The efficacy of δ-opioid receptor-selective drugs

T. H. Burkey, F. J. Ehlert, Y. Hosohata, R. M. Quock, S. Cowell, K. Hosohata, E. Varga, D. Stropova, X. Li, C. Slate, H. Nagase, F. Porreca, V. J. Hruby, W. R. Roeske, H. I. Yamamura

Research output: Contribution to journalArticle

12 Scopus citations

Abstract

δ-Opioid receptor-selective drugs may provide an alternative to μ- opioid-selective drugs currently used for the relief of pain. To develop improved δ-opioid receptor-selective drugs, better measures of drug activity are necessary. In this review we suggest that efficacy calculations provide a superior measure of drug activity as compared to dissociation constants and drug potencies in functional assays. Efficacy, as discussed in this review, is defined as a quantitative measurement of the ability of a drug to stimulate second messenger systems or measurable functional responses in cells or tissues under standard conditions. Efficacy values will allow medicinal chemists to understand the contributions of both the coupling efficiency and dissociation constant to drug potencies in the development of new δ-opioid receptor-selective drugs.

Original languageEnglish (US)
Pages (from-to)1531-1536
Number of pages6
JournalLife Sciences
Volume62
Issue number17-18
DOIs
StatePublished - Mar 27 1998

Keywords

  • Drug efficacy
  • Vas deferens
  • δ-opioid receptor

ASJC Scopus subject areas

  • Biochemistry, Genetics and Molecular Biology(all)
  • Pharmacology, Toxicology and Pharmaceutics(all)

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  • Cite this

    Burkey, T. H., Ehlert, F. J., Hosohata, Y., Quock, R. M., Cowell, S., Hosohata, K., Varga, E., Stropova, D., Li, X., Slate, C., Nagase, H., Porreca, F., Hruby, V. J., Roeske, W. R., & Yamamura, H. I. (1998). The efficacy of δ-opioid receptor-selective drugs. Life Sciences, 62(17-18), 1531-1536. https://doi.org/10.1016/S0024-3205(98)00102-7