Opioids pp 279-293 | Cite as

Selective Nonpeptide Opioid Antagonists

  • P. S. Portoghese
Part of the Handbook of Experimental Pharmacology book series (HEP, volume 104 / 1)


Opioid antagonists have been indispensable as tools in opioid research (Zimmerman and Leander 1990). In fact, the chief criterion for the classification of an agonist effect as opioid receptor-mediated is the ability of naloxone (Sawynok et al. 1979) or naltrexone (Gold et al. 1982) to reversibly antagonize this effect in a competitive fashion. The usefulness of these ligands for this purpose stems from the fact that they are universal opioid antagonists; that is, they are capable of antagonizing the agonist effects mediated by multiple opioid receptor types.


Opioid Receptor Opioid Peptide Opioid Antagonist Opioid Agonist Opioid Receptor Antagonist 
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© Springer-Verlag Berlin Heidelberg 1993

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  • P. S. Portoghese

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