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长期使用氯硝西泮后在生理温度下苯二氮䓬受体亲和力的改变。

Benzodiazepine receptor affinity alterations at physiologic temperature after chronic clonazepam exposure.

作者信息

Sher P K, Machen V L

出版信息

Brain Dev. 1987;9(1):33-6. doi: 10.1016/s0387-7604(87)80007-4.

DOI:10.1016/s0387-7604(87)80007-4
PMID:3037933
Abstract

Cerebral cortical cell cultures obtained from fetal mice were exposed to 200 nM clonazepam (CZP) for 14 days and benzodiazepine (BDZ) receptor binding was measured on intact cells in situ at 37 degrees C. Total, specific, and CZP-displaceable BDZ binding were significantly reduced from control values immediately after drug removal (77.7 +/- 1.4%, 75.1 +/- 3.0%, and 40.9 +/- 6.0% of control, respectively) but Ro5-4864-displaceable binding was not affected (87.6 +/- 5.1%). Binding returned to control values within 48 hours. Saturation analysis of the binding data indicated that a high-affinity binding site could not be detected in CZP-exposed cultures immediately after drug removal (162 nM versus 49 nM in controls, p less than .001), but was present 24 hours later.

摘要

从胎鼠获取的大脑皮质细胞培养物被暴露于200 nM氯硝西泮(CZP)中14天,并于37摄氏度在原位完整细胞上测量苯二氮䓬(BDZ)受体结合情况。在移除药物后立即发现,总的、特异性的以及可被CZP置换的BDZ结合与对照值相比显著降低(分别为对照的77.7±1.4%、75.1±3.0%和40.9±6.0%),但可被Ro5 - 4864置换的结合不受影响(87.6±5.1%)。结合在48小时内恢复到对照值。对结合数据的饱和分析表明,在移除药物后立即在暴露于CZP的培养物中无法检测到高亲和力结合位点(对照中为49 nM,而此处为162 nM,p <.001),但在24小时后存在。

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