5-HT1A agonist alleviates serotonergic potentiation of extrapyramidal disorders via postsynaptic mechanisms

Prog Neuropsychopharmacol Biol Psychiatry. 2013 Oct 1:46:86-91. doi: 10.1016/j.pnpbp.2013.06.016. Epub 2013 Jul 6.

Abstract

We previously demonstrated that 5-HT stimulants, including selective serotonin reuptake inhibitors (SSRIs), potentiated antipsychotic-induced extrapyramidal symptoms (EPS) by stimulating 5-HT2A/2C, 5-HT3 and 5-HT6 receptors. Here, we studied the effects of the 5-HT1A agonist (±)-8-hydroxy-2-(di-n-propylamino) tetralin ((±)-8-OH-DPAT) on the fluoxetine enhancement of EPS (i.e., bradykinesia and catalepsy) to determine if the 5-HT1A agonist can counteract the serotonergic potentiation of EPS. Fluoxetine did not induce EPS signs by itself, but significantly potentiated haloperidol-induced bradykinesia in mice. (±)-8-OH-DPAT (0.1-1mg/kg, i.p.) significantly attenuated the fluoxetine enhancement of haloperidol-induced bradykinesia in a dose-dependent manner. A selective 5-HT1A antagonist (s)-WAY-100135 completely reversed the anti-EPS action of (±)-8-OH-DPAT. Microinjection studies using rats revealed that local application of (±)-8-OH-DPAT into the dorsolateral striatum or the motor cortex significantly diminished fluoxetine-enhanced catalepsy. In contrast, (±)-8-OH-DPAT injected into the medial raphe nucleus failed to affect EPS induction. The present results illustrate that 5-HT1A agonist can alleviate the SSRI enhancement of EPS by activating postsynaptic 5-HT1A receptors in the striatum and cerebral cortex.

Keywords: (±)-8-OH-DPAT; (±)-8-hydroxy-2-(di-n-propylamino) tetralin; 5-HT(1A) agonists; Antidepressants; Antipsychotics; EPS; Extrapyramidal symptoms; MC; MRN; Microinjection; SGA; SSRI; Selective serotonin reuptake inhibitor (SSRI); dlST; dorsolateral striatum; extrapyramidal symptoms; medial raphe nucleus; motor cortex; second generation antipsychotic; selective serotonin reuptake inhibitor.

MeSH terms

  • Animals
  • Basal Ganglia Diseases / drug therapy*
  • Basal Ganglia Diseases / metabolism*
  • Brain / drug effects
  • Brain / metabolism
  • Male
  • Mice
  • Microinjections / methods
  • Rats
  • Rats, Sprague-Dawley
  • Receptor, Serotonin, 5-HT1A / metabolism*
  • Serotonin 5-HT1 Receptor Agonists / administration & dosage*
  • Serotonin 5-HT1 Receptor Antagonists / administration & dosage

Substances

  • Serotonin 5-HT1 Receptor Agonists
  • Serotonin 5-HT1 Receptor Antagonists
  • Receptor, Serotonin, 5-HT1A