给大鼠体内注射艾司唑仑后，脑内苯二氮䓬受体数量增加。
Increased number of brain benzodiazepine receptors after in-vivo administration of estazolam to rats.
作者信息
Mennini T, Gobbi M, Garattini S
出版信息
J Pharm Pharmacol. 1984 Sep;36(9):621-2. doi: 10.1111/j.2042-7158.1984.tb04911.x.
Abstract
Estazolam significantly increased the Kd of [3H]flunitrazepam in-vitro, like other benzodiazepines (BDZs) acting competitively at the receptor site. At variance with other BDZs, estazolam significantly raised the Bmax for [3H]flunitrazepam, at concentrations lower than its Ki for BDZ receptors. This effect may be responsible for the observed increase in [3H]diazepam binding after in-vivo administration of estazolam to rats.
摘要
与其他在受体位点竞争性作用的苯二氮䓬类药物（BDZs）一样，艾司唑仑在体外显著增加了[³H]氟硝西泮的解离常数（Kd）。与其他BDZs不同的是，在低于其对BDZ受体的抑制常数（Ki）的浓度下，艾司唑仑显著提高了[³H]氟硝西泮的最大结合容量（Bmax）。这种效应可能是大鼠体内给予艾司唑仑后观察到的[³H]地西泮结合增加的原因。
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