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.
- Irreversible receptor inactivation
- [H]5-HT release
- [H]NA release
- [H]RX-781094 binding
ASJC Scopus subject areas