The opiate receptor

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8 Scopus citations


This review summarizes the evidence for specific opiate receptor binding. The author reports that affinity for receptor binding of the many opiates closely parallels their pharmacological potency. He suggests that receptor affinity alone can account for the potency of the opiate agonist drugs. He finds that opiate receptor binding is recovered primarily in the synaptic membrane fraction but cautions against drawing conclusions. Techniques for separating presynaptic and postsynaptic membranes should make further studies possible. He has mapped regional variations and opiate receptor binding in more than 40 areas of the rhesus monkey brain. In a variety of vertebrates examined, he detected substantial amounts of opiate receptor binding but could find very little in 9 different invertebrates. He suggests that it is possible to predict the pharmacological properties of different opiates based on differences between their receptor interactions and the presence or absence of sodium. This affords a rapid inexpensive screen for drugs that might be of mixed agonist antagonist, nonaddicting, analgesic action. He reports that while addicted animals are subsensitive to the agonists, they are hypersensitive to the antagonist. He postulates that the tolerance and physical dependence are associated with a change of the receptor with an increase in the antagonist form. (De Boer - Grand Forks, N. Dak.)

Original languageEnglish (US)
Pages (from-to)1-27
Number of pages27
JournalNeurosciences Research Program Bulletin
Issue number3 Sup.
StatePublished - Dec 1 1975

ASJC Scopus subject areas

  • General Medicine


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