IUPHAR review: Recent progress in the development of Mu opioid receptor modulators to treat opioid use disorders

Pagare, Piyusha P.; Flammia, Rachael; Zhang, Yan

doi:10.1016/j.phrs.2023.107023

Pharmacological Research

2024

DOI: 10.1016/j.phrs.2023.107023

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IUPHAR review: Recent progress in the development of Mu opioid receptor modulators to treat opioid use disorders

Piyusha P. Pagare,

Rachael Flammia,

Yan Zhang

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Bivalent and bitopic ligands of the opioid receptors: The prospects of a dual approach

Hovah,

Holzgrabe

2024

Medicinal Research Reviews

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Opioid receptors belonging to the class A G‐protein coupled receptors (GPCRs) are the targets of choice in the treatment of acute and chronic pain. However, their on‐target side effects such as respiratory depression, tolerance and addiction have led to the advent of the ‘opioid crisis’. In the search for safer analgesics, bivalent and more recently, bitopic ligands have emerged as valuable tool compounds to probe these receptors. The activity of bivalent and bitopic ligands rely greatly on the allosteric nature of the GPCRs. Bivalent ligands consist of two pharmacophores, each binding to the individual orthosteric binding site (OBS) of the monomers within a dimer. Bitopic or dualsteric ligands bridge the gap between the OBS and the spatially distinct, less conserved allosteric binding site (ABS) through the simultaneous occupation of these two sites. Bivalent and bitopic ligands stabilize distinct conformations of the receptors which ultimately translates into unique signalling and pharmacological profiles. Some of the interesting properties shown by these ligands include improved affinity and/or efficacy, subtype and/or functional selectivity and reduced side effects. This review aims at providing an overview of some of the bivalent and bitopic ligands of the opioid receptors and, their pharmacology in the hope of inspiring the design and discovery of the next generation of opioid analgesics.

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Bivalent and bitopic ligands of the opioid receptors: The prospects of a dual approach

Hovah,

Holzgrabe

2024

Medicinal Research Reviews

View full text Add to dashboard Cite

show abstract

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IUPHAR review: Recent progress in the development of Mu opioid receptor modulators to treat opioid use disorders

Cited by 1 publication

References 73 publications

Bivalent and bitopic ligands of the opioid receptors: The prospects of a dual approach

Bivalent and bitopic ligands of the opioid receptors: The prospects of a dual approach

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