Molecular and physicochemical aspects of local anesthetics acting on nicotinic acetylcholine receptor-containing membranes.
Local anesthetics inhibit the ion channel activity of nicotinic acetylcholine receptors in a noncompetitive fashion. This inhibitory action is ascribed to two possible inhibitory mechanisms: an open-channel-blocking mechanism and/or an allosteric process where the drug binds either to the closed channel or to other nonluminal sites, respectively.
Arias
Hugo R
HR
Departments of Pharmacology and Anesthesiology, School of Medicine, Texas Tech University Health Sciences Center, Lubbock 79430, USA. huruar@pharmacology.ufl.edu
Blanton
Michael P
MP
D000494:Allosteric Regulation / Q000187:drug effects; D000779:Anesthetics, Local / Q000737:chemistry* / Q000494:pharmacology; D000818:Animals; D006801:Humans; D007473:Ion Channels / Q000037:antagonists & inhibitors*; D008564:Membrane Potentials / Q000187:drug effects; D018733:Nicotinic Antagonists / Q000737:chemistry / Q000494:pharmacology; D011978:Receptors, Nicotinic / Q000737:chemistry / Q000187:drug effects* / Q000502:physiology; D013329:Structure-Activity Relationship
D000779:Anesthetics, Local; D007473:Ion Channels; D018733:Nicotinic Antagonists; D011978:Receptors, Nicotinic