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https://hdl.handle.net/2440/53435
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Type: | Journal article |
Title: | Multiple ligands in opioid research |
Author: | Ballet, S. Pietsch, M. Abell, A. |
Citation: | Protein and Peptide Letters: international journal for rapid publication of short papers in protein and peptide science, 2008; 15(7):668-682 |
Publisher: | Bentham Science Publ Ltd |
Issue Date: | 2008 |
ISSN: | 0929-8665 1875-5305 |
Statement of Responsibility: | Ballet, Steven; Pietsch, Markus and Abell, Andrew D. |
Abstract: | The observation in 1979 that opioid receptors interact, led to the design of bivalent ligands in an attempt to improve selectivity and affinity towards the different subtypes (i.e. μ, δ and κ). Dimers of monovalent “parent” opioid structures have been evaluated and include: (a) endogenous (e.g. enkephalins) or exogenous (e.g. dermorphin) peptide dimer analogues (b) mixed peptidic-non-peptidic bivalent ligands and (c) dual non-peptidic dimers. Chimeric structures, using an opioid pharmacophore in combination with a non-opioid pharmacophore, have also been prepared. The common aim in all these studies is to improve the pharmacological profile of potential analgesics to minimize common opioid-induced side-effects, such as physical dependence and tolerance. Here we present a brief overview of efforts to develop bivalent opioid ligands for use in pain-related research. |
Keywords: | Opioid system bivalent ligands receptor dimer complexes |
DOI: | 10.2174/092986608785133672 |
Grant ID: | http://purl.org/au-research/grants/arc/20103228 |
Published version: | http://dx.doi.org/10.2174/092986608785133672 |
Appears in Collections: | Aurora harvest Chemistry publications |
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