药物给药及撤药对苯二氮䓬受体的急性效应。
Acute effects of drug administration and withdrawal on the benzodiazepine receptor.
作者信息
Scharf M B, Feil P
出版信息
Life Sci. 1983 Apr 11;32(15):1771-7. doi: 10.1016/0024-3205(83)90841-x.
Effects of one week of benzodiazepine drug administration on central benzodiazepine receptor binding characteristics were evaluated in a series of experiments in male Sprague-Dawley rats. Administration of short- and intermediate-acting benzodiazepines was observed to increase the number of available receptor binding sites (Bmax) without changing affinity of drug for receptor. Furthermore, these changes did not occur after administration and withdrawal of long-acting benzodiazepines. In addition, there appeared to be a relationship between the affinity of the different benzodiazepines for the receptor and the degree of increase in the number of receptor binding sites. The results may help to explain the relationship between withdrawal of certain benzodiazepine drugs and the occurrence of rebound phenomena in clinical situations.
在一系列针对雄性斯普拉格-道利大鼠的实验中，评估了一周苯二氮䓬类药物给药对中枢苯二氮䓬受体结合特性的影响。观察到短效和中效苯二氮䓬类药物的给药增加了可用受体结合位点的数量（Bmax），而不改变药物对受体的亲和力。此外，长效苯二氮䓬类药物给药和撤药后未出现这些变化。另外，不同苯二氮䓬类药物对受体的亲和力与受体结合位点数量增加的程度之间似乎存在关联。这些结果可能有助于解释临床情况下某些苯二氮䓬类药物撤药与反弹现象发生之间的关系。
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