Recovery of alpha 2-adrenoceptor binding and function after irreversible inactivation by N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline (EEDQ).
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.
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D000317:Adrenergic alpha-Antagonists / Q000494:pharmacology*; D000818:Animals; D002540:Cerebral Cortex / Q000378:metabolism; D004146:Dioxanes / Q000494:pharmacology; D019329:Idazoxan; D066298:In Vitro Techniques; D007700:Kinetics; D008297:Male; D009638:Norepinephrine / Q000378:metabolism; D011804:Quinolines / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains; D011942:Receptors, Adrenergic, alpha / Q000187:drug effects*; D012701:Serotonin / Q000378:metabolism
D000317:Adrenergic alpha-Antagonists; D004146:Dioxanes; D011804:Quinolines; D011942:Receptors, Adrenergic, alpha; D012701:Serotonin; C000470:EEDQ; D009638:Norepinephrine; D019329:Idazoxan