GABERGIC PHENOLS ARE CAPABLE TO MODULATE LIPID PHASE TRANSITION RESEMBLING PROPOFOL BEHAVIOR.

MIGUEL V; SANCHEZ-BORZONE M; GARCÍA, D. A.

San Miguel de Tucumán

Congreso; III Latin American Federation of Biophysical Societies (LAFeBS) IX IberoAmerican Congress of Biophysics XLV Reunion Anual SAB 2016; 2016

Sociedad Argentina de Biofísica

GABAA receptor (GABA-R) is the main inhibitory receptor of the central nervous system. Its ligands include drugs other than the GABAneurotransmitter, such as benzodiazepines, barbiturates, anesthetics,ethanol and the convulsant picrotoxinin, which behave as allostericmodulators or channel blockers. There is still considerable debate aboutmolecular mechanisms by which general anesthetics induce sedation.Since many lipophilic compounds that regulate GABA-R function canchange the physical properties of the lipid bilayer, it is expected thatthe receptor could be modulated not only by the specific ligand recognition, but also by changes in the physical state of the membrane. Previous experimental results from our group have demonstrated that theintravenous anesthetic propofol, and other derived phenols with gabaergic activity, are able to interact with membranes. NMR, fluorescenceanisotropy and Langmuir films studies indicated that they locate in theregion between the polar group and the first atoms of the acyl chains