Anxiolytic-like profile of mirtazapine in rat conditioned fear stress model: Functional significance of 5-hydroxytryptamine 1A receptor and alpha1-adrenergic receptor

Pharmacol Biochem Behav. 2009 May;92(3):393-8. doi: 10.1016/j.pbb.2008.12.022. Epub 2009 Jan 11.

Abstract

Mirtazapine is an antidepressant with a unique mechanism of action and has been categorized as a Noradrenergic and Specific Serotonergic Antidepressant (NaSSA). Although numerous clinical trials suggested the usefulness of mirtazapine for not only major depressive disorders but also a variety of anxiety disorders, efficacy studies in animal anxiety models have been rarely reported. The present study investigated a potential anxiolytic-like profile of mirtazapine in rat conditioned fear stress model. A 5-hydroxytryptamine (5-HT) 1A receptor partial agonist, buspirone (1-5 mg/kg) exhibited a significant reduction in freezing time, and its maximal effect was reversed by a selective 5-HT(1A) antagonist, WAY-100635 (1 mg/kg). Mirtazapine (1-10 mg/kg) also reduced the freezing time in a dose-related fashion, a substantial proportion (approx. 50%) of which was likewise antagonized by WAY-100635 (1 mg/kg). Mianserin (1-30 mg/kg), a structural analogue for mirtazapine, was ineffective. Furthermore, co-administration of alpha1 adrenoceptor antagonist, prazosin (0.03 mg/kg) completely reversed mirtazapine (10 mg/kg)-induced reduction of freezing time. These findings represent the first demonstration that the anxiolytic-like action of mirtazapine involves activation of 5-HT(1A) receptor and alpha1 adrenoceptor to different extents, and are compatible with one aspect of mirtazapine's pharmacological profile as NaSSA.

MeSH terms

  • Adrenergic alpha-Antagonists / pharmacology*
  • Animals
  • Anti-Anxiety Agents / pharmacology*
  • Conditioning, Classical*
  • Fear*
  • Male
  • Mianserin / analogs & derivatives*
  • Mianserin / pharmacology
  • Mirtazapine
  • Prazosin / pharmacology
  • Rats
  • Rats, Sprague-Dawley
  • Receptor, Serotonin, 5-HT1A / physiology*
  • Receptors, Adrenergic, alpha-1 / physiology*

Substances

  • Adrenergic alpha-Antagonists
  • Anti-Anxiety Agents
  • Receptors, Adrenergic, alpha-1
  • Receptor, Serotonin, 5-HT1A
  • Mianserin
  • Mirtazapine
  • Prazosin