Skerritt J H, Johnston G A
Neurosci Lett. 1983 Aug 8;38(3):315-20. doi: 10.1016/0304-3940(83)90388-9.
Diazepam (10-1000 nM) enhanced the binding of [3H]GABA and of the monocyclic GABA agonist [3H]muscimol, but failed to alter binding of the bicyclic GABA agonist [3H]THIP to fresh, well washed rat brain membranes incubated at 2 degrees C. Although stimulation of [3H]diazepam binding by THIP was observed at higher incubation temperatures and in the presence of chloride ions, these measures did not induce a corresponding enhancement of [3H]THIP binding by diazepam. These results extend earlier observations of the unusual behavior of THIP as a selective GABA agonist, and emphasize that enhancement of benzodiazepine binding by GABA agonists is not necessarily reflected in a complementary manner by any action of benzodiazepines on the binding of GABA agonists.
地西泮（10 - 1000纳摩尔）增强了[³H]γ-氨基丁酸（GABA）和单环GABA激动剂[³H]蝇蕈醇的结合，但在2℃下孵育的新鲜、充分洗涤的大鼠脑膜中，未能改变双环GABA激动剂[³H]4,5,6,7-四氢异喹啉-3-醇（THIP）的结合。尽管在较高孵育温度和存在氯离子的情况下观察到THIP对[³H]地西泮结合的刺激作用，但这些措施并未诱导地西泮对[³H]THIP结合产生相应增强。这些结果扩展了早期关于THIP作为选择性GABA激动剂的异常行为的观察，并强调GABA激动剂对地西泮结合的增强不一定以互补方式反映在苯二氮䓬类药物对GABA激动剂结合的任何作用上。
