Flunitrazepam-membrane binding: a sensor for drug-induced GABAA-R and membrane structure changes

TURINA AV; GARCIA DA; PERILLO MA

Neuropathology of drug addiction and substance misused. 2.2 Club drugs.

Elsevier

Lugar: Londres; Año: 2016; p. 445 - 450

Flunitrazepam (FNZ) is a sedative-hypnotic benzodiazepine with important therapeutic usefulness and significant abuse liability. Its capability to induce anterograde amnesia favors FNZ use as a ?date-rape drug? often at a bar or party (?club drug?) by adding it unknowingly in the drinks of victims who will have limited memory of the assault. Contrary, on the illicit market, ?FNZ preparations? may be faked products that do not contain that substance. FNZ combined with anesthetics, opiods, ethanol, cocaine and methamphetamine can occur in therapeutic use and in polydrug abuse. FNZ action mechanism involves its binding to g-aminobutyricacid receptor (GABAA-R), an intrinsic membrane protein. Changes in the binding site structure through allosteric binding of another drug or affecting lipid phase dynamics in receptor´s surroundings, can modulate this binding activity. Thus, FNZ-GABAA-R binding may serve to sense FNZ concentration, GABAA-R environment organization and FNZ interaction with other drugs, including polydrug use or abuse conditions.