Anxioselective anxiolytics: can less be more?

Eur J Pharmacol. 2004 Oct 1;500(1-3):441-51. doi: 10.1016/j.ejphar.2004.07.043.

Abstract

Benzodiazepines remain widely used for the treatment of anxiety disorders despite a side-effect profile that includes sedation, myorelaxation, amnesia, and ataxia, and the potential for abuse. gamma-Aminobutyric acid(A) (GABA(A)) receptor partial agonists, subtype-selective agents, and compounds combining both of these features are being developed in an attempt to achieve benzodiazepine-like efficacy without these potentially limiting side effects. This article reviews the nonclinical and clinical studies of "anxioselective" anxiolytics that target GABA(A) receptors and discusses potential mechanisms subserving an anxioselective profile.

Publication types

  • Review

MeSH terms

  • Animals
  • Anti-Anxiety Agents / pharmacology*
  • Anti-Anxiety Agents / therapeutic use
  • Anxiety Disorders / drug therapy*
  • Benzodiazepinones / pharmacology
  • Benzodiazepinones / therapeutic use
  • Carbolines / pharmacology
  • Carbolines / therapeutic use
  • Clinical Trials as Topic
  • Fluorobenzenes / pharmacology
  • Fluorobenzenes / therapeutic use
  • GABA-A Receptor Agonists*
  • Humans
  • Indoles / pharmacology
  • Indoles / therapeutic use
  • Pyrroles / pharmacology
  • Pyrroles / therapeutic use
  • Quinolones / pharmacology
  • Quinolones / therapeutic use
  • Triazoles / pharmacology
  • Triazoles / therapeutic use

Substances

  • 6-fluoro-9-methyl-2-phenyl-4-(pyrrolidin-1-yl-carbonyl)-2,9-dihydro-1H-pyrido(3,4-b)indol-1-one
  • Anti-Anxiety Agents
  • Benzodiazepinones
  • Carbolines
  • Fluorobenzenes
  • GABA-A Receptor Agonists
  • Indoles
  • Pyrroles
  • Quinolones
  • Triazoles
  • L 838,417
  • abecarnil
  • bretazenil