Abstract
Neuropathic pain is originated from different alterations of the nervous system. The difficulty of treatment strongly impairs quality of life of affected people. It is associated with severe, chronic sensory disturbances characterized by spontaneous pain, increased responsiveness to painful stimuli and pain perceived in response to normally non-noxious stimuli. The underlying mechanisms are complex and involve both peripheral and central nervous components. The noradrenergic system plays a pivotal role in the control of pain since its widespread distribution in the “pain matrix” representing a valuable therapeutic target. This review focused on the α2 adrenoceptor subtype modulation as strategy for neuropathic pain relief. Drugs acting as direct α2 adrenoceptor agonists (clonidine and dexmedetomidine) were analyzed as well as the indirect α2 adrenoceptor modulators. The overview included norepinephrine reuptake inhibitors (reboxetine, maprotiline), serotonin/norepinephrine reuptake inhibitors (venlafaxine, milnacipran, amitriptyline, duloxetine, bicifadine) and the compounds characterized by a double pharmacodynamic mechanism combining the norepinephrine reuptake inhibition and the μ opioid agonist profile (tramadol and tapentadol). A summary of recent compounds was illustrated.
Keywords: α2 adrenoceptor agonists, α2 adrenoceptor, neuropathic pain, norepinephrine reuptake inhibitors, norepinephrine, serotonin/norepinephrine reuptake inhibitors, μ opioid agonist/norepinephrine reuptake inhibitors.
Mini-Reviews in Medicinal Chemistry
Title:α2 Adrenoceptor: a Target for Neuropathic Pain Treatment
Volume: 17 Issue: 2
Author(s): Lorenzo Di Cesare Mannelli, Laura Micheli, Letizia Crocetti, Maria Paola Giovannoni, Claudia Vergelli and Carla Ghelardini
Affiliation:
Keywords: α2 adrenoceptor agonists, α2 adrenoceptor, neuropathic pain, norepinephrine reuptake inhibitors, norepinephrine, serotonin/norepinephrine reuptake inhibitors, μ opioid agonist/norepinephrine reuptake inhibitors.
Abstract: Neuropathic pain is originated from different alterations of the nervous system. The difficulty of treatment strongly impairs quality of life of affected people. It is associated with severe, chronic sensory disturbances characterized by spontaneous pain, increased responsiveness to painful stimuli and pain perceived in response to normally non-noxious stimuli. The underlying mechanisms are complex and involve both peripheral and central nervous components. The noradrenergic system plays a pivotal role in the control of pain since its widespread distribution in the “pain matrix” representing a valuable therapeutic target. This review focused on the α2 adrenoceptor subtype modulation as strategy for neuropathic pain relief. Drugs acting as direct α2 adrenoceptor agonists (clonidine and dexmedetomidine) were analyzed as well as the indirect α2 adrenoceptor modulators. The overview included norepinephrine reuptake inhibitors (reboxetine, maprotiline), serotonin/norepinephrine reuptake inhibitors (venlafaxine, milnacipran, amitriptyline, duloxetine, bicifadine) and the compounds characterized by a double pharmacodynamic mechanism combining the norepinephrine reuptake inhibition and the μ opioid agonist profile (tramadol and tapentadol). A summary of recent compounds was illustrated.
Export Options
About this article
Cite this article as:
Mannelli Di Cesare Lorenzo, Micheli Laura, Crocetti Letizia, Giovannoni Paola Maria, Vergelli Claudia and Ghelardini Carla, α2 Adrenoceptor: a Target for Neuropathic Pain Treatment, Mini-Reviews in Medicinal Chemistry 2017; 17 (2) . https://dx.doi.org/10.2174/1389557516666160609065535
DOI https://dx.doi.org/10.2174/1389557516666160609065535 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
Call for Papers in Thematic Issues
Bioprospecting of Natural Products as Sources of New Multitarget Therapies
According to the Convention on Biological Diversity, bioprospecting is the exploration of biodiversity and indigenous knowledge to develop commercially valuable products for pharmaceutical and other applications. Bioprospecting involves searching for useful organic compounds in plants, fungi, marine organisms, and microorganisms. Natural products traditionally constituted the primary source of more than ...read more
Computational Frontiers in Medicinal Chemistry
The thematic issue "Computational Frontiers in Medicinal Chemistry" provides a robust platform for delving into state-of-the-art computational methodologies and technologies that significantly propel advancements in medicinal chemistry. This edition seeks to amalgamate top-tier reviews spotlighting the latest trends and breakthroughs in the fusion of computational approaches, including artificial intelligence (AI) ...read more
Natural Products and Dietary Supplements in Alleviation of Metabolic, Cardiovascular, and Neurological Disorders
Metabolic disorders like diabetes, obesity, inflammation, oxidative stress, cancer etc, cardiovascular disorders like angina, myocardial infarction, congestive heart failure etc as well as neurological disorders like Alzheimer?s, Parkinson?s, Epilepsy, Depression, etc are the global burden. They covered the major segment of the diseases and disorders from which the human community ...read more
Natural Products in Drug Discovery
Natural products have always been one of the important ways of drug discovery due to their novel skeleton and diverse functional group characteristics. According to statistics, between 1981 and 2019, the FDA approved a total of 1,394 small molecule drugs for marketing, of which 930 marketed drugs originated from the ...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
-
Recent Advances in Antiarrhythmic Drug Treatment of Atrial Fibrillation
Recent Patents on Cardiovascular Drug Discovery Sida cordifolia, a Traditional Herb in Modern Perspective – A Review
Current Traditional Medicine Laparoscopic Surgery for Pheochromocytoma and Paraganglioma Removal: A Retrospective Analysis of Anaesthetic Management
Current Hypertension Reviews New-Generation, Non-SSRI Antidepressants: Therapeutic Drug Monitoring and Pharmacological Interactions. Part 1: SNRIs, SMSs, SARIs
Current Medicinal Chemistry Antioxidant Properties and Medicinal Uses of Some Crataegus Spp. (Hawthorn) Including <i>C. meyeri</i> and <i>C. pontica</i>
Current Nutrition & Food Science Heart Rate Variability Indexes in Dementia: A Systematic Review with a Quantitative Analysis
Current Alzheimer Research Herb-Drug Interactions: An Insight into Cardiovascular Diseases Based on Case Reports
Cardiovascular & Hematological Agents in Medicinal Chemistry Ivabradine: A Current Overview
Current Clinical Pharmacology Integrating Pharmacogenetics for Assessment of Herb-Drug Interactions: Has the Time Come?
Current Pharmacogenomics and Personalized Medicine Anti-Tumor Necrosis Factor-Alpha (TNF-α) Treatment Strategies in Crohns Disease
Recent Patents on Inflammation & Allergy Drug Discovery L-Arginine Transport in Disease
Current Medicinal Chemistry - Cardiovascular & Hematological Agents Immunosuppressive Therapies in Solid Organ Transplantation
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Tumor Angiogenesis and VEGFR-2: Mechanism, Pathways and Current Biological Therapeutic Interventions
Current Drug Metabolism Fospropofol, A New Sedative Anesthetic, and Its Utility in the Perioperative Period
Current Pharmaceutical Design Kinin Receptors in Vascular Biology and Pathology
Current Vascular Pharmacology Recent Advances on the Roles of NO in Cancer and Chronic Inflammatory Disorders
Current Medicinal Chemistry Pharmacological Therapy in Children with Atrioventricular Reentry: Which Drug?
Current Pharmaceutical Design Solubility Enhancement and Delivery Systems of Curcumin a Herbal Medicine: A Review
Current Drug Delivery The Role of P-Glycoprotein in Psychiatric Disorders: A Reliable Guard of the Brain?
Central Nervous System Agents in Medicinal Chemistry Essential Hypertension: Translating Pathophysiology into Pharmacogenomics
Current Pharmacogenomics