Sharif N A, Zuhowski E G, Burt D R
Neurosci Lett. 1983 Nov 11;41(3):301-6. doi: 10.1016/0304-3940(83)90467-6.
In screening neuroactive compounds for their possible interaction with rat thyrotropin-releasing hormone (TRH) receptors, some benzodiazepines were found to compete relatively potently for specific 3HTRH [( 3H]MeTRH) binding. The profile of activity (chlordiazepoxide greater than diazepam greater than flurazepam greater than lurazepam greater than flunitrazepam) was almost identical for washed pituitary, retina and amygdala preparations. Corresponding Ki values for the latter region were (microM): 0.33, 3.24, 17.4 for the 3 most active inhibitors. Other (47) neuroactive substances exhibited little activity on [3H]MeTRH binding. All benzodiazepines tested were competitive inhibitors in the three tissues. These data support previous evidence for a close similarity of TRH receptors in the pituitary gland and central nervous system, and invoke the possibility of TRH receptor-mediated effects for some benzodiazepines.
在筛选具有与大鼠促甲状腺激素释放激素（TRH）受体发生相互作用可能性的神经活性化合物时，发现某些苯二氮䓬类药物能相对有效地竞争特异性[3H](3 - 甲基 - 组氨酸2)TRH（[3H]MeTRH）结合。对于洗涤过的垂体、视网膜和杏仁核制剂，活性谱（氯氮䓬＞地西泮＞氟西泮＞氯甲西泮＞氟硝西泮）几乎相同。后一区域中三种活性最强抑制剂的相应Ki值（微摩尔）分别为：0.33、3.24、17.4。其他47种神经活性物质对[3H]MeTRH结合几乎没有活性。所测试的所有苯二氮䓬类药物在这三种组织中均为竞争性抑制剂。这些数据支持了垂体和中枢神经系统中TRH受体非常相似的先前证据，并提出某些苯二氮䓬类药物存在TRH受体介导效应的可能性。
