Pain pharmacology in migraine: focus on CGRP and CGRP receptors.
Over the last 100 years, the discovery of new analgesics has been a complex and difficult task. However, remarkable progress in the identification of novel molecular targets relevant for pain medicines has been reported. Here we will focus on the neuropeptide calcitonin generelated peptide (CGRP) and its receptors (CGRP-R) because of their role in migraine mechanism and migraine therapy. Recent preclinical and clinical data on the localisation, regulation and plasma levels of CGRP and on the function of CGRP-R will be summarised. The reviewed findings highlight the major function of CGRP in migraine and the use of CGRP-R antagonists as a novel approach for the treatment of migraine attack and, perhaps, as migraine prophylactic medicines.
Benemei
S
S
Clinical Pharmacology Unit, Department of Critical Care Medicine and Surgery, University of Florence, Italy.
Nicoletti
P
P
Capone
J A
JA
Geppetti
P
P
D000818:Animals; D015740:Calcitonin Gene-Related Peptide / Q000031:analogs & derivatives / Q000037:antagonists & inhibitors / Q000378:metabolism*; D000077221:Calcitonin Gene-Related Peptide Receptor Antagonists; D002536:Cerebral Arteries / Q000294:innervation / Q000503:physiopathology*; D006801:Humans; D008881:Migraine Disorders / Q000188:drug therapy* / Q000378:metabolism / Q000503:physiopathology*; D009420:Nervous System / Q000187:drug effects / Q000378:metabolism / Q000503:physiopathology*; D009475:Neurons, Afferent / Q000187:drug effects / Q000378:metabolism*; D009619:Nociceptors / Q000187:drug effects / Q000378:metabolism; D010879:Piperazines / Q000494:pharmacology / Q000627:therapeutic use; D011799:Quinazolines / Q000494:pharmacology / Q000627:therapeutic use; D018015:Receptors, Calcitonin Gene-Related Peptide / Q000378:metabolism*; D014664:Vasodilation / Q000187:drug effects / Q000502:physiology*
D000077221:Calcitonin Gene-Related Peptide Receptor Antagonists; D010879:Piperazines; D011799:Quinazolines; D018015:Receptors, Calcitonin Gene-Related Peptide; D015740:Calcitonin Gene-Related Peptide; C406305:olcegepant