Biased agonism: the quest for the analgesic holy grail
Abstract. Opioids alleviate pain, but adverse effects severely limit their usefulness. To solve this problem, biased ligands favoring 1 signaling pathway downstream of the μ-opioid receptor over another are being developed. In the target article, the authors synthesize compounds that preferentially...
| Main Authors: | , |
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| Format: | Article |
| Language: | English |
| Published: |
Wolters Kluwer
2018-06-01
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| Series: | PAIN Reports |
| Online Access: | http://journals.lww.com/painrpts/fulltext/10.1097/PR9.0000000000000650 |
| _version_ | 1818541507590750208 |
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| author | M. Alexander Stanczyk Ram Kandasamy |
| author_facet | M. Alexander Stanczyk Ram Kandasamy |
| author_sort | M. Alexander Stanczyk |
| collection | DOAJ |
| description | Abstract. Opioids alleviate pain, but adverse effects severely limit their usefulness. To solve this problem, biased ligands favoring 1 signaling pathway downstream of the μ-opioid receptor over another are being developed. In the target article, the authors synthesize compounds that preferentially activate G-protein or β-arrestin signaling. They find that increased bias towards G-protein signaling produces better antinociception with minimal side effects in mice models. G-protein–biased opioids may provide a safer treatment strategy. |
| first_indexed | 2024-12-11T22:10:12Z |
| format | Article |
| id | doaj.art-971cb6377c854dc6bc4506945dc60dfa |
| institution | Directory Open Access Journal |
| issn | 2471-2531 |
| language | English |
| last_indexed | 2024-12-11T22:10:12Z |
| publishDate | 2018-06-01 |
| publisher | Wolters Kluwer |
| record_format | Article |
| series | PAIN Reports |
| spelling | doaj.art-971cb6377c854dc6bc4506945dc60dfa2022-12-22T00:48:49ZengWolters KluwerPAIN Reports2471-25312018-06-0133e65010.1097/PR9.0000000000000650201806000-00001Biased agonism: the quest for the analgesic holy grailM. Alexander Stanczyk0Ram Kandasamy1Department of Pharmacology and Edward F. Domino Research Center, University of Michigan Medical School, Ann Arbor, MI, USADepartment of Pharmacology and Edward F. Domino Research Center, University of Michigan Medical School, Ann Arbor, MI, USAAbstract. Opioids alleviate pain, but adverse effects severely limit their usefulness. To solve this problem, biased ligands favoring 1 signaling pathway downstream of the μ-opioid receptor over another are being developed. In the target article, the authors synthesize compounds that preferentially activate G-protein or β-arrestin signaling. They find that increased bias towards G-protein signaling produces better antinociception with minimal side effects in mice models. G-protein–biased opioids may provide a safer treatment strategy.http://journals.lww.com/painrpts/fulltext/10.1097/PR9.0000000000000650 |
| spellingShingle | M. Alexander Stanczyk Ram Kandasamy Biased agonism: the quest for the analgesic holy grail PAIN Reports |
| title | Biased agonism: the quest for the analgesic holy grail |
| title_full | Biased agonism: the quest for the analgesic holy grail |
| title_fullStr | Biased agonism: the quest for the analgesic holy grail |
| title_full_unstemmed | Biased agonism: the quest for the analgesic holy grail |
| title_short | Biased agonism: the quest for the analgesic holy grail |
| title_sort | biased agonism the quest for the analgesic holy grail |
| url | http://journals.lww.com/painrpts/fulltext/10.1097/PR9.0000000000000650 |
| work_keys_str_mv | AT malexanderstanczyk biasedagonismthequestfortheanalgesicholygrail AT ramkandasamy biasedagonismthequestfortheanalgesicholygrail |