Opioids and Their Receptors
The interest in opioids such as morphine, the prototypical opioid ligand, has been maintained through the years. The identification of endogenous opioids and their receptors (mu, delta, kappa, and nociceptin), molecular cloning, and the elucidation of the crystal structures of opioid receptors repre...
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| Aineistotyyppi: | Online |
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| Kieli: | englanti |
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MDPI - Multidisciplinary Digital Publishing Institute
2021
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| Linkit: | ONIX_20210501_9783036500461_1174 |
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| collection | Directory of Open Access Books |
| description | The interest in opioids such as morphine, the prototypical opioid ligand, has been maintained through the years. The identification of endogenous opioids and their receptors (mu, delta, kappa, and nociceptin), molecular cloning, and the elucidation of the crystal structures of opioid receptors represent key milestones in opioid research. The opioid system modulates numerous pharmacological responses, with therapeutic (i.e., analgesia) and detrimental side effects (i.e., addiction). The medical use and misuse of opioids have dramatically increased, leading to the 21st century opioid crisis. This book presents recent developments in opioid drug discovery, specifically in the medicinal chemistry and pharmacology of new ligands targeting the opioid receptors as effective and safe therapeutics for human diseases. Furthermore, it draws a special attention to advancing concepts and strategies in opioid drug discovery to mitigate opioid liabilities. The diversity among the discussed topics is a testimony to the complexity of the opioid system, which results from the expression, regulation, and functional role of ligands and receptors. The array of multidisciplinary research areas illustrates the rapidly developing basic research and translational activities in opioid drug discovery. This book will serve as a useful reference while also stimulating continued research in the chemistry and pharmacology of opioids and their receptors, with the prospect of developing improved therapies for human diseases, but also improving health and quality of life in general. |
| format | Online |
| id | doab-20.500.12854ir-69428 |
| institution | Directory of Open Access Books |
| language | eng |
| publishDate | 2021 |
| publishDateRange | 2021 |
| publishDateSort | 2021 |
| publisher | MDPI - Multidisciplinary Digital Publishing Institute |
| publisherStr | MDPI - Multidisciplinary Digital Publishing Institute |
| record_format | ojs |
| spelling | doab-20.500.12854ir-694282024-03-30T23:22:42Z Opioids and Their Receptors Spetea, Mariana Schmidhammer, Helmut opioid receptors neurokinin-1 receptor peptide synthesis receptor binding studies functional assay writhing test tolerance Leu-enkephalin beta-arrestin mu opioid receptor delta opioid receptor biased signaling DADLE ischemia plasma stability morphinan BNTX δ opioid receptor antagonist 1H-NMR experiments mechanism elucidation peripheral antinociception 14-methoxycodeine-6-O-sulfate codeine-6-O-sulfate opioid peptides and peptidomimetics DAMGO DALDA [Dmt1]DALDA KGOP01 binding molecular docking structure-activity relationships β2-amino acids β2-Homo-amino acids µ-opioid receptor opioid peptides TAPP racemic synthesis of β2-amino acids peripheral µ-opioid receptors analgesia peripheral analgesic tolerance dysbiosis opioid bifunctional ligands (−)-N-phenethylnorhydromorphone analogs [35S]GTPgammaS assay forskolin-induced cAMP accumulation assays β-arrestin recruitment assays MOR and DOR agonists respiratory depression bias factor molecular modeling & simulation δ opioid receptor NTI derivative sulfonamide inverse agonist neutral antagonist agonist opioids mu receptor opioid side effects biased agonism partial agonism zerumbone chronic constriction injury (CCI) allodynia hyperalgesia potassium channels over-the-counter drugs misuse abuse opioid drugs pharmacology codeine dihydrocodeine loperamide opioid peptide macrocyclic tetrapeptide multifunctional ligands kappa opioid receptor analgesics opioid liabilities μ opioid receptor receptor model biased ligands dependence pain therapy neonatal opioid withdrawal syndrome naltrexone 6β-naltrexol buprenorphine G-protein bias arrestin recruitment respiration mitragynine heteromer internalization primary hippocampal culture lysosomes µ opioid receptor molecular dynamics docking interaction fingerprints biased agonists SR-17018 PZM21 morphine fentanyl diphenethylamines design and synthesis structure–activity relationships partial agonist biased agonist antagonist binding affinity selectivity n/a thema EDItEUR::M Medicine and Nursing The interest in opioids such as morphine, the prototypical opioid ligand, has been maintained through the years. The identification of endogenous opioids and their receptors (mu, delta, kappa, and nociceptin), molecular cloning, and the elucidation of the crystal structures of opioid receptors represent key milestones in opioid research. The opioid system modulates numerous pharmacological responses, with therapeutic (i.e., analgesia) and detrimental side effects (i.e., addiction). The medical use and misuse of opioids have dramatically increased, leading to the 21st century opioid crisis. This book presents recent developments in opioid drug discovery, specifically in the medicinal chemistry and pharmacology of new ligands targeting the opioid receptors as effective and safe therapeutics for human diseases. Furthermore, it draws a special attention to advancing concepts and strategies in opioid drug discovery to mitigate opioid liabilities. The diversity among the discussed topics is a testimony to the complexity of the opioid system, which results from the expression, regulation, and functional role of ligands and receptors. The array of multidisciplinary research areas illustrates the rapidly developing basic research and translational activities in opioid drug discovery. This book will serve as a useful reference while also stimulating continued research in the chemistry and pharmacology of opioids and their receptors, with the prospect of developing improved therapies for human diseases, but also improving health and quality of life in general. 2021-05-01T15:49:24Z 2021-05-01T15:49:24Z 2020 book ONIX_20210501_9783036500461_1174 9783036500461 9783036500478 https://directory.doabooks.org/handle/20.500.12854/69428 eng application/octet-stream Attribution 4.0 International https://mdpi.com/books/pdfview/book/3230 https://mdpi.com/books/pdfview/book/3230 MDPI - Multidisciplinary Digital Publishing Institute 10.3390/books978-3-03650-047-8 10.3390/books978-3-03650-047-8 46cabcaa-dd94-4bfe-87b4-55023c1b36d0 9783036500461 9783036500478 358 Basel, Switzerland open access |
| spellingShingle | opioid receptors neurokinin-1 receptor peptide synthesis receptor binding studies functional assay writhing test tolerance Leu-enkephalin beta-arrestin mu opioid receptor delta opioid receptor biased signaling DADLE ischemia plasma stability morphinan BNTX δ opioid receptor antagonist 1H-NMR experiments mechanism elucidation peripheral antinociception 14-methoxycodeine-6-O-sulfate codeine-6-O-sulfate opioid peptides and peptidomimetics DAMGO DALDA [Dmt1]DALDA KGOP01 binding molecular docking structure-activity relationships β2-amino acids β2-Homo-amino acids µ-opioid receptor opioid peptides TAPP racemic synthesis of β2-amino acids peripheral µ-opioid receptors analgesia peripheral analgesic tolerance dysbiosis opioid bifunctional ligands (−)-N-phenethylnorhydromorphone analogs [35S]GTPgammaS assay forskolin-induced cAMP accumulation assays β-arrestin recruitment assays MOR and DOR agonists respiratory depression bias factor molecular modeling & simulation δ opioid receptor NTI derivative sulfonamide inverse agonist neutral antagonist agonist opioids mu receptor opioid side effects biased agonism partial agonism zerumbone chronic constriction injury (CCI) allodynia hyperalgesia potassium channels over-the-counter drugs misuse abuse opioid drugs pharmacology codeine dihydrocodeine loperamide opioid peptide macrocyclic tetrapeptide multifunctional ligands kappa opioid receptor analgesics opioid liabilities μ opioid receptor receptor model biased ligands dependence pain therapy neonatal opioid withdrawal syndrome naltrexone 6β-naltrexol buprenorphine G-protein bias arrestin recruitment respiration mitragynine heteromer internalization primary hippocampal culture lysosomes µ opioid receptor molecular dynamics docking interaction fingerprints biased agonists SR-17018 PZM21 morphine fentanyl diphenethylamines design and synthesis structure–activity relationships partial agonist biased agonist antagonist binding affinity selectivity n/a thema EDItEUR::M Medicine and Nursing Opioids and Their Receptors |
| title | Opioids and Their Receptors |
| title_full | Opioids and Their Receptors |
| title_fullStr | Opioids and Their Receptors |
| title_full_unstemmed | Opioids and Their Receptors |
| title_short | Opioids and Their Receptors |
| title_sort | opioids and their receptors |
| topic | opioid receptors neurokinin-1 receptor peptide synthesis receptor binding studies functional assay writhing test tolerance Leu-enkephalin beta-arrestin mu opioid receptor delta opioid receptor biased signaling DADLE ischemia plasma stability morphinan BNTX δ opioid receptor antagonist 1H-NMR experiments mechanism elucidation peripheral antinociception 14-methoxycodeine-6-O-sulfate codeine-6-O-sulfate opioid peptides and peptidomimetics DAMGO DALDA [Dmt1]DALDA KGOP01 binding molecular docking structure-activity relationships β2-amino acids β2-Homo-amino acids µ-opioid receptor opioid peptides TAPP racemic synthesis of β2-amino acids peripheral µ-opioid receptors analgesia peripheral analgesic tolerance dysbiosis opioid bifunctional ligands (−)-N-phenethylnorhydromorphone analogs [35S]GTPgammaS assay forskolin-induced cAMP accumulation assays β-arrestin recruitment assays MOR and DOR agonists respiratory depression bias factor molecular modeling & simulation δ opioid receptor NTI derivative sulfonamide inverse agonist neutral antagonist agonist opioids mu receptor opioid side effects biased agonism partial agonism zerumbone chronic constriction injury (CCI) allodynia hyperalgesia potassium channels over-the-counter drugs misuse abuse opioid drugs pharmacology codeine dihydrocodeine loperamide opioid peptide macrocyclic tetrapeptide multifunctional ligands kappa opioid receptor analgesics opioid liabilities μ opioid receptor receptor model biased ligands dependence pain therapy neonatal opioid withdrawal syndrome naltrexone 6β-naltrexol buprenorphine G-protein bias arrestin recruitment respiration mitragynine heteromer internalization primary hippocampal culture lysosomes µ opioid receptor molecular dynamics docking interaction fingerprints biased agonists SR-17018 PZM21 morphine fentanyl diphenethylamines design and synthesis structure–activity relationships partial agonist biased agonist antagonist binding affinity selectivity n/a thema EDItEUR::M Medicine and Nursing |
| topic_facet | opioid receptors neurokinin-1 receptor peptide synthesis receptor binding studies functional assay writhing test tolerance Leu-enkephalin beta-arrestin mu opioid receptor delta opioid receptor biased signaling DADLE ischemia plasma stability morphinan BNTX δ opioid receptor antagonist 1H-NMR experiments mechanism elucidation peripheral antinociception 14-methoxycodeine-6-O-sulfate codeine-6-O-sulfate opioid peptides and peptidomimetics DAMGO DALDA [Dmt1]DALDA KGOP01 binding molecular docking structure-activity relationships β2-amino acids β2-Homo-amino acids µ-opioid receptor opioid peptides TAPP racemic synthesis of β2-amino acids peripheral µ-opioid receptors analgesia peripheral analgesic tolerance dysbiosis opioid bifunctional ligands (−)-N-phenethylnorhydromorphone analogs [35S]GTPgammaS assay forskolin-induced cAMP accumulation assays β-arrestin recruitment assays MOR and DOR agonists respiratory depression bias factor molecular modeling & simulation δ opioid receptor NTI derivative sulfonamide inverse agonist neutral antagonist agonist opioids mu receptor opioid side effects biased agonism partial agonism zerumbone chronic constriction injury (CCI) allodynia hyperalgesia potassium channels over-the-counter drugs misuse abuse opioid drugs pharmacology codeine dihydrocodeine loperamide opioid peptide macrocyclic tetrapeptide multifunctional ligands kappa opioid receptor analgesics opioid liabilities μ opioid receptor receptor model biased ligands dependence pain therapy neonatal opioid withdrawal syndrome naltrexone 6β-naltrexol buprenorphine G-protein bias arrestin recruitment respiration mitragynine heteromer internalization primary hippocampal culture lysosomes µ opioid receptor molecular dynamics docking interaction fingerprints biased agonists SR-17018 PZM21 morphine fentanyl diphenethylamines design and synthesis structure–activity relationships partial agonist biased agonist antagonist binding affinity selectivity n/a thema EDItEUR::M Medicine and Nursing |
| url | ONIX_20210501_9783036500461_1174 |