channel blocking mechanism accounts for these results. Thus, lamotrigine exerts a blocking action on the muscle nicotinic acetylcholine receptor.
authors.affiliation: UNESCO Chair of Biophysics and Molecular Neurobiology and Instituto de Investigaciones Bioquímicas de Bahía Blanca, Bahía Blanca, Buenos Aires, Argentina. svalles@criba.edu.ar
authors.forename: Ana S
authors.initials: AS
authors.lastname: Vallés
authors.forename: Ingrid
authors.initials: I
authors.lastname: Garbus
authors.forename: Francisco J
authors.initials: FJ
authors.lastname: Barrantes
mesh_terms: D000818:Animals; D016466:CHO Cells; D006224:Cricetinae; D003412:Cricetulus; D004305:Dose-Response Relationship, Drug; D004307:Dose-Response Relationship, Radiation; D004558:Electric Stimulation; D018691:Excitatory Amino Acid Antagonists / Q000737:chemistry / Q000494:pharmacology*; D015640:Ion Channel Gating / Q000187:drug effects*; D000077213:Lamotrigine; D008564:Membrane Potentials / Q000187:drug effects; D018408:Patch-Clamp Techniques; D011978:Receptors, Nicotinic / Q000187:drug effects*; D014227:Triazines / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D018691:Excitatory Amino Acid Antagonists; D011978:Receptors, Nicotinic; D014227:Triazines; D000077213:Lamotrigine