Recovery of alpha 2-adrenoceptor binding and function after irreversible inactivation by N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline (EEDQ).
Recovery of alpha 2-adrenoceptor binding and function after irreversible inactivation by N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline (EEDQ).
复制标题
N-乙氧基羰基-2-乙氧基-1,2-二氢喹啉 (EEDQ) 不可逆失活后，α2-肾上腺素受体结合和功能恢复。
DOI：
10.1016/0014-2999(85)90200-6
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发表时间：
1985
影响因子：
5
通讯作者：
Goldstein,M
中科院分区：
文献类型：
--
作者：
Adler,CH;Meller,E;Goldstein,M
摘要N-乙氧羰基-2-乙氧基-1，2-二氢喹啉(EEDQ)处理大鼠后，大脑皮层[H]α2受体结合显著丧失([H]RX-781094)，α2激动剂UK-14,304抑制K+刺激的[H]NA和[3 H]5-羟色胺释放的能力显著降低。α2受体再聚集为单指数型，t1 2为4 1d，功能恢复也为单指数型，恢复α2对[3 H]NA和[3 H]5-HT释放的抑制作用的t1 2值分别为2.4和4.6d。其他研究表明，功能恢复率的差异可能反映了相对于异型受体，自体受体存在着大量的受体储备。
Abstract Treatment of rats with N-ethoxycarbonyl-2-ethoxy-1, 2-dihydroquinoline (EEDQ) resulted in a pronounced loss of α 2-adrenoceptor binding ([3 H] RX-781094) and a marked reduction in the ability of the α 2-agonist UK-14,304 to inhibit K+-stimulated release of both [3 H] NA and [3 H] 5-HT in cerebral cortex. Repopulation of α 2-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 α 2-mediated inhibition of [3 H] NA and [3 H] 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.