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Possible sites of action of the new calcitonin gene-related peptide receptor antagonists.

Eftekhari, Sajedeh LU and Edvinsson, Lars LU (2010) In Therapeutic Advances in Neurological Disorders 3(6). p.369-378
Abstract
Migraine is considered a neurovascular disease affecting more than 10% of the general population. Currently available drugs for the acute treatment of migraine are vasoconstrictors, which have limitations in their therapeutic use. The calcitonin gene-related peptide (CGRP) has a key role in migraine, where levels of CGRP are increased during acute migraine attacks. CGRP is expressed throughout the central and peripheral nervous system, consistent with control of vasodilatation and transmission of nociceptive information. In migraine, CGRP is released from the trigeminal system. At peripheral synapses CGRP results in vasodilatation via receptors on the smooth muscle cells. At central synapses, CGRP acts postjunctionally on second-order... (More)
Migraine is considered a neurovascular disease affecting more than 10% of the general population. Currently available drugs for the acute treatment of migraine are vasoconstrictors, which have limitations in their therapeutic use. The calcitonin gene-related peptide (CGRP) has a key role in migraine, where levels of CGRP are increased during acute migraine attacks. CGRP is expressed throughout the central and peripheral nervous system, consistent with control of vasodilatation and transmission of nociceptive information. In migraine, CGRP is released from the trigeminal system. At peripheral synapses CGRP results in vasodilatation via receptors on the smooth muscle cells. At central synapses, CGRP acts postjunctionally on second-order neurons to transmit pain centrally via the brainstem and midbrain to higher cortical pain regions. The recently developed CGRP-receptor antagonists have demonstrated clinical efficacy in the treatment of acute migraine attacks. A remaining question is their site of action. The CGRP-receptor components (calcitonin receptor-like receptor, receptor activity modifying protein 1 and receptor component protein) are found to colocalize in the smooth muscle cells of intracranial arteries and in large-sized neurons in the trigeminal ganglion. The CGRP receptor has also been localized within parts of the brain and the brainstem. The aim of this paper is to review recent localization studies of CGRP and its receptor components within the nervous system and to discuss whether these sites could be possible targets for the CGRP-receptor antagonists. (Less)
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publishing date
type
Contribution to journal
publication status
published
subject
in
Therapeutic Advances in Neurological Disorders
volume
3
issue
6
pages
369 - 378
publisher
SAGE Publications
external identifiers
  • pmid:21179597
  • scopus:78649940547
  • pmid:21179597
ISSN
1756-2864
DOI
10.1177/1756285610388343
language
English
LU publication?
yes
id
67dc6b0c-4a76-4285-bb3c-924beb4f0722 (old id 1755855)
alternative location
http://www.ncbi.nlm.nih.gov/pubmed/21179597?dopt=Abstract
date added to LUP
2016-04-04 09:23:14
date last changed
2024-10-13 01:01:03
@article{67dc6b0c-4a76-4285-bb3c-924beb4f0722,
  abstract     = {{Migraine is considered a neurovascular disease affecting more than 10% of the general population. Currently available drugs for the acute treatment of migraine are vasoconstrictors, which have limitations in their therapeutic use. The calcitonin gene-related peptide (CGRP) has a key role in migraine, where levels of CGRP are increased during acute migraine attacks. CGRP is expressed throughout the central and peripheral nervous system, consistent with control of vasodilatation and transmission of nociceptive information. In migraine, CGRP is released from the trigeminal system. At peripheral synapses CGRP results in vasodilatation via receptors on the smooth muscle cells. At central synapses, CGRP acts postjunctionally on second-order neurons to transmit pain centrally via the brainstem and midbrain to higher cortical pain regions. The recently developed CGRP-receptor antagonists have demonstrated clinical efficacy in the treatment of acute migraine attacks. A remaining question is their site of action. The CGRP-receptor components (calcitonin receptor-like receptor, receptor activity modifying protein 1 and receptor component protein) are found to colocalize in the smooth muscle cells of intracranial arteries and in large-sized neurons in the trigeminal ganglion. The CGRP receptor has also been localized within parts of the brain and the brainstem. The aim of this paper is to review recent localization studies of CGRP and its receptor components within the nervous system and to discuss whether these sites could be possible targets for the CGRP-receptor antagonists.}},
  author       = {{Eftekhari, Sajedeh and Edvinsson, Lars}},
  issn         = {{1756-2864}},
  language     = {{eng}},
  number       = {{6}},
  pages        = {{369--378}},
  publisher    = {{SAGE Publications}},
  series       = {{Therapeutic Advances in Neurological Disorders}},
  title        = {{Possible sites of action of the new calcitonin gene-related peptide receptor antagonists.}},
  url          = {{http://dx.doi.org/10.1177/1756285610388343}},
  doi          = {{10.1177/1756285610388343}},
  volume       = {{3}},
  year         = {{2010}},
}