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

Eur J Pharmacol. 1985 Oct 8;116(1-2):175-8. doi: 10.1016/0014-2999(85)90200-6.


Treatment of rats with N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline (EEDQ) resulted in a pronounced loss of alpha 2-adrenoceptor binding ( [3H]RX-781094) and a marked reduction in the ability of the alpha 2-agonist UK-14,304 to inhibit K+-stimulated release of both [3H]NA and [3H]5-HT in cerebral cortex. Repopulation of alpha 2-adrenoceptors was monoexponential with a t1/2 of 4.1 days; functional recovery was also monoexponential, with t1/2 values of 2.4 and 4.6 days for restoration of alpha 2-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.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Adrenergic alpha-Antagonists / pharmacology*
  • Animals
  • Cerebral Cortex / metabolism
  • Dioxanes / pharmacology
  • Idazoxan
  • In Vitro Techniques
  • Kinetics
  • Male
  • Norepinephrine / metabolism
  • Quinolines / pharmacology*
  • Rats
  • Rats, Inbred Strains
  • Receptors, Adrenergic, alpha / drug effects*
  • Serotonin / metabolism


  • Adrenergic alpha-Antagonists
  • Dioxanes
  • Quinolines
  • Receptors, Adrenergic, alpha
  • Serotonin
  • EEDQ
  • Norepinephrine
  • Idazoxan