Arsenic decreases antinociceptive activity of paracetamol: possible involvement of serotonergic and endocannabinoid receptors

Environ Toxicol Pharmacol. 2014 Sep;38(2):397-405. doi: 10.1016/j.etap.2014.07.001. Epub 2014 Jul 10.

Abstract

We assessed whether repeated arsenic exposure can decrease paracetamol-mediated antinociception by modulating serotonergic and endocannabinoid pathways. Rats were preexposed to elemental arsenic (4ppm) as sodium arsenite through drinking water for 28 days. Next day paracetamol's (400mg/kg, oral) antinociceptive activity was assessed through formalin-induced nociception. Serotonin content and gene expression of 5-HT1A, 5-HT2A and CB1 receptors were evaluated in brainstem and frontal cortex. Arsenic decreased paracetamol-mediated analgesia. Paracetamol, but not arsenic, increased serotonin content in these regions. Arsenic attenuated paracetamol-mediated increase in serotonin level. Paracetamol did not alter 5-HT1A expression, but caused down-regulation of 5-HT2A and up-regulation of CB1 receptors. Arsenic down-regulated these receptors. However, paracetamol-mediated down-regulation of 5-HT2A was more pronounced. Arsenic did not modify paracetamol's effect on 5-HT1A expression, but reduced paracetamol-mediated down-regulation of 5-HT2A and reversed up-regulation of CB1 receptors. Results suggest arsenic reduced paracetamol-induced analgesia possibly by interfering with pronociceptive 5-HT2A and antinociceptive CB1 receptors.

Keywords: 5-HT receptors, CB(1) receptor; Antinociception; Arsenic; Paracetamol; Rat.

MeSH terms

  • Acetaminophen / administration & dosage*
  • Acetaminophen / pharmacology
  • Analgesics / administration & dosage*
  • Analgesics / pharmacology
  • Animals
  • Arsenites / toxicity*
  • Brain Stem / metabolism
  • Drinking Water / chemistry*
  • Drug Interactions
  • Frontal Lobe / metabolism
  • Gene Expression Regulation / drug effects
  • Rats
  • Rats, Wistar
  • Receptor, Cannabinoid, CB1 / genetics
  • Receptor, Cannabinoid, CB1 / metabolism*
  • Receptors, Serotonin / genetics
  • Receptors, Serotonin / metabolism*
  • Sodium Compounds / toxicity*
  • Water Pollutants, Chemical / toxicity*

Substances

  • Analgesics
  • Arsenites
  • Drinking Water
  • Receptor, Cannabinoid, CB1
  • Receptors, Serotonin
  • Sodium Compounds
  • Water Pollutants, Chemical
  • Acetaminophen
  • sodium arsenite