Abstract
Management of pain is an essential aspect of medicine; however, current therapies are frequently insufficient owing to severe side effects or limited effectiveness. Therefore, the discovery of new analgesics is needed, especially to treat the proportion of painful patients poorly improved by available analgesics. The transmission of nociceptive stimuli in primary afferent neurons critically depends on a peculiar repertoire of various types of ion channels such as a number of TRP channels, persistent sodium channels, inwardly rectifying potassium channels and voltage-gated calcium channels that either detect noxious stimuli, or regulate cellular excitability and synaptic transmission. Moreover, some of these channels are redistributed and upregulated in pathological states leading to abnormal detection or transmission of harmful stimuli, and consequently lead to states of chronic pain. Hence, these channels are considered key targets for the development of analgesics. The nervous system expresses multiple types of calcium channels with specialized roles in neurophysiology. Here, we review the role of these channels and their accessory subunits in nociceptive signaling, and their potential as targets for development of innovative analgesics.
Keywords: n-type channel, t-type channel, opioid receptors, nociception, prialt, gabapentin, neurontin, lyrica, nociceptin receptors
Current Topics in Medicinal Chemistry
Title: Voltage Gated Calcium Channels as Targets for Analgesics
Volume: 5 Issue: 6
Author(s): Emmanuel Bourinet and Gerald W. Zamponi
Affiliation:
Keywords: n-type channel, t-type channel, opioid receptors, nociception, prialt, gabapentin, neurontin, lyrica, nociceptin receptors
Abstract: Management of pain is an essential aspect of medicine; however, current therapies are frequently insufficient owing to severe side effects or limited effectiveness. Therefore, the discovery of new analgesics is needed, especially to treat the proportion of painful patients poorly improved by available analgesics. The transmission of nociceptive stimuli in primary afferent neurons critically depends on a peculiar repertoire of various types of ion channels such as a number of TRP channels, persistent sodium channels, inwardly rectifying potassium channels and voltage-gated calcium channels that either detect noxious stimuli, or regulate cellular excitability and synaptic transmission. Moreover, some of these channels are redistributed and upregulated in pathological states leading to abnormal detection or transmission of harmful stimuli, and consequently lead to states of chronic pain. Hence, these channels are considered key targets for the development of analgesics. The nervous system expresses multiple types of calcium channels with specialized roles in neurophysiology. Here, we review the role of these channels and their accessory subunits in nociceptive signaling, and their potential as targets for development of innovative analgesics.
Export Options
About this article
Cite this article as:
Emmanuel Bourinet and Gerald W. Zamponi , Voltage Gated Calcium Channels as Targets for Analgesics, Current Topics in Medicinal Chemistry 2005; 5 (6) . https://dx.doi.org/10.2174/1568026054367610
DOI https://dx.doi.org/10.2174/1568026054367610 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
Adaptogens—History and Future Perspectives
Adaptogens are pharmacologically active compounds or plant extracts that are associated with the ability to enhance the body’s stability against stress. The intake of adaptogens is associated not only with a better ability to adapt to stress and maintain or normalise metabolic functions but also with better mental and physical ...read more
AlphaFold in Medicinal Chemistry: Opportunities and Challenges
AlphaFold, a groundbreaking AI tool for protein structure prediction, is revolutionizing drug discovery. Its near-atomic accuracy unlocks new avenues for designing targeted drugs and performing efficient virtual screening. However, AlphaFold's static predictions lack the dynamic nature of proteins, crucial for understanding drug action. This is especially true for multi-domain proteins, ...read more
Artificial intelligence for Natural Products Discovery and Development
Our approach involves using computational methods to predict the potential therapeutic benefits of natural products by considering factors such as drug structure, targets, and interactions. We also employ multitarget analysis to understand the role of drug targets in disease pathways. We advocate for the use of artificial intelligence in predicting ...read more
Chemistry Based on Natural Products for Therapeutic Purposes
The development of new pharmaceuticals for a wide range of medical conditions has long relied on the identification of promising natural products (NPs). There are over sixty percent of cancer, infectious illness, and CNS disease medications that include an NP pharmacophore, according to the Food and Drug Administration. Since NP ...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
- Announcements
Related Articles
-
Epigenetic Targets and their Inhibitors in Cancer Therapy
Current Topics in Medicinal Chemistry Anticancer Therapeutic Strategies Based on CDK Inhibitors
Current Pharmaceutical Design Gene Therapy in Plastic and Reconstructive Surgery
Current Gene Therapy Developmental and Biological Insights Obtained from Gene Expression Profiling of the Nematode Caenorhabditis Elegans
Current Genomics Seeing Genes at Work in the Living Brain with Non-Invasive Molecular Imaging
Current Gene Therapy Prostate Cancer, miRNAs, Metallothioneins and Resistance to Cytostatic Drugs
Current Medicinal Chemistry Unraveling Potential Candidate Targets Associated with Expression of p16<sup>INK4a</sup> or p16 Truncated Fragment by Comparative Proteomics Analysis
Current Proteomics Genome and Transcriptome Analysis of Neuroblastoma Advanced Diagnosis from Innovative Therapies
Current Pharmaceutical Design The Need for Calcium Channels in Cell Proliferation
Recent Patents on Anti-Cancer Drug Discovery Cyclin Dependent Kinase as Significant Target for Cancer Treatment
Current Cancer Therapy Reviews Advances in the Management of Brain Tumors in Infants
Current Cancer Therapy Reviews Nonviral Vectors for Cancer Gene Therapy: Prospects for Integrating Vectors and Combination Therapies
Current Gene Therapy Prodrug Strategies in Ocular Drug Delivery
Medicinal Chemistry Towards Cure of CML: Why We Need to Know More About CML Stem Cells?
Current Stem Cell Research & Therapy Targeting the L-Arginine-Nitric Oxide Pathway for Cancer Treatment
Current Pharmaceutical Design Type 2 Transglutaminase in Neurodegenerative Diseases: The Mitochondrial Connection
Current Pharmaceutical Design Evolution of Resistance to Cancer Therapy
Current Pharmaceutical Design Survivin as a Prognostic/Predictive Marker and Molecular Target in Cancer Therapy
Current Medicinal Chemistry iNOS: A Potential Therapeutic Target for Malignant Glioma
Current Molecular Medicine Cancer Metastasis as Disrupted Developmental Phenotype
Current Genomics