The μ1-opioid receptor and 5-HT2A- and 5HT2C-serotonergic receptors of the locus coeruleus are critical in elaborating hypoalgesia induced by tonic and tonic-clonic seizures

Neuroscience. 2016 Nov 12:336:133-145. doi: 10.1016/j.neuroscience.2016.08.040. Epub 2016 Sep 4.

Abstract

It has been proposed that the post-ictal state is associated with the expression of hypoalgesia. It is clear that the projections among the periaqueductal gray matter (PAG), dorsal raphe nucleus (DRN) and locus coeruleus (LC) play a role in pain management. These mesencephalic structures have direct reciprocal opioid and monoaminergic projections to the LC that can possibly modulate post-ictal hypoalgesia. The goal of this study was to examine if LC-opioid and serotonergic/noradrenergic mechanisms signal the post-ictal hypoalgesic responses to tonic-clonic seizures produced by intraperitoneal administration of pentylenetetrazole (PTZ at 64mg/kg), causing an ionophore γ-aminobutyric acid (GABA)-mediated Cl- influx antagonism. The rodents' nociceptive threshold was measured by the tail-flick test. Intra-LC cobalt chloride (1.0nM/0.2μL) microinjections produced intermittent local synaptic inhibition and were able to reduce post-ictal hypoalgesia. Central administration of naltrexone (a non-selective antagonist for opioid receptors), naloxonazine (a selective antagonist for μ1-opioid-receptors), methysergide (a non-selective antagonist for serotonergic receptors) or ketanserin (an antagonist for both α1-noradrenergic and 5-Hydroxytryptamine(HT)2A/2C receptors) at 5.0μg/0.2μL, R-96544 (a 5-HT2A receptor selective antagonist) at 10nM/0.2μL, or RS-102221 (a 5-HT2C receptor selective antagonist) at 0.15μg/0.2μL into the LC also decreased post-ictal hypoalgesia. The data presented here suggest that the post-ictal antinociception mechanism involves the μ1-opiod, 5-HT2A- and 5-HT2C-serotonergic, and α1-noradrenergic receptors in the LC.

Keywords: 5-HT(2A)- and 5-HT(2C)-serotonergic receptors; GABA-A receptor; locus coeruleus; post-ictal antinociception; α(1)-noradrenergic receptors; μ(1)-opiod receptors.

MeSH terms

  • Animals
  • Locus Coeruleus / physiopathology*
  • Male
  • Pain Threshold / physiology
  • Pentylenetetrazole / pharmacology
  • Rats, Wistar
  • Receptor, Serotonin, 5-HT2A / metabolism*
  • Receptor, Serotonin, 5-HT2C / metabolism*
  • Receptors, Opioid, mu / metabolism*
  • Seizures / chemically induced
  • Seizures / physiopathology*

Substances

  • Receptor, Serotonin, 5-HT2A
  • Receptor, Serotonin, 5-HT2C
  • Receptors, Opioid, mu
  • Pentylenetetrazole