5-HT2C receptor activation prevents stress-induced enhancement of brain 5-HT turnover and extracellular levels in the mouse brain: modulation by chronic paroxetine treatment

J Neurochem. 2010 Oct;115(2):438-49. doi: 10.1111/j.1471-4159.2010.06932.x. Epub 2010 Aug 25.

Abstract

Stress is known to activate the central 5-hydroxytryptamine (5-HT) system, and this is probably part of a coping response involving several 5-HT receptors. Although 5-HT(2C) receptors are well known to be implicated in anxiety, their participation in stress-induced changes had not been investigated in parallel at both behavioral and neurochemical levels. We show here that the preferential 5-HT(2C) receptor agonist, m-chlorophenylpiperazine, as well as restraint stress increased anxiety in the mouse social interaction test. The selective 5-HT(2C) receptor antagonist, SB 242,084, prevented both of these anxiogenic effects. Restraint stress increased 5-HT turnover in various brain areas, and this effect was prevented by the 5-HT(2B/2C) receptor agonist RO 60-0175 (1 mg/kg), but not the preferential 5-HT(2A) agonist 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (1 mg/kg), and in contrast potentiated by SB 242,084 (1 mg/kg), which also blocked the effect of RO 60-0175. Using microdialysis, RO 60-0175 was shown to inhibit cortical 5-HT overflow in stressed mice when 5-HT reuptake was blocked locally. Chronic paroxetine prevented both the anxiogenic effect of m-chlorophenylpiperazine and the inhibitory effect of RO 60-0175 on locomotion and stress-induced increase in 5-HT turnover. The anxiolytic action of chronic paroxetine might be associated with an enhancement of 5-HT neurotransmission caused by a decreased 5-HT(2C) receptor-mediated inhibition of stress-induced increase in 5-HT release.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amphetamines / pharmacology
  • Analysis of Variance
  • Animals
  • Antidepressive Agents, Second-Generation / pharmacology*
  • Behavior, Animal
  • Brain / drug effects*
  • Brain / metabolism
  • Ethylamines / pharmacology
  • Extracellular Fluid / drug effects
  • Gene Expression Regulation / drug effects
  • Indoles / pharmacology
  • Interpersonal Relations
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Motor Activity / drug effects
  • Paroxetine / pharmacology*
  • Piperazines / pharmacology
  • Receptor, Serotonin, 5-HT2C / metabolism*
  • Serotonin / metabolism*
  • Serotonin Receptor Agonists / pharmacology
  • Stress, Psychological* / drug therapy
  • Stress, Psychological* / metabolism
  • Stress, Psychological* / pathology

Substances

  • Amphetamines
  • Antidepressive Agents, Second-Generation
  • Ethylamines
  • Indoles
  • Piperazines
  • Receptor, Serotonin, 5-HT2C
  • Ro 60-0175
  • Serotonin Receptor Agonists
  • Serotonin
  • Paroxetine
  • 4-iodo-2,5-dimethoxyphenylisopropylamine
  • 1-(3-chlorophenyl)piperazine