PNU-120596, a positive allosteric modulator of α7 nicotinic acetylcholine receptors, reverses a sub-chronic phencyclidine-induced cognitive deficit in the attentional set-shifting task in female rats

J Psychopharmacol. 2012 Sep;26(9):1265-70. doi: 10.1177/0269881111431747. Epub 2011 Dec 18.

Abstract

The α7 nicotinic acetylcholine receptors (nAChRs) have been highlighted as a target for cognitive enhancement in schizophrenia. Adult female hooded Lister rats received sub-chronic phencyclidine (PCP) (2 mg/kg) or vehicle i.p. twice daily for 7 days, followed by 7 days' washout. PCP-treated rats then received PNU-120596 (10 mg/kg; s.c.) or saline and were tested in the attentional set-shifting task. Sub-chronic PCP produced a significant cognitive deficit in the extra-dimensional shift (EDS) phase of the task (p < 0.001, compared with vehicle). PNU-120596 significantly improved performance of PCP-treated rats in the EDS phase of the attentional set-shifting task (p < 0.001). In conclusion, these data demonstrate that PNU-120596 improves cognitive dysfunction in our animal model of cognitive dysfunction in schizophrenia, most likely via modulation of α7 nACh receptors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Allosteric Regulation
  • Animals
  • Attention / drug effects
  • Behavior, Animal / drug effects
  • Brain / metabolism
  • Cognition Disorders / chemically induced
  • Cognition Disorders / drug therapy*
  • Cognition Disorders / physiopathology
  • Discrimination Learning / drug effects
  • Disease Models, Animal
  • Drug Interactions
  • Female
  • Half-Life
  • Hallucinogens / administration & dosage
  • Hallucinogens / toxicity
  • Isoxazoles / metabolism
  • Isoxazoles / pharmacokinetics
  • Isoxazoles / therapeutic use*
  • Neurons / metabolism
  • Neuroprotective Agents / metabolism
  • Neuroprotective Agents / pharmacokinetics
  • Neuroprotective Agents / therapeutic use*
  • Neurotoxicity Syndromes / drug therapy*
  • Neurotoxicity Syndromes / physiopathology
  • Nicotinic Agonists / metabolism
  • Nicotinic Agonists / pharmacokinetics
  • Nicotinic Agonists / therapeutic use*
  • Phencyclidine / administration & dosage
  • Phencyclidine / toxicity*
  • Phenylurea Compounds / metabolism
  • Phenylurea Compounds / pharmacokinetics
  • Phenylurea Compounds / therapeutic use*
  • Rats
  • Rats, Inbred Strains
  • Receptors, Nicotinic / chemistry*
  • Tissue Distribution
  • alpha7 Nicotinic Acetylcholine Receptor

Substances

  • 1-(5-chloro-2,4-dimethoxyphenyl)-3-(5-methylisoxazol-3-yl)urea
  • Chrna7 protein, rat
  • Hallucinogens
  • Isoxazoles
  • Neuroprotective Agents
  • Nicotinic Agonists
  • Phenylurea Compounds
  • Receptors, Nicotinic
  • alpha7 Nicotinic Acetylcholine Receptor
  • Phencyclidine