Plasma membrane lipid composition modulates action of anesthetics. 1986

W D Sweet, and F Schroeder

The effect of LM fibroblast plasma membrane phospholipid composition on the selectivity of charged amphipathic anesthetics for exofacial or cytofacial leaflets was examined. Because preference of charged amphipaths for one of the plasma membrane bilayer leaflets may be conferred by net changes in the polar headgroup composition, LM fibroblasts were cultured in the presence of choline or N-demethylated analogs in order to change this polar headgroup composition. These altered bases were incorporated into plasma membrane phospholipids. A significant difference in 1,6-diphenyl-1,3,5-hexatriene (DPH) limiting anisotropy was observed between plasma membrane leaflets of phosphatidylcholine-, but not phosphatidylethanolamine-enriched cells. Phenobarbital, which preferentially decreased the limiting anisotropy of 1,6-diphenyl-1,3,5-hexatriene in the exofacial leaflet, had little or no preferential effect in phosphatidyl-N,N-dimethylethanolamine-enriched membranes. Prilocaine preferentially reduced the limiting anisotropy of 1,6-diphenyl-1,3,5-hexatriene in the exofacial leaflet in phosphatidyl-N-methylethanolamine-enriched membranes, exactly opposite to its effect in phosphatidylcholine-enriched membranes. In contrast, prilocaine had no selective effect in phosphatidylethanolamine-enriched membranes. In summary, the phospholipid polar headgroup composition can dramatically affect the selectivity of charged amphipathic anesthetics in altering the limiting anisotropy, a measure of restriction to motion of 1,6-diphenyl-1,3,5-hexatriene, in individual monolayers.

UI MeSH Term Description Entries
D008563 Membrane Lipids Lipids, predominantly phospholipids, cholesterol and small amounts of glycolipids found in membranes including cellular and intracellular membranes. These lipids may be arranged in bilayers in the membranes with integral proteins between the layers and peripheral proteins attached to the outside. Membrane lipids are required for active transport, several enzymatic activities and membrane formation. Cell Membrane Lipid,Cell Membrane Lipids,Membrane Lipid,Lipid, Cell Membrane,Lipid, Membrane,Lipids, Cell Membrane,Lipids, Membrane,Membrane Lipid, Cell,Membrane Lipids, Cell
D010634 Phenobarbital A barbituric acid derivative that acts as a nonselective central nervous system depressant. It potentiates GAMMA-AMINOBUTYRIC ACID action on GABA-A RECEPTORS, and modulates chloride currents through receptor channels. It also inhibits glutamate induced depolarizations. Phenemal,Phenobarbitone,Phenylbarbital,Gardenal,Hysteps,Luminal,Phenobarbital Sodium,Phenobarbital, Monosodium Salt,Phenylethylbarbituric Acid,Acid, Phenylethylbarbituric,Monosodium Salt Phenobarbital,Sodium, Phenobarbital
D011318 Prilocaine A local anesthetic that is similar pharmacologically to LIDOCAINE. Currently, it is used most often for infiltration anesthesia in dentistry. Propitocaine,Citanest,Citanest Octapressin,Prilocaine Hydrochloride,Xylonest
D002627 Chemistry, Physical The study of CHEMICAL PHENOMENA and processes in terms of the underlying PHYSICAL PHENOMENA and processes. Physical Chemistry,Chemistries, Physical,Physical Chemistries
D002794 Choline A basic constituent of lecithin that is found in many plants and animal organs. It is important as a precursor of acetylcholine, as a methyl donor in various metabolic processes, and in lipid metabolism. Bursine,Fagine,Vidine,2-Hydroxy-N,N,N-trimethylethanaminium,Choline Bitartrate,Choline Chloride,Choline Citrate,Choline Hydroxide,Choline O-Sulfate,Bitartrate, Choline,Chloride, Choline,Choline O Sulfate,Citrate, Choline,Hydroxide, Choline,O-Sulfate, Choline
D005347 Fibroblasts Connective tissue cells which secrete an extracellular matrix rich in collagen and other macromolecules. Fibroblast
D000777 Anesthetics Agents capable of inducing a total or partial loss of sensation, especially tactile sensation and pain. They may act to induce general ANESTHESIA, in which an unconscious state is achieved, or may act locally to induce numbness or lack of sensation at a targeted site. Anesthetic,Anesthetic Agents,Anesthetic Drugs,Anesthetic Effect,Anesthetic Effects,Agents, Anesthetic,Drugs, Anesthetic,Effect, Anesthetic,Effects, Anesthetic
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D013050 Spectrometry, Fluorescence Measurement of the intensity and quality of fluorescence. Fluorescence Spectrophotometry,Fluorescence Spectroscopy,Spectrofluorometry,Fluorescence Spectrometry,Spectrophotometry, Fluorescence,Spectroscopy, Fluorescence
D051379 Mice The common name for the genus Mus. Mice, House,Mus,Mus musculus,Mice, Laboratory,Mouse,Mouse, House,Mouse, Laboratory,Mouse, Swiss,Mus domesticus,Mus musculus domesticus,Swiss Mice,House Mice,House Mouse,Laboratory Mice,Laboratory Mouse,Mice, Swiss,Swiss Mouse,domesticus, Mus musculus

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