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
-
Silica Nanoparticles as Promising Drug/Gene Delivery Carriers and Fluorescent Nano-Probes: Recent Advances
Current Cancer Drug Targets Antiproliferative and Proapoptotic Effects of Proteasome Inhibitors and their Combination with Histone Deacetylase Inhibitors on Leukemia Cells
Cardiovascular & Hematological Disorders-Drug Targets Pharmacotherapies to Manage Bone Loss-Associated Diseases: A Quest for the Perfect Benefit-to-Risk Ratio
Current Medicinal Chemistry Regulatable Gene Expression Systems for Gene Therapy
Current Gene Therapy Retinoid Receptors and Therapeutic Applications of RAR/RXR Modulators
Current Topics in Medicinal Chemistry Functional Chemical Groups that May Likely Become a Source for the Synthesis of Novel Central Nervous System (CNS) Acting Drugs
Central Nervous System Agents in Medicinal Chemistry Leptin and Inflammation
Current Immunology Reviews (Discontinued) Mitochondria-Associated Membranes (MAMs): A Novel Therapeutic Target for Treating Metabolic Syndrome
Current Medicinal Chemistry Hypericin - The Facts About a Controversial Agent
Current Pharmaceutical Design Gonadotropin-Releasing Hormone (GnRH) Receptors in Tumors: a New Rationale for the Therapeutical Application of GnRH Analogs in Cancer Patients?
Current Cancer Drug Targets Glucagon and Glucagon-Like Peptide Receptors as Drug Targets
Current Pharmaceutical Design Pathophysiology of Erectile Dysfunction
Current Drug Targets Role of Nuclear Steroid Receptors in Apoptosis
Current Medicinal Chemistry A Scientometrics Analysis and Visualization of Depressive Disorder
Current Neuropharmacology The Effect of Psychological Stress and Social Isolation on Neuroimmunoendocrine Communication
Current Pharmaceutical Design Mechanisms Explaining the Influence of Subclinical Hypothyroidism on the Onset and Progression of Chronic Heart Failure
Endocrine, Metabolic & Immune Disorders - Drug Targets T-type Calcium Channels in Health and Disease
Current Medicinal Chemistry Drug Resistance: Challenges to Effective Therapy
Current Cancer Drug Targets Estrogen Receptors: Mechanism of Action and Relevance to Schizophrenia
Current Psychiatry Reviews Epigenetic Basis of Individual Variability to Major Psychosis
Current Pharmacogenomics and Personalized Medicine