Effects of CGRP receptor antagonism in nitroglycerin-induced hyperalgesia

Cephalalgia. 2014 Jul;34(8):594-604. doi: 10.1177/0333102413517776. Epub 2013 Dec 23.

Abstract

Background: The release of calcitonin gene-related peptide (CGRP) from trigeminal nerves plays a central role in the pathophysiology of migraine and clinical evidence shows an antimigraine effect for CGRP receptor antagonists. Systemic administration of nitroglycerin (NTG), a nitrovasodilator, consistently provokes spontaneous-like migraine attacks in migraine sufferers; in the rat, systemic NTG induces a condition of hyperalgesia, probably through the activation of cerebral/spinal structures involved in nociceptive transmission.

Aim: The aim of this article is to test the analgesic effect of the CGRP receptor antagonist MK-8825 in two animal models of pain that may be relevant for migraine: the tail flick test and the formalin test performed during NTG-induced hyperalgesia.

Results: MK-8825 showed analgesic activity when administered alone at both the tail flick test and the formalin test. Furthermore, the CGRP antagonist proved effective in counteracting NTG-induced hyperalgesia in both tests. MK-8825 indeed reduced the nociceptive behavior when administered either simultaneously or prior to (30-60 minutes before) NTG.

Conclusion: These data suggest that MK-8825 may represent a potential therapeutic tool for the treatment of migraine.

Keywords: CGRP receptor antagonist; Nitroglycerin; hyperalgesia; migraine.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Calcitonin Gene-Related Peptide Receptor Antagonists*
  • Disease Models, Animal*
  • Hyperalgesia / chemically induced*
  • Hyperalgesia / physiopathology*
  • Male
  • Migraine Disorders / physiopathology*
  • Nitroglycerin / pharmacology*
  • Nociceptors / drug effects
  • Nociceptors / physiology
  • Pain Threshold / drug effects
  • Pain Threshold / physiology
  • Pyridines / pharmacology*
  • Rats
  • Rats, Sprague-Dawley
  • Reaction Time / drug effects
  • Spiro Compounds / pharmacology*

Substances

  • Calcitonin Gene-Related Peptide Receptor Antagonists
  • MK-8825
  • Pyridines
  • Spiro Compounds
  • Nitroglycerin