Abstract
Management of acute and chronic pain has always been a key area of clinical research. Enkephalinase inhibitors (EIs) seem to be promising as therapeutic agents having antinociceptive action. They additionally possess anticraving, antidiarrhoeal and antidepressant actions. The antinociceptive action of EIs has been reported for over a decade however, their therapeutic potential is yet to be effectively explored. EIs may be broadly classified as endogenous and those that are obtained synthetically. Endogenous EIs include peptides like spinorphin and opiorphin. And compounds like RB 101, RB 120, RB 3007 constitute the synthetically obtained EIs. Endogenous and synthetic inhibitors enkephalin degrading enzymes have been studied in vivo using standard animal models. The potential EI targets appear to be APN (Aminopeptidase N), NEP (Neutral endopeptidase), DPP-III (Dipeptidyl peptidase). EIs possess the advantage that they lack the opioid side effects. This article reviews the mechanisms by which EIs act and elucidates the pathways involved.
Keywords: Enkephalinase inhibitors, antinociception, pain
Current Drug Targets
Title: Enkephalinase Inhibitors: Potential Agents for the Management of Pain
Volume: 9 Issue: 10
Author(s): V. Thanawala, V. J. Kadam and R. Ghosh
Affiliation:
Keywords: Enkephalinase inhibitors, antinociception, pain
Abstract: Management of acute and chronic pain has always been a key area of clinical research. Enkephalinase inhibitors (EIs) seem to be promising as therapeutic agents having antinociceptive action. They additionally possess anticraving, antidiarrhoeal and antidepressant actions. The antinociceptive action of EIs has been reported for over a decade however, their therapeutic potential is yet to be effectively explored. EIs may be broadly classified as endogenous and those that are obtained synthetically. Endogenous EIs include peptides like spinorphin and opiorphin. And compounds like RB 101, RB 120, RB 3007 constitute the synthetically obtained EIs. Endogenous and synthetic inhibitors enkephalin degrading enzymes have been studied in vivo using standard animal models. The potential EI targets appear to be APN (Aminopeptidase N), NEP (Neutral endopeptidase), DPP-III (Dipeptidyl peptidase). EIs possess the advantage that they lack the opioid side effects. This article reviews the mechanisms by which EIs act and elucidates the pathways involved.
Export Options
About this article
Cite this article as:
Thanawala V., Kadam J. V. and Ghosh R., Enkephalinase Inhibitors: Potential Agents for the Management of Pain, Current Drug Targets 2008; 9 (10) . https://dx.doi.org/10.2174/138945008785909356
DOI https://dx.doi.org/10.2174/138945008785909356 |
Print ISSN 1389-4501 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5592 |
Call for Papers in Thematic Issues
New drug therapy for eye diseases
Eyesight is one of the most critical senses, accounting for over 80% of our perceptions. Our quality of life might be significantly affected by eye disease, including glaucoma, diabetic retinopathy, dry eye, etc. Although the development of microinvasive ocular surgery reduces surgical complications and improves overall outcomes, medication therapy is ...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
-
Cross-Talk Between NO Synthase Isoforms in Neuro-Inflammation: Possible Implications in HIV-Associated Neurocognitive Disorders
Current Medicinal Chemistry The Impact of Cardiovascular Diseases on Cardiovascular Regulation During Exercise in Humans: Studies on Metaboreflex Activation Elicited by the Post-exercise Muscle Ischemia Method
Current Cardiology Reviews Potential Therapeutic Application of Chondroitin Sulfate/Dermatan Sulfate
Current Drug Discovery Technologies Cardiovascular Proteomics
Current Proteomics Early Pathogenesis of Atherosclerosis: The Childhood Obesity
Current Pharmaceutical Design Angiotensin Converting Enzyme 2 Activator (DIZE) Modulates Metabolic Profiles in Mice, Decreasing Lipogenesis
Protein & Peptide Letters Poly(ADP-Ribose) Polymerase Inhibitors: New Pharmacological Functions and Potential Clinical Implications
Current Pharmaceutical Design Angiogenetic Potential of Ad2/Hif-1α/Vp16 after Regional Application in a Preclinical Pig Model of Chronic Ischemia
Current Vascular Pharmacology Acute Respiratory Failure in Obstetric Patients
Current Women`s Health Reviews Reactive Oxygen Species in Myocardial Reperfusion Injury: From Physiopathology to Therapeutic Approaches
Current Pharmaceutical Biotechnology The Use of Exercise Echocardiography in the Evaluation of Mitral Regurgitation
Current Cardiology Reviews Plasminogen Activation-Based Thrombolysis for Ischaemic Stroke: The Diversity of Targets may Demand New Approaches
Current Drug Targets Theoretical and Evidence-Based Benefit of Afterload Reduction in the Postoperative Pediatric Heart
Current Vascular Pharmacology Small Players With Big Roles: MicroRNAs as Targets to Inhibit Breast Cancer Progression
Current Drug Targets High Density Lipoprotein Administration: A New Therapeutic Modality for the Treatment of Cardiovascular Diseases
Current Medicinal Chemistry - Immunology, Endocrine & Metabolic Agents Effects of Metabolic Approach in Diabetic Patients with Coronary Artery Disease
Current Pharmaceutical Design Why Multiples of 21? Why does Selenoprotein P Contain Multiple Selenocysteine Residues?
Current Nutraceuticals Antiarrhythmic Potential of Drugs Targeting the Cardiac Ryanodine Receptor Ca<sup>2+</sup> Release Channel: Case Study of Dantrolene
Current Pharmaceutical Design Atheromatosis Extent in Coronary Artery Disease is not Correlated with Apolipoprotein-E Polymorphism and its Plasma Levels, but Associated with Cognitive Decline
Current Alzheimer Research Cardiovascular Involvement in Pediatric Systemic Autoimmune Diseases: The Emerging Role of Noninvasive Cardiovascular Imaging
Inflammation & Allergy - Drug Targets (Discontinued)