Anxiolytic-like effects of YL-IPA08, a potent ligand for the translocator protein (18 kDa) in animal models of post-traumatic stress disorder

Int J Neuropsychopharmacol. 2014 Oct;17(10):1659-69. doi: 10.1017/S1461145714000479. Epub 2014 Apr 24.

Abstract

Recently, the translocator protein (18 kDa) (TSPO), previously called peripheral benzodiazepine receptor (PBR) and both the starting point and an important rate-limiting step in neurosteroidogenesis, has received increased attention in the pathophysiology of post-traumatic stress disorder (PTSD) because it affects the production of neurosteroids, reinforcing the hypothesis that selective TSPO ligands could potentially be used as anti-PTSD drugs. As expected, we showed that chronic treatment with YL-IPA08 [N-ethyl-N-(2-pyridinylmethyl)-2-(3,4-ichlorophenyl)-7-methylimidazo [1,2-a] pyridine-3-acetamide hydrochloride], a potent and selective TSPO ligand synthesized by our institute, caused significant suppression of enhanced anxiety and contextual fear induced in the inescapable electric foot-shock-induced mouse model of PTSD and the time-dependent sensitization (TDS) procedure. These effects were completely blocked by the TSPO antagonist PK11195. Furthermore, YL-IPA08 could increase the level of allopregnanolone in the prefrontal cortex and serum of post-TDS rats, and these effects were antagonized by PK11195. In summary, the findings from the current study showed that YL-IPA08, a potent and selective TSPO ligand, had a clear anti-PTSD-like effect, which might be partially mediated by binding to TSPO and the subsequent synthesis of allopregnanolone.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Analysis of Variance
  • Animals
  • Anti-Anxiety Agents / chemistry
  • Anti-Anxiety Agents / pharmacology
  • Anti-Anxiety Agents / therapeutic use*
  • Disease Models, Animal
  • Dose-Response Relationship, Drug
  • Electroshock / adverse effects
  • Freezing Reaction, Cataleptic / drug effects
  • Imidazoles / pharmacology
  • Imidazoles / therapeutic use
  • Isoquinolines / pharmacology
  • Isoquinolines / therapeutic use
  • Male
  • Mice
  • Mice, Inbred ICR
  • Motor Activity / drug effects
  • Pyridines / pharmacology
  • Pyridines / therapeutic use
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, GABA / metabolism
  • Sertraline / pharmacology
  • Sertraline / therapeutic use
  • Stress Disorders, Post-Traumatic / drug therapy*
  • Stress Disorders, Post-Traumatic / etiology

Substances

  • Anti-Anxiety Agents
  • Bzrp protein, mouse
  • Imidazoles
  • Isoquinolines
  • N-ethyl-N-(2-pyridinylmethyl)-2-(3,4-chlorophenyl)-7-methylimidazo(1,2-a)pyridine-3-acetamide
  • Pyridines
  • Receptors, GABA
  • Sertraline
  • PK 11195