title: Non-peptidic δ opioid receptor agonists and antagonists (2000 - 2012).
abstract: BACKGROUND
  The δ opioid receptor mediates various pharmacological effects such as antinociceptive and antidepressant effects, whereas it does not appear to induce μ opioid-like side effects such as dependence, respiratory depression and constipation. Therefore, the δ opioid receptor is a promising drug target.
  
  
  METHODS
  This review covers literature and patents concerning non-peptidic δ opioid receptor agonists, antagonists, modulators and ligands from 2000 to 2012. Pharmacological effects induced by δ receptor agonists or antagonists are also discussed.
  
  
  CONCLUSIONS
  Potential therapeutic effects by δ receptor agonists are antinociceptive, antidepressant, anxiolytic, cardioprotective and neuroprotective effects. Among them, anxiolytic effects are of particular interest because the anxiolytic effects by a δ receptor agonist have been observed in humans. Although non-peptidic δ receptor agonists were reported to show convulsive effects via the δ opioid receptor, some δ receptor agonists are known to produce no convulsive behaviors. Therefore, it may be possible to eliminate convulsion induced by a δ receptor agonist. Many δ receptor antagonists were also reported but there is little new information about pharmacological effects by a δ receptor antagonist. Although detailed results were not revealed, two δ receptor antagonists with μ receptor agonistic or antagonistic properties are in the late stages of the clinical trial.
authors.affiliation: Kitasato University, School of Pharmacy, 5-9-1, Shirokane, Minato-ku, Tokyo, 108-8641, Japan.
authors.forename: Hideaki
authors.initials: H
authors.lastname: Fujii
authors.forename: Toshihiro
authors.initials: T
authors.lastname: Takahashi
authors.forename: Hiroshi
authors.initials: H
authors.lastname: Nagase
mesh_terms: D000701:Analgesics, Opioid / Q000009:adverse effects / Q000494:pharmacology; D000818:Animals; D002986:Clinical Trials as Topic; D015195:Drug Design; D006801:Humans; D058990:Molecular Targeted Therapy; D010330:Patents as Topic; D017465:Receptors, Opioid, delta / Q000819:agonists* / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D000701:Analgesics, Opioid; D017465:Receptors, Opioid, delta