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Papers of the Week

Papers: 9 Mar 2019 - 15 Mar 2019

Pharmacology/Drug Development

2019 Jun



Bifunctional opioid receptor ligands as novel analgesics.


Cunningham CW, Elballa WM, Vold SU
Neuropharmacology. 2019 Jun; 151:195-207.
PMID: 30858102.


Prolonged treatment of chronic severe pain with opioid analgesics is frought with problematic adverse effects including tolerance, dependence, and life-threatening respiratory depression. Though these effects are mediated predominately through preferential activation of μ opioid peptide (μOP) receptors, there is an emerging appreciation that actions at κOP and δOP receptors contribute to the observed pharmacologic and behavioral profile of μOP receptor agonists and may be targeted simultaneously to afford improved analgesic effects. Recent developments have also identified the related nociceptin opioid peptide (NOP) receptor as a key modulator of the effects of μOP receptor signaling. We review here the available literature describing OP neurotransmitter systems and highlight recent drug and probe design strategies.