Inverse agonism at the delta opioid receptors

Eva V. Varga, Keiko Hosohata, Yoshiaki Hosohata, Jennifer Tsang, Thomas Burkey, Josue Alfaro-Lopez, Xuejun Tang, Victor J. Hruby, William R. Roeske, Henry I. Yamamura

Research output: Chapter in Book/Report/Conference proceedingChapter

1 Scopus citations


According to the traditional concept of agonist activity, agonist occupation of the receptor is a fundamental condition of receptor activation [1]. The ternary complex model furthermore postulates that in order to produce a cellular response, the agonist-receptor complex should interact with a third, guanine nucleotide-sensitive binding partner (guanine nucleotide binding, or G protein) [2]. According to this classical concept, two classes of physiologically active ligands can be anticipated: agonists, and competitive antagonists. Synthetic agonists are thought to interact with the receptors the same way as endogenous hormones, and produce identical physiological response (the '‘pharmacophore’' concept, reviewed in [3]. Competitive antagonists share the receptor binding site with agonists, but are not able to promote the formation of the ternary complex. Therefore, competitive antagonists pro-duce physiological response by competing with the endogenous agonist for the common receptor binding site.

Original languageEnglish (US)
Title of host publicationThe Delta Receptor
PublisherCRC Press
Number of pages20
ISBN (Electronic)9780203025765
ISBN (Print)9780824740313
StatePublished - Jan 1 2003

ASJC Scopus subject areas

  • General Neuroscience
  • General Health Professions
  • General Medicine


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