Utilizing nature as a source of new probes for opioid pharmacology

Background: Traditional and current opioid pharmacology is fundamentally based on interactions between opioid receptors and compounds isolated from natural sources. Adverse effects associated with opioids have led to the search for compounds with diminished side effects. Discussion: Recent discoveries of non-nitrogenous and structurally diverse alkaloids as novel opioid ligands have led to renewed interest in the development of novel chemotypes for opioid receptors. Conclusion: The strong history of natural products as opioid receptor ligands suggests that nature is one of the most promising for the identification of novel opioids. This review highlights the vast potential of investigating natural products as novel probes of opioid receptors.