SSR181507, a dopamine D₂ receptor and 5-HT(₁A) receptor ligand: evidence for mixed anxiolytic- and antidepressant-like activities

Pharmacol Biochem Behav. 2011 Jan;97(3):428-35. doi: 10.1016/j.pbb.2010.09.019.

Abstract

SSR181507, a dopamine D₂ receptor antagonist/partial agonist and 5-HT(₁A) receptor agonist, is active in animal models of schizophrenia. Furthermore, it shows activity in several anxiety and/or depression models (Depoortere et al. 2003). Presently, we sought to further characterize the latter two activities in rats, using a step-down passive avoidance procedure, a shock-induced ultrasonic vocalization (UV) test in adult subjects and a social interaction test. SSR181507 (0.3 & 1 mg/kg ip), but not the atypical antipsychotics clozapine and olanzapine, decreased the latency time to step-down from a "safety" platform. Effects of SSR181507 were reversed by the selective 5-HT(₁A) receptor antagonist SL88.0338. SSR181507 also reduced UV (0.3 & 1 mg/kg ip), an effect not reversed by SL88.0338, and observed with olanzapine, haloperidol, fluoxetine and the 5-HT(₁A) receptor agonists 8-OH-DPAT and buspirone, but not diazepam. Furthermore, SSR181507 remained active following 3 weeks of administration (1 mg/kg ip, once daily) in the UV test. Lastly, SSR181507 (3 mg/kg ip) potentiated social interaction, an effect shared by diazepam and buspirone, but not by olanzapine, clozapine, haloperidol and 8-OH-DPAT. These data further strengthen previous findings that the putative atypical antipsychotic SSR181507 has mixed antidepressant and anxiolytic activities.

MeSH terms

  • Animal Communication
  • Animals
  • Anti-Anxiety Agents / pharmacology*
  • Antidepressive Agents / pharmacology*
  • Behavior, Animal / drug effects
  • Dioxanes / pharmacology*
  • Ligands
  • Male
  • Rats
  • Rats, Sprague-Dawley
  • Rats, Wistar
  • Receptor, Serotonin, 5-HT1A / drug effects*
  • Receptor, Serotonin, 5-HT1A / metabolism
  • Receptors, Dopamine D2 / drug effects*
  • Receptors, Dopamine D2 / metabolism
  • Tropanes / pharmacology*

Substances

  • (3-exo)-8-benzoyl-N-(((2S)7-chloro-2,3-dihydro-1,4-benzodioxin-1-yl)methyl)-8-azabicyclo(3.2.1)octane-3-methanamine monohydrochloride
  • Anti-Anxiety Agents
  • Antidepressive Agents
  • Dioxanes
  • Ligands
  • Receptors, Dopamine D2
  • Tropanes
  • Receptor, Serotonin, 5-HT1A