Abstract
Opioid receptors and opioid peptides constitute the endogenous opioid system. The most relevant function of the opioid system seems to be the inhibitory modulation of nociceptive information at supraspinal, spinal and peripheral sites, although it is also implicated in the modulation of many other processes in the body. Centrally acting plant opiates, such as morphine, are the most frequently used analgesics for the relief of severe pain, even though their undesired side-effects are serious limitation to their usefulness. Opioid peptides have the potential to be pharmaceutical agents for the treatment of pain, devoid of side-effects accompanying morphine. Unfortunately, peptides are generally hydrophilic compounds that will not enter the central nervous system via passive diffusion, due to the existence of the blood-brain barrier. Peptides are also easily degraded by proteolytic enzymes which further reduces their therapeutic value. Therefore, the design of peptide analogs based on the sequence of endogenous opioid peptides must be focused on increasing bioavailability and enhancing brain uptake.
Current Pharmaceutical Design
Title: Development of Opioid Peptide Analogs for Pain Relief
Volume: 16 Issue: 9
Author(s): A. Janecka, R. Perlikowska, K. Gach, A. Wyrebska and J. Fichna
Affiliation:
Abstract: Opioid receptors and opioid peptides constitute the endogenous opioid system. The most relevant function of the opioid system seems to be the inhibitory modulation of nociceptive information at supraspinal, spinal and peripheral sites, although it is also implicated in the modulation of many other processes in the body. Centrally acting plant opiates, such as morphine, are the most frequently used analgesics for the relief of severe pain, even though their undesired side-effects are serious limitation to their usefulness. Opioid peptides have the potential to be pharmaceutical agents for the treatment of pain, devoid of side-effects accompanying morphine. Unfortunately, peptides are generally hydrophilic compounds that will not enter the central nervous system via passive diffusion, due to the existence of the blood-brain barrier. Peptides are also easily degraded by proteolytic enzymes which further reduces their therapeutic value. Therefore, the design of peptide analogs based on the sequence of endogenous opioid peptides must be focused on increasing bioavailability and enhancing brain uptake.
Export Options
About this article
Cite this article as:
Janecka A., Perlikowska R., Gach K., Wyrebska A. and Fichna J., Development of Opioid Peptide Analogs for Pain Relief, Current Pharmaceutical Design 2010; 16 (9) . https://dx.doi.org/10.2174/138161210790963869
DOI https://dx.doi.org/10.2174/138161210790963869 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
Call for Papers in Thematic Issues
"Tuberculosis Prevention, Diagnosis and Drug Discovery"
The Nobel Prize-winning discoveries of Mycobacterium tuberculosis and streptomycin have enabled an appropriate diagnosis and an effective treatment of tuberculosis (TB). Since then, many newer diagnosis methods and drugs have been saving millions of lives. Despite advances in the past, TB is still a leading cause of infectious disease mortality ...read more
Current Pharmaceutical challenges in the treatment and diagnosis of neurological dysfunctions
Neurological dysfunctions (MND, ALS, MS, PD, AD, HD, ALS, Autism, OCD etc..) present significant challenges in both diagnosis and treatment, often necessitating innovative approaches and therapeutic interventions. This thematic issue aims to explore the current pharmaceutical landscape surrounding neurological disorders, shedding light on the challenges faced by researchers, clinicians, and ...read more
Emerging and re-emerging diseases
Faced with a possible endemic situation of COVID-19, the world has experienced two important phenomena, the emergence of new infectious diseases and/or the resurgence of previously eradicated infectious diseases. Furthermore, the geographic distribution of such diseases has also undergone changes. This context, in turn, may have a strong relationship with ...read more
Melanoma and Non-Melanoma Skin Cancer Treatment: Standard of Care and Recent Advances
In this thematic issue, we aim to provide a standard of care of the diagnosis and treatment of melanoma and non-melanoma skin cancer. The editor will invite authors from different countries who will write review articles of melanoma and non-melanoma skin cancers. The Diagnosis, Staging, Surgical Treatment, Non-Surgical Treatment all ...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
-
Defining and Regulating Acute Inflammatory Lesion Formation during the Pathogenesis of Multiple Sclerosis and Experimental Autoimmune Encephalomyelitis
CNS & Neurological Disorders - Drug Targets PiWi RNA in Neurodevelopment and Neurodegenerative Disorders
Current Molecular Pharmacology Cancer and Treatment Modalities
Current Cancer Therapy Reviews Cardiomyopathy of Pregnancy
Current Women`s Health Reviews Patent Selections:
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery Recent Advances in Pharmacological Interventions of Chronic Prostatitis/ Chronic Pelvic Pain Syndrome
Current Pharmaceutical Design Metabolic Basis of Sporadic Alzeimer’s Disease. Role of Hormones Related to Energy Metabolism
Current Pharmaceutical Design Endoradiotherapy with Peptides - Status and Future Development
Current Medicinal Chemistry Correlation between Potassium Channel Expression and Sensitivity to Drug-induced Cell Death in Tumor Cell Lines
Current Pharmaceutical Design Rational Design and Development of Colon-Specific Prodrugs
Current Topics in Medicinal Chemistry G Protein-Coupled Receptor Transmembrane Binding Pockets and their Applications in GPCR Research and Drug Discovery: A Survey
Current Topics in Medicinal Chemistry Cytokine and Immune System Abnormalities in Fibromyalgia and Other Central Sensitivity Syndromes
Current Rheumatology Reviews Tamoxifen and its New Derivatives in Cancer Research
Recent Patents on Anti-Cancer Drug Discovery Leptin and Inflammation
Current Immunology Reviews (Discontinued) Role of Prolyl Endopeptidase in Intracellular Transport and Protein Secretion
CNS & Neurological Disorders - Drug Targets Pharmacogenetics of Asthma Therapy
Current Pharmaceutical Design The Hormetic Role of Dietary Antioxidants in Free Radical-Related Diseases
Current Pharmaceutical Design Hypothyroidism and Cardiovascular Disease: Factors, Mechanism and Future Perspectives
Current Medicinal Chemistry Mitochondria-Associated Membranes (MAMs): A Novel Therapeutic Target for Treating Metabolic Syndrome
Current Medicinal Chemistry Assessing the Neuronal Serotonergic Target-based Antidepressant Stratagem: Impact of In Vivo Interaction Studies and Knockout Models
Current Neuropharmacology