Chronic clonazepam administration induced benzodiazepine receptor subsensitivity

Chronic clonazepam administration induced benzodiazepine receptor subsensitivity
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长期服用氯硝西泮可引起苯二氮卓受体不敏感

DOI:
10.1016/0028-3908(82)90216-7
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发表时间:
1982
期刊:
影响因子:
4.7
通讯作者:
F. Goodwin
F. Goodwin
中科院分区:
医学2区
文献类型:
--
作者:
J. Crawley;P. Marangos;J. Stivers;F. Goodwin

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Clonazepam and chlordiazepoxide were administered chronically in increasing doses for three weeks in two different strains of mice. Forebrain [3H]diazepam binding was assayed in groups of mice sacrified at 2, 26, 50 hr and 10 days following the last dose. Scatchard and single point analyses revealed a significant decrease in the number of [3H]diazepam binding sites [Bmax] which persisted for at least two days following chronic clonazepam treatment. TheBmaxchanges observed following chlordiazepoxide treatment were less pronounced than those elicited by clonazepam. No significant changes in receptor binding affinity (Kd) were detected with either drug. In the clonazepam-treated animals,Bmaxvalues returned to normal by day 10 after drug treatment. Chronic benzodiazepine administration therefore induced a decrease in the apparent number of benzodiazepine binding sites in the mouse forebrain. The magnitude and duration of the observed subsensitivity appears to depend on the potency of the administered benzodiazepine.