EFFECT OF AN IMIDAZOBENZODIAZEPINE, RO15-4513, ON THE INCOORDINATION AND HYPOTHERMIA PRODUCED BY ETHANOL AND PENTOBARBITAL
EFFECT OF AN IMIDAZOBENZODIAZEPINE, RO15-4513, ON THE INCOORDINATION AND HYPOTHERMIA PRODUCED BY ETHANOL AND PENTOBARBITAL
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DOI：
10.1016/0024-3205(87)90415-2
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发表时间：
1987-08-03
期刊：
影响因子：
6.1
通讯作者：
PAUL, SM
中科院分区：
文献类型：
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作者：
HOFFMAN, PL;TABAKOFF, B;PAUL, SM
咪唑苯并二氮类药物Ro15-4513是脑部苯二氮卓受体的部分反向激动剂，它逆转了乙醇在小鼠体内的不协调效应，在加速旋转棒上进行了测量。这种作用可被苯二氮卓类受体拮抗剂阻断。相反，Ro15-4513对乙醇诱导的小鼠体温下降没有影响。然而，Ro15-4513逆转了戊巴比妥的降温作用，并且在较高剂量时也逆转了戊巴比妥对小鼠的不协调作用。这些数据支持这样的假设，即乙醇的某些药理作用是通过GABA-苯二氮卓类受体偶联氯离子通道的作用而介导的。
The imidazobenzodiazepine, Ro15-4513, which is a partial inverse agonist at brain benzodiazepine receptors, reversed the incoordinating effect of ethanol in mice, as measured on an accelerating Rotarod. This effect was blocked by benzodiazepine receptor antagonists. In contrast, Ro15-4513 had no effect on ethanol-induced hypothermia in mice. However, Ro15-4513 reversed the hypothermic effect of pentobarbital, and, at a higher dose also reversed the incoordinating effect of pentobarbital in mice. The data support the hypothesis that certain of the pharmacological effects of ethanol are mediated by actions at the GABA-benzodiazepine receptor-coupled chloride channel.