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Novel migraine therapy with calcitonin gene-regulated peptide receptor antagonists

Edvinsson, Lars LU (2007) In Expert Opinion on Therapeutic Targets 11(9). p.1179-1188
Abstract
Primary headaches, for example, migraine and cluster headaches represent the most prevalent neurological disorders, affecting up to 15 - 20% of the adult population. There is a clear association between head pain and the release of calcitonin gene-related peptide (CGRP). In this review the role of CGRP in human cranial circulation is described and the role for specific CGRP antagonism elucidated. It is well known that triptans (5-HT1B/1D agonist) alleviate headache in part through normalisation of CGRP levels. The central role of CGRP in migraine pathophysiology has resulted in the development of small-molecule CGRP antagonists with no cardiovascular side effects. Such compounds have high selectivity for human CGRP receptors and are... (More)
Primary headaches, for example, migraine and cluster headaches represent the most prevalent neurological disorders, affecting up to 15 - 20% of the adult population. There is a clear association between head pain and the release of calcitonin gene-related peptide (CGRP). In this review the role of CGRP in human cranial circulation is described and the role for specific CGRP antagonism elucidated. It is well known that triptans (5-HT1B/1D agonist) alleviate headache in part through normalisation of CGRP levels. The central role of CGRP in migraine pathophysiology has resulted in the development of small-molecule CGRP antagonists with no cardiovascular side effects. Such compounds have high selectivity for human CGRP receptors and are efficacious in the relief of acute migraine attacks. Research indicates that they effect the abluminal side of the blood-brain barrier and that they are not vasoconstrictive, providing a new dimension in therapy. (Less)
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author
organization
publishing date
type
Contribution to journal
publication status
published
subject
keywords
reflex, VIP, trigeminovascular, migraine, cluster headache, CGRP, CGRP blocker
in
Expert Opinion on Therapeutic Targets
volume
11
issue
9
pages
1179 - 1188
publisher
Ashley Publications
external identifiers
  • wos:000249857100005
  • scopus:34548834456
ISSN
1472-8222
DOI
10.1517/14728222.11.9.1179
language
English
LU publication?
yes
id
4555182f-b3eb-4133-9f7a-da9f4415b4b2 (old id 656145)
date added to LUP
2007-12-06 11:45:18
date last changed
2017-01-01 04:36:40
@article{4555182f-b3eb-4133-9f7a-da9f4415b4b2,
  abstract     = {Primary headaches, for example, migraine and cluster headaches represent the most prevalent neurological disorders, affecting up to 15 - 20% of the adult population. There is a clear association between head pain and the release of calcitonin gene-related peptide (CGRP). In this review the role of CGRP in human cranial circulation is described and the role for specific CGRP antagonism elucidated. It is well known that triptans (5-HT1B/1D agonist) alleviate headache in part through normalisation of CGRP levels. The central role of CGRP in migraine pathophysiology has resulted in the development of small-molecule CGRP antagonists with no cardiovascular side effects. Such compounds have high selectivity for human CGRP receptors and are efficacious in the relief of acute migraine attacks. Research indicates that they effect the abluminal side of the blood-brain barrier and that they are not vasoconstrictive, providing a new dimension in therapy.},
  author       = {Edvinsson, Lars},
  issn         = {1472-8222},
  keyword      = {reflex,VIP,trigeminovascular,migraine,cluster headache,CGRP,CGRP blocker},
  language     = {eng},
  number       = {9},
  pages        = {1179--1188},
  publisher    = {Ashley Publications},
  series       = {Expert Opinion on Therapeutic Targets},
  title        = {Novel migraine therapy with calcitonin gene-regulated peptide receptor antagonists},
  url          = {http://dx.doi.org/10.1517/14728222.11.9.1179},
  volume       = {11},
  year         = {2007},
}