Recovery of α2-adrenoceptor binding and function after irreversible inactivation by N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline (EEDQ)

C. H. Adler, E. Meller, M. Goldstein

Research output: Contribution to journalArticle

41 Scopus citations

Abstract

Treatment of rats with N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline (EEDQ) resulted in a pronounced loss of α2-adrenoceptor binding ([3H]RX-781094) and a marked reduction in the ability of the α2-agonist UK-14,304 to inhibit K+-stimulated release of both [3H]NA and [3H]5-HT in cerebral cortex. Repopulation of α2-anderoceptors was monoexponential with a t 1 2 of 4.1 days; functional recovery was also monoexponential, with t 1 2 values of 2.4 and 4.6 days for restoration of α2-mediated inhibition of [3H]NA and [3H]5-HT release, respectively. Other studies suggest the difference in functional recovery rate may reflect the presence of a large receptor reserve for autoreceptors relative to heteroreceptors.

Original languageEnglish (US)
Pages (from-to)175-178
Number of pages4
JournalEuropean Journal of Pharmacology
Volume116
Issue number1-2
DOIs
StatePublished - Oct 8 1985

Keywords

  • Irreversible receptor inactivation
  • N-Ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline
  • [H]5-HT release
  • [H]NA release
  • [H]RX-781094 binding
  • α-Receptors

ASJC Scopus subject areas

  • Pharmacology

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