Bivalent and bitopic ligands of the opioid receptors: The prospects of a dual approach
Marie Emilie Hovah,
Ulrike Holzgrabe
Abstract: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 natu… Show more
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