Abstract
The search for new peptides to be used as analgesics in place of morphine has been mainly directed to develop peptide analogues or peptidomimetics having higher biological stability and receptor selectivity. Indeed, most of the alkaloid opioid counterindications are due to the scarce stability and the contemporary activation of different receptor types. However, the development of several extremely stable and selective peptide ligands for the different opioid receptors, and the recent discovery of the μ-receptor selective endomorphins, rendered this search less fundamental. In recent years, other opioid peptide properties have been investigated in the search for new pharmacological tools. The utility of a drug depends on its ability to reach appropriate receptors at the target tissue and to remain metabolically stable in order to produce the desired effect. This review deals with the recent investigations on peptide bioavailability, in particular barrier penetration and resistance against enzymatic degradation; with the development of peptides having activity at different receptors; with chimeric peptides, with propeptides, and with non-conventional peptides, lacking basic pharmacophoric features.
Keywords: Opioid peptide analogues, opioid receptors, pain, antinociception, peptide stability, bioavailability
Current Topics in Medicinal Chemistry
Title: SNew Trends in the Development of Opioid Peptide Analogues as Advanced Remedies for Pain Relief
Volume: 4 Issue: 1
Author(s): Luca Gentilucci
Affiliation:
Keywords: Opioid peptide analogues, opioid receptors, pain, antinociception, peptide stability, bioavailability
Abstract: The search for new peptides to be used as analgesics in place of morphine has been mainly directed to develop peptide analogues or peptidomimetics having higher biological stability and receptor selectivity. Indeed, most of the alkaloid opioid counterindications are due to the scarce stability and the contemporary activation of different receptor types. However, the development of several extremely stable and selective peptide ligands for the different opioid receptors, and the recent discovery of the μ-receptor selective endomorphins, rendered this search less fundamental. In recent years, other opioid peptide properties have been investigated in the search for new pharmacological tools. The utility of a drug depends on its ability to reach appropriate receptors at the target tissue and to remain metabolically stable in order to produce the desired effect. This review deals with the recent investigations on peptide bioavailability, in particular barrier penetration and resistance against enzymatic degradation; with the development of peptides having activity at different receptors; with chimeric peptides, with propeptides, and with non-conventional peptides, lacking basic pharmacophoric features.
Export Options
About this article
Cite this article as:
Gentilucci Luca, SNew Trends in the Development of Opioid Peptide Analogues as Advanced Remedies for Pain Relief, Current Topics in Medicinal Chemistry 2004; 4 (1) . https://dx.doi.org/10.2174/1568026043451663
DOI https://dx.doi.org/10.2174/1568026043451663 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
Chemistry Based on Natural Products for Therapeutic Purposes
The development of new pharmaceuticals for a wide range of medical conditions has long relied on the identification of promising natural products (NPs). There are over sixty percent of cancer, infectious illness, and CNS disease medications that include an NP pharmacophore, according to the Food and Drug Administration. Since NP ...read more
Current Trends in Drug Discovery Based on Artificial Intelligence and Computer-Aided Drug Design
Drug development discovery has faced several challenges over the years. In fact, the evolution of classical approaches to modern methods using computational methods, or Computer-Aided Drug Design (CADD), has shown promising and essential results in any drug discovery campaign. Among these methods, molecular docking is one of the most notable ...read more
Drug Discovery in the Age of Artificial Intelligence
In the age of artificial intelligence (AI), we have witnessed a significant boom in AI techniques for drug discovery. AI techniques are increasingly integrated and accelerating the drug discovery process. These developments have not only attracted the attention of academia and industry but also raised important questions regarding the selection ...read more
From Biodiversity to Chemical Diversity: Focus of Flavonoids
Flavonoids are the largest group of polyphenols, plant secondary metabolites arising from the essential aromatic amino acid phenylalanine (or more rarely from tyrosine) via the phenylpropanoid pathway. The flavan nucleus is the basic 15-carbon skeleton of flavonoids (C6-C3-C6), which consists of two phenyl rings (A and B) and a heterocyclic ...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
-
Trophoblast Invasion: A Possible Link Between Implantation Deficiencies and Preeclampsia
Current Women`s Health Reviews Cell Proliferation and Cytotoxicity Assays
Current Pharmaceutical Biotechnology Identification of Disease-Relevant Genes for Molecularly-Targeted Drug Discovery
Current Cancer Drug Targets Current Treatment Strategies for Multiple Sclerosis - Efficacy Versus Neurological Adverse Effects
Current Pharmaceutical Design Drug Design Targeting the CXCR4/CXCR7/CXCL12 Pathway
Current Topics in Medicinal Chemistry The Role and Therapeutic Potential of Ser/Thr Phosphatase PP2A in Apoptotic Signalling Networks in Human Cancer Cells
Current Molecular Medicine Activin Receptor-Like Kinases: Structure, Function and Clinical Implications
Endocrine, Metabolic & Immune Disorders - Drug Targets New Perspectives in Glioma Immunotherapy
Current Pharmaceutical Design The Carnitine Transporter Network: Interactions with Drugs
Current Chemical Biology Recent Patents on Glioblastoma Signaling
Recent Patents on Biomarkers Negative Glucocorticoid Receptor Response Elements and their Role in Glucocorticoid Action
Current Pharmaceutical Design Blockade of Neoangiogenesis, a New and Promising Technique to Control the Growth of Malignant Tumors and their Metastases
Current Vascular Pharmacology Genomic and Epigenetic Complexity of the FOXF1 Locus in 16q24.1: Implications for Development and Disease
Current Genomics Natural Products Based Anticancer Agents
Mini-Reviews in Organic Chemistry The Impact of Gynecological Cancer on Reproductive Issues and Pregnancy:Psychological Implications
Current Women`s Health Reviews Testicular Germ Cell Tumors: A Paradigm for the Successful Treatment of Solid Tumor Stem Cells
Current Cancer Therapy Reviews Emulsomes Meet S-layer Proteins: An Emerging Targeted Drug Delivery System
Current Pharmaceutical Biotechnology Therapeutic Potential of Targeting Glypican-3 in Hepatocellular Carcinoma
Anti-Cancer Agents in Medicinal Chemistry Endometriosis and Perinatal Outcome - A Systematic Review of the Literature
Current Women`s Health Reviews Suppressing Glioblastoma Stem Cell Function by Aldehyde Dehydrogenase Inhibition with Chloramphenicol or Disulfiram as a New Treatment Adjunct: A Hypothesis
Current Stem Cell Research & Therapy