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.
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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 |
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