Opioid Analgesics: Rise and Fall of Ligand Biased Signaling and Future Perspectives in the Quest for the Holy Grail.
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| Title: | Opioid Analgesics: Rise and Fall of Ligand Biased Signaling and Future Perspectives in the Quest for the Holy Grail. |
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| Authors: | Breault, Émile (AUTHOR), Brouillette, Rebecca L. (AUTHOR), Hébert, Terence E. (AUTHOR), Sarret, Philippe (AUTHOR), Besserer-Offroy, Élie (AUTHOR) |
| Source: | CNS Drugs. Jun2025, Vol. 39 Issue 6, p565-581. 17p. |
| Subjects: | Opioid analgesics, Opioid receptors, Chronic pain, Cellular signal transduction, Pain medicine, Ligands (Biochemistry), Opioid epidemic |
| Abstract: | Opioid analgesics have been used for more than 5000 years and remain the main pain medications prescribed today. Although morphine is considered the gold standard of pain relief, this selective µ-opioid receptor (MOP) agonist provides only moderate relief for many chronic pain conditions and produces a number of unwanted effects that can affect the patient's quality of life, prevent adherence to treatment or lead to addiction. In addition to the lack of progress in developing better analgesics, there have been no significant breakthroughs to date in combating the above-mentioned side effects. Fortunately, a better understanding of opioid pharmacology has given renewed hope for the development of better and safer pain medications. In this review, we describe how clinically approved opioids were initially characterized as biased ligands and what impact this approach might have on clinical practice. We also look at the preclinical and clinical development of biased MOP agonists, focusing on the history of oliceridine, the first specifically designed biased analgesic. In addition, we explore the discrepancies between ligands with low intrinsic efficacy and those with biased properties. Finally, we examine the rationale behind the development of biased ligands during the opioid crisis. [ABSTRACT FROM AUTHOR] |
| Copyright of CNS Drugs is the property of Springer Nature and its content may not be copied or emailed to multiple sites without the copyright holder's express written permission. Additionally, content may not be used with any artificial intelligence tools or machine learning technologies. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.) | |
| Database: | Psychology and Behavioral Sciences Collection |
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| Header | DbId: pbh DbLabel: Psychology and Behavioral Sciences Collection An: 184993001 AccessLevel: 6 PubType: Academic Journal PubTypeId: academicJournal PreciseRelevancyScore: 0 |
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| Items | – Name: Title Label: Title Group: Ti Data: Opioid Analgesics: Rise and Fall of Ligand Biased Signaling and Future Perspectives in the Quest for the Holy Grail. – Name: Author Label: Authors Group: Au Data: <searchLink fieldCode="AR" term="%22Breault%2C+Émile%22">Breault, Émile</searchLink> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Brouillette%2C+Rebecca+L%2E%22">Brouillette, Rebecca L.</searchLink> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Hébert%2C+Terence+E%2E%22">Hébert, Terence E.</searchLink> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Sarret%2C+Philippe%22">Sarret, Philippe</searchLink> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Besserer-Offroy%2C+Élie%22">Besserer-Offroy, Élie</searchLink> (AUTHOR) – Name: TitleSource Label: Source Group: Src Data: <searchLink fieldCode="JN" term="%22CNS+Drugs%22">CNS Drugs</searchLink>. Jun2025, Vol. 39 Issue 6, p565-581. 17p. – Name: Subject Label: Subjects Group: Su Data: <searchLink fieldCode="DE" term="%22Opioid+analgesics%22">Opioid analgesics</searchLink><br /><searchLink fieldCode="DE" term="%22Opioid+receptors%22">Opioid receptors</searchLink><br /><searchLink fieldCode="DE" term="%22Chronic+pain%22">Chronic pain</searchLink><br /><searchLink fieldCode="DE" term="%22Cellular+signal+transduction%22">Cellular signal transduction</searchLink><br /><searchLink fieldCode="DE" term="%22Pain+medicine%22">Pain medicine</searchLink><br /><searchLink fieldCode="DE" term="%22Ligands+%28Biochemistry%29%22">Ligands (Biochemistry)</searchLink><br /><searchLink fieldCode="DE" term="%22Opioid+epidemic%22">Opioid epidemic</searchLink> – Name: Abstract Label: Abstract Group: Ab Data: Opioid analgesics have been used for more than 5000 years and remain the main pain medications prescribed today. Although morphine is considered the gold standard of pain relief, this selective µ-opioid receptor (MOP) agonist provides only moderate relief for many chronic pain conditions and produces a number of unwanted effects that can affect the patient's quality of life, prevent adherence to treatment or lead to addiction. In addition to the lack of progress in developing better analgesics, there have been no significant breakthroughs to date in combating the above-mentioned side effects. Fortunately, a better understanding of opioid pharmacology has given renewed hope for the development of better and safer pain medications. In this review, we describe how clinically approved opioids were initially characterized as biased ligands and what impact this approach might have on clinical practice. We also look at the preclinical and clinical development of biased MOP agonists, focusing on the history of oliceridine, the first specifically designed biased analgesic. In addition, we explore the discrepancies between ligands with low intrinsic efficacy and those with biased properties. Finally, we examine the rationale behind the development of biased ligands during the opioid crisis. [ABSTRACT FROM AUTHOR] – Name: AbstractSuppliedCopyright Label: Group: Ab Data: <i>Copyright of CNS Drugs is the property of Springer Nature and its content may not be copied or emailed to multiple sites without the copyright holder's express written permission. Additionally, content may not be used with any artificial intelligence tools or machine learning technologies. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract.</i> (Copyright applies to all Abstracts.) |
| PLink | https://search.ebscohost.com/login.aspx?direct=true&site=eds-live&db=pbh&AN=184993001 |
| RecordInfo | BibRecord: BibEntity: Identifiers: – Type: doi Value: 10.1007/s40263-025-01172-w Languages: – Code: eng Text: English PhysicalDescription: Pagination: PageCount: 17 StartPage: 565 Subjects: – SubjectFull: Opioid analgesics Type: general – SubjectFull: Opioid receptors Type: general – SubjectFull: Chronic pain Type: general – SubjectFull: Cellular signal transduction Type: general – SubjectFull: Pain medicine Type: general – SubjectFull: Ligands (Biochemistry) Type: general – SubjectFull: Opioid epidemic Type: general Titles: – TitleFull: Opioid Analgesics: Rise and Fall of Ligand Biased Signaling and Future Perspectives in the Quest for the Holy Grail. Type: main BibRelationships: HasContributorRelationships: – PersonEntity: Name: NameFull: Breault, Émile – PersonEntity: Name: NameFull: Brouillette, Rebecca L. – PersonEntity: Name: NameFull: Hébert, Terence E. – PersonEntity: Name: NameFull: Sarret, Philippe – PersonEntity: Name: NameFull: Besserer-Offroy, Élie IsPartOfRelationships: – BibEntity: Dates: – D: 01 M: 06 Text: Jun2025 Type: published Y: 2025 Identifiers: – Type: issn-print Value: 11727047 Numbering: – Type: volume Value: 39 – Type: issue Value: 6 Titles: – TitleFull: CNS Drugs Type: main |
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