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CGRP Receptor Antagonists for Migraine: Challenges and Promises

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The calcitonin gene-related peptide family

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Abstract

Migraine headache is one of the most prevalent neurological disorders afflicting approximately 11% of the global adult population. The last decade has seen advancements in migraine treatment with the introduction of the triptans. However, some patients do not respond optimally to triptans and many only partially respond. Clearly there remains a need for new approaches to treat migraineurs which offer improved safety and sustained efficacy. The neuropeptide calcitonin gene-related peptide (CGRP) has long been postulated as an attractive target for the development of novel antimigraine therapies. Although a complete understanding of the pathogenic role of CGRP in migraine is still unknown, recent clinical studies involving antagonism of the CGRP receptor clearly demonstrated there is a correlation between the function of CGRP and migraine headache. CGRP receptor antagonists have the potential to be a major advance in antimigraine therapy and continued evaluation in larger clinical studies are necessary to characterize fully the clinical potential of this new class of molecules.

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Abbreviations

CGRP:

calcitonin gene-related peptide

VIP:

vasoactive intestinal peptide

AM:

adrenomedullin

GPCR:

G protein-coupled receptor

RAM:

Preceptor activity-modifying protein

CL:

calcitonin receptor-like

R:

receptor

RCP:

receptor component protein

DBF:

dermal microvascular blood flow

PK/PD:

pharmacokinetic/pharmacodynamic

CIDV:

capsaicin-induced dermal vasodilation

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Authors and Affiliations

  1. Department of Pain & Migraine Research, Merck Research Laboratories, WP26A-2000, West Point, PA, USA

    Christopher A. Salvatore & Stefanie A. Kane

Authors
  1. Christopher A. Salvatore
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  2. Stefanie A. Kane
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Correspondence to Christopher A. Salvatore .

Editor information

Editors and Affiliations

  1. School of Biological Sciences, University of Auckland, Symonds St. 9, Auckland , 1142, New Zealand

    Deborah L. Hay

  2. University of Auckland, Symonds Street 3A, Auckland, 1142, New Zealand

    Ian M. Dickerson

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Salvatore, C.A., Kane, S.A. (2010). CGRP Receptor Antagonists for Migraine: Challenges and Promises. In: Hay, D., Dickerson, I. (eds) The calcitonin gene-related peptide family. Springer, Dordrecht. https://doi.org/10.1007/978-90-481-2909-6_12

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