Tolerance during chronic benzodiazepine treatment associated with decreased receptor binding.
Tolerance during chronic benzodiazepine treatment associated with decreased receptor binding.
复制标题
慢性苯二氮卓治疗期间的耐受性与受体结合减少相关。
DOI：
10.1016/0014-2999(81)90356-3
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发表时间：
1981
影响因子：
5
通讯作者：
Chiu,TH
中科院分区：
文献类型：
--
作者：
Rosenberg,HC;Chiu,TH
进行研究以评估慢性治疗期间发生的特异性苯二氮平结合变化的时间过程和可能的意义。给大鼠提供糖精溶液中的氟拉西泮作为其唯一的液体供应。每只大鼠每天消耗100-150毫克/公斤。这种处理对氟硝西泮特异性[3H]结合常数（KD）没有影响。最大结合能力（Bmax）在治疗4周或8周后下降约20%，但在2周或更短时间内没有下降。慢性治疗结束后24 h内bmax恢复正常。通过注射20 ~ 200 mg/kg，检测大鼠对氟西泮的敏感性，并评估运动障碍。剂量-反应分析显示，仅在治疗后和bmax降低时才有耐受性。结果表明，bmax的减少是对慢性苯二氮卓类药物治疗的适应性变化，其耐受性的机制是受体的减少。
Studies were performed to evaluate the time course and possible significance of changes in specific benzodiazephine binding that occur during chronic treatment. Rats were offered flurazepam in a saccharin solution as their only fluid supply. Each rat consumed 100–150 mg/kg daily. Such treatment produced no change in the binding constant (KD) of specific [3H]flunitrazepam binding. Maximal binding capacity (Bmax) was reduced by about 20% after 4 or 8 weeks of treatment, but not by 2 weeks or less. Bmaxreturned to control within 24 h after the end of chronic treatment. Rats were tested for suceptibility to flurazepam by injecting 20–200 mg/kg i.p., and assessing locomotor impairment. Dose-response analysis showed tolerance only after treatments and at times when Bmaxwas reduced. The results suggest that the reduced Bmaxis an adaptive change in response to chronic benzodiazepine treatment, and that the mechanism for tolerance is a reduction of receptors.
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