Abstract
Neuropeptides are signaling molecules participating in the modulation of synaptic transmission. Neuropeptides are stored in dense core synaptic vesicles, the release of which requires profound excitation. Only in the extracellular space, neuropeptides act on G-protein coupled receptors to exert a relatively slow action both pre- and postsynaptically. Consequently, neuropeptide modulators are ideal candidates to influence epileptic tissue overexcited during seizures. Indeed, a number of neuropeptides have receptors implicated in epilepsy and many of them are considered to participate in endogenous neuroprotective actions. Neuropeptide receptors, present in the hippocampus, the most frequent focus of seizures in temporal lobe epilepsy, received the largest attention as potential anti-epileptic targets. Receptors of hippocampal neuropeptides, somatostatin, neuropeptide Y, galanin, dynorphin, enkephalin, substance P, cholecystokinin, vasoactive intestinal polypeptide, and receptors of some neuropeptides, which are also hormones such as ghrelin, angiotensins, corticotropin- releasing hormone, adrenocorticotropin, thyrotropin-releasing hormone, oxytocin and vasopressin involved in epilepsy are discussed in the review article. Activation and inhibition of receptors by oral application of peptides as drugs is typically not efficient because of low bioavailability: rapid degradation and insufficient penetration of peptides through the blood-brain barrier. Recent progress in the development of non-peptide agonists and antagonists of neuropeptide receptors as well as gene therapeutic approaches leading to the local production of agonists and antagonists within the central nervous system will also be discussed.
Keywords: Neuromodulation, neuronal plasticity, neuropeptide receptors, seizure, temporal lobe epilepsy, therapeutic application.
Current Medicinal Chemistry
Title:Receptors of Peptides as Therapeutic Targets in Epilepsy Research
Volume: 21 Issue: 6
Author(s): A. Dobolyi, K.A. Kekesi, G. Juhasz, A.D. Szekely, G. Lovas and Z. Kovacs
Affiliation:
Keywords: Neuromodulation, neuronal plasticity, neuropeptide receptors, seizure, temporal lobe epilepsy, therapeutic application.
Abstract: Neuropeptides are signaling molecules participating in the modulation of synaptic transmission. Neuropeptides are stored in dense core synaptic vesicles, the release of which requires profound excitation. Only in the extracellular space, neuropeptides act on G-protein coupled receptors to exert a relatively slow action both pre- and postsynaptically. Consequently, neuropeptide modulators are ideal candidates to influence epileptic tissue overexcited during seizures. Indeed, a number of neuropeptides have receptors implicated in epilepsy and many of them are considered to participate in endogenous neuroprotective actions. Neuropeptide receptors, present in the hippocampus, the most frequent focus of seizures in temporal lobe epilepsy, received the largest attention as potential anti-epileptic targets. Receptors of hippocampal neuropeptides, somatostatin, neuropeptide Y, galanin, dynorphin, enkephalin, substance P, cholecystokinin, vasoactive intestinal polypeptide, and receptors of some neuropeptides, which are also hormones such as ghrelin, angiotensins, corticotropin- releasing hormone, adrenocorticotropin, thyrotropin-releasing hormone, oxytocin and vasopressin involved in epilepsy are discussed in the review article. Activation and inhibition of receptors by oral application of peptides as drugs is typically not efficient because of low bioavailability: rapid degradation and insufficient penetration of peptides through the blood-brain barrier. Recent progress in the development of non-peptide agonists and antagonists of neuropeptide receptors as well as gene therapeutic approaches leading to the local production of agonists and antagonists within the central nervous system will also be discussed.
Export Options
About this article
Cite this article as:
Dobolyi A., Kekesi K.A., Juhasz G., Szekely A.D., Lovas G. and Kovacs Z., Receptors of Peptides as Therapeutic Targets in Epilepsy Research, Current Medicinal Chemistry 2014; 21 (6) . https://dx.doi.org/10.2174/0929867320666131119154018
DOI https://dx.doi.org/10.2174/0929867320666131119154018 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
Call for Papers in Thematic Issues
Advances in Medicinal Chemistry: From Cancer to Chronic Diseases.
The broad spectrum of the issue will provide a comprehensive overview of emerging trends, novel therapeutic interventions, and translational insights that impact modern medicine. The primary focus will be diseases of global concern, including cancer, chronic pain, metabolic disorders, and autoimmune conditions, providing a broad overview of the advancements in ...read more
Approaches to the treatment of chronic inflammation
Chronic inflammation is a hallmark of numerous diseases, significantly impacting global health. Although chronic inflammation is a hot topic, not much has been written about approaches to its treatment. This thematic issue aims to showcase the latest advancements in chronic inflammation treatment and foster discussion on future directions in this ...read more
Cellular and Molecular Mechanisms of Non-Infectious Inflammatory Diseases: Focus on Clinical Implications
The Special Issue covers the results of the studies on cellular and molecular mechanisms of non-infectious inflammatory diseases, in particular, autoimmune rheumatic diseases, atherosclerotic cardiovascular disease and other age-related disorders such as type II diabetes, cancer, neurodegenerative disorders, etc. Review and research articles as well as methodology papers that summarize ...read more
Chalcogen-modified nucleic acid analogues
Chalcogen-modified nucleosides, nucleotides and oligonucleotides have been of great interest to scientific research for many years. The replacement of oxygen in the nucleobase, sugar or phosphate backbone by chalcogen atoms (sulfur, selenium, tellurium) gives these biomolecules unique properties resulting from their altered physical and chemical properties. The continuing interest in ...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
-
2-Oxo-1,2,3,4-tetrahydropyrimidines Ethyl Esters as Potent β- Glucuronidase Inhibitors: One-pot Synthesis, In vitro and In silico Studies
Medicinal Chemistry Pharmacogenetics of Target Genes Across Doxorubicin Disposition Pathway: A Review
Current Drug Metabolism PET Imaging of Opioid Receptors in Pain: Progress and New Directions
Current Pharmaceutical Design Role of Methylene Blue in Trauma Neuroprotection and Neuropsychiatric Diseases
CNS & Neurological Disorders - Drug Targets Diabetes, Cognitive Function, and the Blood-Brain Barrier
Current Pharmaceutical Design ABC Transporters in the CNS – An Inventory
Current Pharmaceutical Biotechnology The Progress Towards the Development of DHQO Derivatives and Related Analogues with Inotropic Effects
Mini-Reviews in Medicinal Chemistry Somatostatin and Cognitive Function in Neurodegenerative Disorders
Mini-Reviews in Medicinal Chemistry Active Metabolites Resulting from Decarboxylation, Reduction and Ester Hydrolysis of Parent Drugs
Current Drug Metabolism RhoGEFs in Cell Motility: Novel Links Between Rgnef and Focal Adhesion Kinase
Current Molecular Medicine Meet Our Editorial Board Member
Current Neuropharmacology Pharmacological Screening of Lantana camara for its Antiallergic Activity in Rodents
Clinical Anti-Inflammatory & Anti-Allergy Drugs (Discontinued) Disease-Related Changes in TRPV1 Expression and Its Implications for Drug Development
Current Topics in Medicinal Chemistry Herbal Compounds with Special Reference to Gastrodin as Potential Therapeutic Agents for Microglia Mediated Neuroinflammation
Current Medicinal Chemistry Cytopathological Mechanisms in Mitochondrial Disease
Current Chemical Biology Drugs in Newborn Resuscitation: The More We Learn the Least We Use
Current Medicinal Chemistry Focus on the Role of Glutamate in the Pathology of the Peripheral Nervous System
CNS & Neurological Disorders - Drug Targets Pediatric Catatonia: Updating An Old Syndrome in Young People
Current Psychiatry Reviews The Role of IRE1 Signaling in the Central Nervous System Diseases
Current Neuropharmacology Celiac Disease: An Emerging Epidemic
Current Nutrition & Food Science