Hruska R E, Silbergeld E K
J Neurochem. 1980 Sep;35(3):750-2. doi: 10.1111/j.1471-4159.1980.tb03718.x.
The in vitro addition of ethanol at concentrations greater than 0.2% produced an inhibition of [3H]spiroperidol binding. This inhibition was competitive, lowering the affinity without altering the maximum number of sites. Both the rates of association and dissociation were altered such that the ligand spent less time attached to the receptor. Since the binding was competitive, little inhibition was seen at ligand concentrations greater than 300 pM. These results are important for in vitro studies when drugs are dissolved in ethanol, and also for in vivo studies on the effects of ethanol.
在体外添加浓度大于0.2%的乙醇会抑制[3H]螺哌啶醇的结合。这种抑制是竞争性的，降低了亲和力但不改变最大结合位点数。结合和解离速率均发生改变，使得配体与受体结合的时间减少。由于这种结合是竞争性的，在配体浓度大于300 pM时几乎看不到抑制作用。这些结果对于药物溶解于乙醇中的体外研究以及乙醇作用的体内研究都很重要。
