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Assessment of the effects of NS11394 and L-838417, α2/3 subunit-selective GABA(A) [corrected] receptor-positive allosteric modulators, in tests for pain, anxiety, memory and motor function.

Abstract
The aim of the present paper was to study the effects of GABAA receptor-positive modulators (L-838417 and NS11394) showing a preference for α2/3 subunits of the GABAA receptor, in models of pain, anxiety, learning, memory and motor function. These compounds have been suggested to have a favourable therapeutic profile over nonselective compounds such as diazepam. In this study, we tested both compounds for their effects in rat models of formalin-induced pain, spinal nerve-ligation-induced mechanical allodynia, plus maze, open field, rotarod, balance beam walking, contextual fear conditioning and Morris water maze. Both compounds exerted analgesic, but no anxiolytic effects. However, they induced motor side-effects, and learning and memory impairment at similar doses. Therefore, the anxiolytic effect and the lack of side-effects of these compounds, as described in the literature, could not be confirmed in the present study.
AuthorsMartine Hofmann, Krisztina Sz Kordás, Andreas Gravius, Kata Bölcskei, Chris G Parsons, Andrzej Dekundy, Wojciech Danysz, László Dézsi, Ina M Wittko-Schneider, Katalin Sághy, István Gyertyán, Csilla Horváth
JournalBehavioural pharmacology (Behav Pharmacol) Vol. 23 Issue 8 Pg. 790-801 (Dec 2012) ISSN: 1473-5849 [Electronic] England
PMID23075708 (Publication Type: Comparative Study, Journal Article)
Chemical References
  • 3'-(5-(1-hydroxy-1-methylethyl)benzoimidazol-1-yl)biphenyl-2-carbonitrile
  • Analgesics
  • Benzimidazoles
  • Fluorobenzenes
  • GABA-A Receptor Agonists
  • Receptors, GABA-A
  • Triazoles
  • L 838,417
Topics
  • Allosteric Regulation
  • Analgesics (administration & dosage, pharmacology, toxicity)
  • Animals
  • Anxiety (drug therapy)
  • Benzimidazoles (administration & dosage, pharmacology, toxicity)
  • Disease Models, Animal
  • Dose-Response Relationship, Drug
  • Fear
  • Fluorobenzenes (administration & dosage, pharmacology, toxicity)
  • GABA-A Receptor Agonists (administration & dosage, pharmacology, toxicity)
  • Male
  • Maze Learning (drug effects)
  • Memory Disorders (chemically induced)
  • Motor Activity
  • Pain (drug therapy, physiopathology)
  • Rats
  • Rats, Wistar
  • Receptors, GABA-A (drug effects, metabolism)
  • Triazoles (administration & dosage, pharmacology, toxicity)

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