Abstract
Migraine remains one of the most prevalent and disabling neurological disorders that often affects a person during their most productive years. Migraine afflicts approximately 11% of the adult population globally, causes substantial disability, which translates into lost productivity both at home and at work. Clearly there remains a need for new approaches to treat migraine and calcitonin gene-related peptide (CGRP) receptor antagonists have the potential to be a major advance in antimigraine therapy. CGRP was first proposed to play a role in migraine pathophysiology a little over 20 years ago and today there is considerable evidence that CGRP plays a key role in the pathogenesis of migraine. CGRP is a 37 amino acid vasoactive neuropeptide largely expressed in sensory neurons. It was observed that plasma levels of CGRP were elevated during the headache phase of migraine and the levels were normalized concomitantly with pain relief. This observation, along with other evidence, suggested that CGRP receptor antagonists might represent a novel approach to migraine treatment. The advent of small molecule CGRP receptor antagonists has clearly demonstrated a clinical link between blocking the CGRP receptor and effectiveness in treating migraine. This review will highlight the biology of CGRP as it pertains to migraine; discuss the CGRP receptor; spotlight the development of CGRP receptor antagonists; and examine site of action.
Keywords: Migraine, CGRP, CGRP receptor antagonist, neuropeptide, trigeminovascular, substantial disability, calcitonin gene-related peptide (CGRP), antimigraine therapy, vasoactive neuropeptide, sensory neurons, CGRP receptor antagonists, examine potential therapeutic utility
Current Pharmaceutical Biotechnology
Title: CGRP Receptor Antagonists: Toward a Novel Migraine Therapy
Volume: 12 Issue: 10
Author(s): C. A. Salvatore and S. A. Kane
Affiliation:
Keywords: Migraine, CGRP, CGRP receptor antagonist, neuropeptide, trigeminovascular, substantial disability, calcitonin gene-related peptide (CGRP), antimigraine therapy, vasoactive neuropeptide, sensory neurons, CGRP receptor antagonists, examine potential therapeutic utility
Abstract: Migraine remains one of the most prevalent and disabling neurological disorders that often affects a person during their most productive years. Migraine afflicts approximately 11% of the adult population globally, causes substantial disability, which translates into lost productivity both at home and at work. Clearly there remains a need for new approaches to treat migraine and calcitonin gene-related peptide (CGRP) receptor antagonists have the potential to be a major advance in antimigraine therapy. CGRP was first proposed to play a role in migraine pathophysiology a little over 20 years ago and today there is considerable evidence that CGRP plays a key role in the pathogenesis of migraine. CGRP is a 37 amino acid vasoactive neuropeptide largely expressed in sensory neurons. It was observed that plasma levels of CGRP were elevated during the headache phase of migraine and the levels were normalized concomitantly with pain relief. This observation, along with other evidence, suggested that CGRP receptor antagonists might represent a novel approach to migraine treatment. The advent of small molecule CGRP receptor antagonists has clearly demonstrated a clinical link between blocking the CGRP receptor and effectiveness in treating migraine. This review will highlight the biology of CGRP as it pertains to migraine; discuss the CGRP receptor; spotlight the development of CGRP receptor antagonists; and examine site of action.
Export Options
About this article
Cite this article as:
A. Salvatore C. and A. Kane S., CGRP Receptor Antagonists: Toward a Novel Migraine Therapy, Current Pharmaceutical Biotechnology 2011; 12 (10) . https://dx.doi.org/10.2174/138920111798357401
DOI https://dx.doi.org/10.2174/138920111798357401 |
Print ISSN 1389-2010 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4316 |
Call for Papers in Thematic Issues
Artificial Intelligence in Bioinformatics
Bioinformatics is an interdisciplinary field that analyzes and explores biological data. This field combines biology and information system. Artificial Intelligence (AI) has attracted great attention as it tries to replicate human intelligence. It has become common technology for analyzing and solving complex data and problems and encompasses sub-fields of machine ...read more
Latest Advancements in Biotherapeutics
The scope of this thematic issue is to comprehensively explore the rapidly evolving landscape of biotherapeutics, emphasizing breakthroughs in precision medicine. Encompassing diverse therapeutic modalities, the issue will delve into the latest developments in monoclonal antibodies, CRISPR/Cas gene editing, CAR-T cell therapies, and innovative drug delivery systems, such as nanoparticle-based ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Cytochrome P450-Activated Prodrugs: Targeted Drug Delivery
Current Medicinal Chemistry Dysregulation of RNA Mediated Gene Expression in Motor Neuron Diseases
CNS & Neurological Disorders - Drug Targets Recent Advances in Asthma Genetics and Antiasthma Therapy
Current Respiratory Medicine Reviews Transforming Growth Factor β Signaling Perturbation in the Loeys-Dietz Syndrome
Current Medicinal Chemistry Nonalcoholic Fatty Liver Disease: The Pathogenetic Roles of Insulin Resistance and Adipocytokines
Current Molecular Medicine Nicotine, Lung and Cancer
Anti-Cancer Agents in Medicinal Chemistry Neuroprotective Effects of Tetracyclines: Molecular Targets, Animal Models and Human Disease
CNS & Neurological Disorders - Drug Targets Lipid-Lowering Therapies for Atherosclerosis: Statins, Fibrates, Ezetimibe and PCSK9 Monoclonal Antibodies
Current Medicinal Chemistry The Many Roles of Chemokine Receptors in Neurodegenerative Disorders: Emerging New Therapeutical Strategies
Current Medicinal Chemistry Previously Apparently Undescribed Autosomal-Recessive Multiple Congenital Anomalies/ Mental Retardation (MCA/MR) Syndrome Comprising: Fronto-Nasal Dysplasia, Hypertelorism, Short Stature and Brachydactily
Current Pediatric Reviews Teratogenic Activity of HDAC Inhibitors
Current Pharmaceutical Design Tandem Mass Spectrometry Newborn Screening for Inborn Errors of Intermediary Metabolism: Abnormal Profile Interpretation
Current Medicinal Chemistry Flavonoids as Sirtuin Modulators
Current Topics in Medicinal Chemistry The Design of Vectors for RNAi Delivery System
Current Pharmaceutical Design Beyond Single Pathway Inhibition: MEK Inhibitors as a Platform for the Development of Pharmacological Combinations with Synergistic Anti-Leukemic Effects
Current Pharmaceutical Design Structure, Function, and Pathogenesis of SHP2 in Developmental Disorders and Tumorigenesis
Current Cancer Drug Targets Nose to Brain Delivery of Nanoformulations for Neurotherapeutics in Parkinson’s Disease: Defining the Preclinical, Clinical and Toxicity Issues
Current Drug Delivery Immunotoxins Constructed with Ribosome-Inactivating Proteins and their Enhancers: A Lethal Cocktail with Tumor Specific Efficacy
Current Pharmaceutical Design COVID-19, Angiotensin-Converting Enzyme 2 and Renin-Angiotensin System Inhibition: Implications for Practice
Current Hypertension Reviews Immunological Mechanism and Clinical Application of PAMP Adjuvants
Recent Patents on Anti-Cancer Drug Discovery