title: Multitarget opioid ligands in pain relief: New players in an old game.
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.
authors.affiliation: Department of Drug Sciences-Medicinal Chemistry Section, University of Catania, Viale A. Doria 6, 95125 Catania, Italy. Electronic address: rita.turnaturi@tiscali.it.
authors.forename: Rita
authors.initials: R
authors.lastname: Turnaturi
authors.affiliation: Department of Drug Sciences-Medicinal Chemistry Section, University of Catania, Viale A. Doria 6, 95125 Catania, Italy.
authors.forename: Giuseppina
authors.initials: G
authors.lastname: Aricò
authors.affiliation: Department of Drug Sciences-Medicinal Chemistry Section, University of Catania, Viale A. Doria 6, 95125 Catania, Italy.
authors.forename: Giuseppe
authors.initials: G
authors.lastname: Ronsisvalle
authors.affiliation: Department of Drug Sciences-Pharmacology and Toxicology Section, University of Catania, Viale A. Doria 6, 95125 Catania, Italy.
authors.forename: Carmela
authors.initials: C
authors.lastname: Parenti
authors.affiliation: Department of Drug Sciences-Medicinal Chemistry Section, University of Catania, Viale A. Doria 6, 95125 Catania, Italy.
authors.forename: Lorella
authors.initials: L
authors.lastname: Pasquinucci
mesh_terms: D000701:Analgesics, Opioid / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D000818:Animals; D006801:Humans; D008024:Ligands; D015394:Molecular Structure; D010146:Pain / Q000188:drug therapy*; D011957:Receptors, Opioid / Q000819:agonists*
chemical_list: D000701:Analgesics, Opioid; D008024:Ligands; D011957:Receptors, Opioid
keywords: Bifunctional ligands; Bivalent ligands; DOR; KOR; MOR; Pain