Becker H C
Veterans Administration Medical Center, Charleston, SC.
Life Sci. 1988;43(7):643-50. doi: 10.1016/0024-3205(88)90069-0.
The purpose of this study was to investigate the effects of the imidazobenzodiazepine RO15-4513, a partial inverse agonist at benzodiazepine (BDZ) receptors, on the stimulant and depressant actions of ethanol in mice. For comparative purposes, another BDZ inverse agonist, FG-7142, was examined as well. Neither RO15-4513 nor FG-7142 influenced the low-dose excitatory effects of ethanol on spontaneous locomotor activity. However, both RO15-4513 and FG-7142 significantly antagonized the depressant effects of ethanol, and this antagonism was completely reversed by pretreatment with the BDZ receptor antagonist, RO15-1788. These data suggest that RO15-4513 is capable of antagonizing only some of the behavioral effects of ethanol, and in particular, those responses to ethanol that are mediated by modulation of the GABA/BDZ-chloride channel receptor complex.
本研究的目的是调查苯二氮䓬（BDZ）受体部分反向激动剂咪唑并苯二氮䓬RO15 - 4513对乙醇在小鼠体内的兴奋和抑制作用的影响。为作比较，还检测了另一种BDZ反向激动剂FG - 7142。RO15 - 4513和FG - 7142均未影响乙醇对自发运动活性的低剂量兴奋作用。然而，RO15 - 4513和FG - 7142均显著拮抗乙醇的抑制作用，且这种拮抗作用可被BDZ受体拮抗剂RO15 - 1788预处理完全逆转。这些数据表明，RO15 - 4513仅能拮抗乙醇的某些行为效应，尤其是那些通过γ-氨基丁酸/苯二氮䓬-氯化物通道受体复合物调节介导的对乙醇的反应。
