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History and development of mixed opioid agonists, partial agonists and antagonists.
Author(s) -
Martin WR
Publication year - 1979
Publication title -
british journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.216
H-Index - 146
eISSN - 1365-2125
pISSN - 0306-5251
DOI - 10.1111/j.1365-2125.1979.tb04700.x
Subject(s) - nalorphine , partial agonist , agonist , pentazocine , pharmacology , κ opioid receptor , opioid , medicine , (+) naloxone , morphine , chemistry , receptor
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 (mu, kappa and sigma) is required to rationalize the pharmacology of the antagonists 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 kappa‐partial agonist, nalorphine and the mu‐partial agonist buprenorphine are outlined.