General and local anaesthetics perturb the fusion of phospholipid vesicles.
The effects of general and local anaesthetics on Ca2+-induced fusion of negatively charged lipid vesicles have been investigated. Vesicles composed of phosphatidylcholine and phosphatidic acid (2:1 molar ratio) were induced to fuse using 5 mM free Ca2+. Fusion, assessed by an increase in size using gel filtration techniques and confirmed by electron microscopy, displayed a dependence on Ca2+ and Mg2+ concentration and on temperature. The inhalational anaesthetics halothane, methoxyflurane and diethyl ether enhanced fusion as did the uncharged local anaesthetic benzocaine. In contrast, the charged local anaesthetics lignocaine and bupivacaine inhibited the fusion process. It is suggested that the enhancement observed with the inhalational anaesthetics and benzocaine was mediated by an effect on lipid fluidity and the inhibition observed with the charged tertiary amine anaesthetics was due to an antagonism towards Ca2+.
D000777:Anesthetics / Q000494:pharmacology*; D000779:Anesthetics, Local / Q000494:pharmacology; D002045:Bupivacaine / Q000494:pharmacology; D002118:Calcium / Q000494:pharmacology; D002850:Chromatography, Gel; D004986:Ether / Q000494:pharmacology; D006221:Halothane / Q000494:pharmacology; D008012:Lidocaine / Q000494:pharmacology; D008081:Liposomes; D008561:Membrane Fusion / Q000187:drug effects*; D008733:Methoxyflurane / Q000494:pharmacology; D008854:Microscopy, Electron; D010712:Phosphatidic Acids; D010713:Phosphatidylcholines; D013696:Temperature
D000777:Anesthetics; D000779:Anesthetics, Local; D008081:Liposomes; D010712:Phosphatidic Acids; D010713:Phosphatidylcholines; D004986:Ether; D008733:Methoxyflurane; D008012:Lidocaine; D002118:Calcium; D006221:Halothane; D002045:Bupivacaine