Hippocampal Bcl-2 expression is selectively increased following chronic but not acute treatment with antidepressants, 5-HT(1A) or 5-HT(2C/2B) receptor antagonists

Eur J Pharmacol. 2007 Aug 13;569(1-2):41-7. doi: 10.1016/j.ejphar.2007.05.006. Epub 2007 May 13.

Abstract

Expression of the anti-apoptotic protein Bcl-2 has been shown to increase in the hippocampus and cortex following chronic administration of mood stabilizers such as lithium and valproate, but the effects of long-term antidepressant administration have not been demonstrated. CD1 mice were dosed either acutely or chronically with either antidepressants or 5-HT receptor subtype selective antagonists. Cortex, hippocampus and hypothalamus from these mice were analysed by Western blot for changes in expression of Bcl-2 and Bax protein. Fourteen day but not acute treatment with citalopram (20 mg/kg), imipramine (10 mg/kg) and amitriptyline (10 mg/kg) in mice significantly elevated hippocampal Bcl-2 protein expression as compared to vehicle treated animals (59, 48 and 42% respectively). Similarly, fourteen day but not acute treatment with the 5-HT(1A) and 5-HT(2C/2B) receptor antagonists WAY100635 (0.3 mg/kg) and SB221284 (1 mg/kg) also markedly and significantly increased hippocampal Bcl-2 expression (95 and 52% respectively). Bcl-2 expression was unaffected in cortex by any treatment. There was a smaller increase of hippocampal Bax protein levels following treatment with imipramine after 1 or 14 days, and following citalopram and amitriptyline after 14 but not 1 day. These data present the first substantive evidence that clinically used antidepressants increase the expression of hippocampal Bcl-2 as did chronic blockade of 5-HT(1A) and 5-HT(2C/2B) receptors, which may be involved in the mechanism of action of antidepressants. The induction of hippocampal Bcl-2 expression by long-term antidepressant treatment may contribute to the clinical efficacy of such compounds via its well described neurotrophic and/or anti-apoptotic effects on neuronal function.

MeSH terms

  • Amitriptyline / pharmacology
  • Analysis of Variance
  • Animals
  • Antidepressive Agents / pharmacology*
  • Antidepressive Agents, Second-Generation / pharmacology
  • Antidepressive Agents, Tricyclic / pharmacology
  • Apoptosis / drug effects
  • Blotting, Western
  • Citalopram / pharmacology
  • Fluorobenzenes / pharmacology
  • Hippocampus / drug effects*
  • Hippocampus / metabolism
  • Imipramine / pharmacology
  • Indoles / pharmacology
  • Male
  • Mice
  • Piperazines / pharmacology
  • Piperidines / pharmacology
  • Proto-Oncogene Proteins c-bcl-2 / metabolism*
  • Pyridines / pharmacology
  • Selective Serotonin Reuptake Inhibitors / pharmacology
  • Serotonin 5-HT1 Receptor Antagonists
  • Serotonin 5-HT2 Receptor Antagonists
  • Serotonin Antagonists / pharmacology*
  • Sulfonamides / pharmacology
  • bcl-2-Associated X Protein / metabolism

Substances

  • 3,N-dimethyl-N-(1-methyl-3-(4-methylpiperidin-1-yl)propyl)benzenesulfonamide
  • Antidepressive Agents
  • Antidepressive Agents, Second-Generation
  • Antidepressive Agents, Tricyclic
  • Bax protein, mouse
  • Fluorobenzenes
  • Indoles
  • Piperazines
  • Piperidines
  • Proto-Oncogene Proteins c-bcl-2
  • Pyridines
  • SB 221284
  • Serotonin 5-HT1 Receptor Antagonists
  • Serotonin 5-HT2 Receptor Antagonists
  • Serotonin Antagonists
  • Serotonin Uptake Inhibitors
  • Sulfonamides
  • bcl-2-Associated X Protein
  • Citalopram
  • Amitriptyline
  • N-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-N-(2-pyridinyl)cyclohexanecarboxamide
  • volinanserin
  • Imipramine