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Eur J Med Chem. 2016 Jan 27;108:211-228. doi: 10.1016/j.ejmech.2015.11.028. Epub 2015 Nov 22.

Multitarget opioid ligands in pain relief: New players in an old game.

Author information

1
Department of Drug Sciences-Medicinal Chemistry Section, University of Catania, Viale A. Doria 6, 95125 Catania, Italy. Electronic address: rita.turnaturi@tiscali.it.
2
Department of Drug Sciences-Medicinal Chemistry Section, University of Catania, Viale A. Doria 6, 95125 Catania, Italy.
3
Department of Drug Sciences-Pharmacology and Toxicology Section, University of Catania, Viale A. Doria 6, 95125 Catania, Italy.

Abstract

Still nowadays pain is one of the most common disabling conditions and yet it remains too often unsolved. Analgesic opioid drugs, and mainly MOR agonists such as morphine, are broadly employed for pain management. MOR activation, however, has been seen to cause not only analgesia but also undesired side effects. A potential pain treatment option is represented by the simultaneous targeting of different opioid receptors. In fact, ligands possessing multitarget capabilities led to an improved pharmacological fingerprint. This review focuses on the examination of multitarget opioid ligands which have been distinguished in peptide and non-peptide and further listed as bivalent and bifunctional ligands. Moreover, the potential of these compounds, both as analgesic drugs and pharmacological tools to explore heteromer receptors, has been stressed.

KEYWORDS:

Bifunctional ligands; Bivalent ligands; DOR; KOR; MOR; Pain

PMID:
26656913
DOI:
10.1016/j.ejmech.2015.11.028
[Indexed for MEDLINE]

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