New therapeutic target in primary headaches - blocking theCGRP receptor

56 Citations (Scopus)


The primary headaches are among the most prevalent neurological disorders, afflicting up to 16% of the adult population. The associated pain originates from intracranial blood vessels that are innervated by sensory nerves storing several neurotransmitters. In primary headaches, there is a clear association between the headache and the release of calcitonin gene-related peptide (CGRP), but not other neuronal messengers. The specific purpose of this review is to describe CGRP in the human cranial circulation and to elucidate a possible role for a specific antagonist in the treatment of primary headaches. Acute treatment with administration of a 5-HT(1B/1D) agonist (triptan) results in alleviation of the headache and normalisation of the CGRP level. The mechanism of action of triptans involves vasoconstriction of intracranial vessels and a presynaptic inhibitory effect of sensory nerves. The central role of CGRP in migraine and cluster headache pathophysiology has led to the search for small-molecule CGRP antagonists, which are predicted to have fewer cardiovascular side effects in comparison to the triptans. The initial pharmacological profile of such a group of compounds has recently been disclosed. These compounds have high selectivity for human CGRP receptors and are reportedly efficacious in the relief of acute attacks of migraine.

Original languageEnglish
JournalExpert Opinion on Therapeutic Targets
Issue number3
Pages (from-to)377-83
Number of pages7
Publication statusPublished - Jun 2003
Externally publishedYes


  • Adolescent
  • Adult
  • Analgesics, Non-Narcotic
  • Animals
  • Calcitonin
  • Child
  • Clinical Trials as Topic
  • Drug Evaluation, Preclinical
  • Headache
  • Humans
  • Migraine Disorders
  • Neurotransmitter Agents
  • Piperazines
  • Protein Precursors
  • Quinazolines
  • Rats
  • Receptors, Calcitonin Gene-Related Peptide
  • Signal Transduction
  • Trigeminal Nerve
  • Vasodilation


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