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. 1979;7(Suppl 3):273S–279S. doi: 10.1111/j.1365-2125.1979.tb04700.x

History and development of mixed opioid agonists, partial agonists and antagonists

W R Martin
PMCID: PMC1429308  PMID: 380616

Abstract

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.

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Selected References

These references are in PubMed. This may not be the complete list of references from this article.

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