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1 A brief history of the development of narcotic antagonists is outlined.
2 The clinical and pharmacological observations leading to the discovery of dualism of opiate receptors are reviewed.
3 An extension of this theory to a three-receptor model (μ, χ and σ) is required to rationalize the pharmacology of the antagonist analgesics cyclazocine, pentazocine and nalorphine.
4 The methodologies available for the study of compounds with dual agonist-antagonist activity are discussed in the light of the above receptor multiplicity, and data appertaining to the χ-partial agonist, nalorphine and the μ-partial agonist buprenorphine are outlined.