Endozepinas: el valium cerebral

Abstract

Las benzodiazepinas conforman uno de los grupos de fármacos más demandados por la población debido a su potente acción sedante, hipnótica, ansiolítica, anticonvulsiva y miorrelajante. Se unen al receptor GABAA actuando como moduladores alostéricos positivos. El estudio del receptor benzodiazepínico llevó a los investigadores a plantearse la posible existencia de unas moléculas endógenas que se unieran al mismo, justificando así su presencia en el organismo. Estos ligandos son conocidos como endozepinas. Existen varias candidatas, entre las que destaca el inhibidor de la unión a diazepam (DBI). A día de hoy, por su complejidad, no se conoce con exactitud su mecanismo de acción. Lo que sí se ha demostrado es su participación en diversos procesos patológicos como la encefalopatía hepática, el estupor idiopático y el cáncer de pulmón.

Benzodiazepines are one of the most commonly prescribed drugs due to their sedative, anxiolytic, muscle relaxing, hypnotic and relief from spasticity properties. Their mechanism of action is based on their binding to the GABAA receptor, acting as positive allosteric modulators. Surveys about the benzodiazepinic receptor has lead researchers to consider the possible existence of endogenous ligands which bound to it. This fact would justify its presence in our organism. These endogenous ligands are known as endozepines, a term which has uncovered a variety of ligands that might fulfill this role. The protein diazepam-binding inhibitor (DBI) is the most studied endozepine. Yet today, as a matter of its complexity, their mechanism of action hasn’t been elucidated. What has already been demonstrated is their involvement in some pathological processes such as hepatic encephalopathy, recurrent idiopathic stupor and lung cancer.