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Structure-Activity Relationships of Synthetic and Semisynthetic Opioid Agonists and Antagonists
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1995
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Medicinal ChemistryBiochemistryMedicineNatural SciencesMechanism Of ActionOpioid Use DisorderStructure-activity RelationshipsNeuropharmacologyPharmacological AgentTor ModelsPharmacotherapySemisynthetic 4,5ASynthetic MorphinansPharmacologyAnesthetic PharmacologyDrug Discovery
This paper surveys the relationships between the chemical structures and pharmacological activities of natural or semisynthetic 4,5a epoxymorphinans, synthetic morphinans and benzomorphans. Substitution . of the N-methyl group affords strong analgesics, opioid antagonists and mixed agonist-antagonists respectively. The role of opioid agonists and antagonists in the development of opioid receJ:>tor models is also discussed.