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

Abstract

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
Pages211-230
Number of pages20
ISBN (Electronic)9780203025765
ISBN (Print)9780824740313
StatePublished - Jan 1 2003

ASJC Scopus subject areas

  • Neuroscience(all)
  • Health Professions(all)
  • Medicine(all)

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    Varga, E. V., Hosohata, K., Hosohata, Y., Tsang, J., Burkey, T., Alfaro-Lopez, J., Tang, X., Hruby, V. J., Roeske, W. R., & Yamamura, H. I. (2003). Inverse agonism at the delta opioid receptors. In The Delta Receptor (pp. 211-230). CRC Press.