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Front Pharmacol. 2018 Aug 31;9:1002. doi: 10.3389/fphar.2018.01002. eCollection 2018.

[No title available]

Frontiers in pharmacology

Roberta Lattanzi, Silvia Rief, Helmut Schmidhammer, Lucia Negri, Mariana Spetea

Affiliations

  1. Department of Physiology and Pharmacology "Vittorio Erspamer," Sapienza University of Rome, Rome, Italy.
  2. Department of Pharmaceutical Chemistry, Institute of Pharmacy and Center for Molecular Biosciences Innsbruck, University of Innsbruck, Innsbruck, Austria.

PMID: 30233377 PMCID: PMC6127270 DOI: 10.3389/fphar.2018.01002

Abstract

Pain, particularly chronic pain, is still an unsolved medical condition. Central goals in pain control are to provide analgesia of adequate efficacy and to reduce complications associated with the currently available drugs. Opioids are the mainstay for the treatment of moderate to severe pain. However, opioid pain medications also cause detrimental side effects, thus highlighting the need of innovative and safer analgesics. Opioids mediate their actions via the activation of opioid receptors, with the mu-opioid receptor as the primary target for analgesia, but also for side effects. One long-standing focus of drug discovery is the pursuit for new opioids exhibiting a favorable dissociation between analgesia and adverse effects. In this study, we describe the

Keywords: analgesia; binding affinity; constipation; morphinans; opioid agonist; opioid receptor; pain

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